fbpx
Wikipedia

5-HT receptor

January 01, 1970

5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems.[1][2][3] They mediate both excitatory and inhibitory neurotransmission. The serotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The 5-HT1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation

The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.[4]

Serotonin receptors are found in almost all animals and are even known to regulate longevity and behavioral aging in the primitive nematode, Caenorhabditis elegans.[5][6]

Classification edit

5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors are found in the central and peripheral nervous systems.[1][2] They can be divided into 7 families of G protein-coupled receptors which activate an intracellular second messenger cascade to produce an excitatory or inhibitory response. The exception to this is the 5-HT3 receptor which is a ligand-gated ion channel. In 2014, a novel 5-HT receptor was isolated from the small white butterfly, Pieris rapae, and named pr5-HT8. It does not occur in mammals and shares relatively low similarity to the known 5-HT receptor classes.[7]

Families edit

Family Type Mechanism Potential
5-HT1 Gi/Go-protein coupled. Decreasing cellular levels of cAMP. Inhibitory
5-HT2 Gq/G11-protein coupled. Increasing cellular levels of IP3 and DAG. Excitatory
5-HT3 Ligand-gated Na+ and K+ cation channel. Depolarizing plasma membrane. Excitatory
5-HT4 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT5 Gi/Go-protein coupled.[8] Decreasing cellular levels of cAMP. Inhibitory
5-HT6 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT7 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory

Subtypes edit

The 7 general serotonin receptor classes include a total of 14 known serotonin receptors.[9] The 15th receptor 5-HT1P has been distinguished on the basis of functional and radioligand binding studies, its existence has never been definitely affirmed or refuted.[10][11] The specific types have been characterized as follows:[12][13][14]

Information on serotonin receptors (human isoforms if nothing else is stated)
Receptor First cloned – PDB entries Gene(s) Distribution Function Agonists Antagonists Uses of drugs that act on this receptor
Blood vessels CNS GI Tract Platelets PNS Smooth Muscle
5-HT1A 1987 –
  • 7e2x
  • 7e2y
  • 7e2z

 

  • HTR1A
 Yes Yes No No No No

Selective (for 5-HT1A over other 5-HT receptors)

Nonselective

5-HT1B 1992 –
  • 6g79
  • HTR1B
 Yes Yes No No No No
5-HT1D 1991 –
  • 7e32

 

  • HTR1D
 Yes Yes No No No No
5-HT1E 1992 –
  • 7e33

 

  • HTR1E
 Yes Yes No No No No
  • None known
5-HT1F 1993 –
  • 7exd

 

  • HTR1F
 No Yes No No No No
  • Migraine
  • None known
5-HT1P Not cloned No No Yes No No No
  • None known
5-HT2A 1988
  • HTR2A
 Yes Yes Yes Yes Yes Yes
  • Addiction (potentially modulating)[54]
  • Anxiety[55]
  • Appetite
  • Cognition
  • Imagination
  • Learning
  • Memory
  • Mood
  • Perception
  • Sexual Behavior[56]
  • Sleep[57]
  • Thermoregulation[58]
  • Vasoconstriction[59]
5-HT2B 1992
  • HTR2B
 Yes Yes Yes Yes Yes Yes
5-HT2C 1988
  • HTR2C
 Yes Yes Yes Yes Yes Yes
5-HT3 1993
  • HTR3A
  • HTR3B
  • HTR3C
  • HTR3D
  • HTR3E
 No Yes Yes No Yes No
  • Addiction
  • Anxiety
  • Emesis
  • GI Motility[77]
  • Learning[78]
  • Memory[78]
  • Nausea
5-HT4 1995
  • HTR4
 No Yes Yes No Yes No
5-HT5A 1994
  • 7UM4
  • 7UM5
  • 7UM6
  • 7UM7
  • HTR5A
 No Yes No No No No
  • None thus far
5-HT5B 1993
  • HTR5BP
 No No No No No No

Functions in rodents,
pseudogene in humans

  • None thus far
5-HT6 1993
  • HTR6
 No Yes No No No No
5-HT7 1993
  • HTR7
 Yes Yes Yes No No No

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor.[107]

Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.[38] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A and 5-HT6 agonist.[38]

Expression patterns edit

The genes coding for serotonin receptors are expressed across the mammalian brain. Genes coding for different receptors types follow different developmental curves. Specifically, there is a developmental increase of HTR5A expression in several subregions of the human cortex, paralleled by a decreased expression of HTR1A from the embryonic period to the post-natal one. [108]

5-HT1-like edit

A number of receptors were classed as "5-HT1-like" - by 1998 it was being argued that, since these receptors were "a heterogeneous population of 5-HT1B, 5-HT1D and 5-HT7" receptors the classification was redundant.[109]

References edit

  1. ^ a b Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, et al. (June 1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacological Reviews. 46 (2): 157–203. PMID 7938165.
  2. ^ a b Frazer A, Hensler JG (1999). "Chapter 13: Serotonin Receptors". In Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD (eds.). Basic Neurochemistry: MolecularCellular, and Medical Aspects. Philadelphia: Lippincott-Raven. pp. 263–292. ISBN 978-0-397-51820-3.
  3. ^ Beliveau V, Ganz M, Feng L, Ozenne B, Højgaard L, Fisher PM, et al. (January 2017). "A High-Resolution In Vivo Atlas of the Human Brain's Serotonin System". The Journal of Neuroscience. 37 (1): 120–128. doi:10.1523/jneurosci.2830-16.2016. PMC 5214625. PMID 28053035.
  4. ^ Nichols DE, Nichols CD (May 2008). "Serotonin receptors". Chemical Reviews. 108 (5): 1614–1641. doi:10.1021/cr078224o. PMID 18476671.
  5. ^ Murakami H, Murakami S (August 2007). "Serotonin receptors antagonistically modulate Caenorhabditis elegans longevity". Aging Cell. 6 (4): 483–488. doi:10.1111/j.1474-9726.2007.00303.x. PMID 17559503. S2CID 8345654.
  6. ^ Murakami H, Bessinger K, Hellmann J, Murakami S (July 2008). "Manipulation of serotonin signal suppresses early phase of behavioral aging in Caenorhabditis elegans". Neurobiology of Aging. 29 (7): 1093–1100. doi:10.1016/j.neurobiolaging.2007.01.013. PMID 17336425. S2CID 37671716.
  7. ^ Qi YX, Xia RY, Wu YS, Stanley D, Huang J, Ye GY (December 2014). "Larvae of the small white butterfly, Pieris rapae, express a novel serotonin receptor". Journal of Neurochemistry. 131 (6): 767–777. doi:10.1111/jnc.12940. PMID 25187179. S2CID 21621635.
  8. ^ Francken BJ, Jurzak M, Vanhauwe JF, Luyten WH, Leysen JE (November 1998). "The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells". European Journal of Pharmacology. 361 (2–3): 299–309. doi:10.1016/S0014-2999(98)00744-4. PMID 9865521.
  9. ^ Malenka RC, Nestler EJ, Hyman SE (2009). Sydor A, Brown RY (eds.). Molecular Neuropharmacology: A Foundation for Clinical Neuroscience (2nd ed.). New York: McGraw-Hill Medical. p. 4. ISBN 9780071481274. Similarly, little is known about which of serotonin's 14 known receptors must be activated to achieve an antidepressant response.
  10. ^ Brady ST (2012). Basic Neurochemistry - Principles of Molecular, Cellular and Medical Neurobiology (8th ed.). Waltham, MA: USA: Elsevier. pp. 320–321. ISBN 978-0-12-374947-5.
  11. ^ a b c d Mitchell NA, Pepperell E, Ociepka S, Brown JD, Witherington J, Tuladhar B, et al. (July 2009). "5-hydroxyindalpine, an agonist at the putative 5-HT receptor, has no activity on human recombinant monoamine receptors but accelerates distension-induced peristalsis in mouse isolated colon". Neurogastroenterology and Motility. 21 (7): 760–e48. doi:10.1111/j.1365-2982.2009.01275.x. PMID 19309442. S2CID 9532359.
  12. ^ Glennon RA, Dukat M, Westkaemper RB (2000-01-01). "Serotonin Receptor Subtypes and Ligands". American College of Neurophyscopharmacology. from the original on 21 April 2008. Retrieved 2008-04-11.
  13. ^ "5-Hydroxytryptamine Receptors". IUPHAR Receptor Database. International Union of Basic and Clinical Pharmacology. Retrieved 2008-04-11.
  14. ^ Wesołowska A (2002). "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors" (PDF). Polish Journal of Pharmacology. 54 (4): 327–341. PMID 12523486.
  15. ^ Tomkins DM, Higgins GA, Sellers EM (June 1994). "Low doses of the 5-HT1A agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH DPAT) increase ethanol intake". Psychopharmacology. 115 (1–2): 173–179. doi:10.1007/BF02244769. PMID 7862892. S2CID 38012716.
  16. ^ Müller CP, Carey RJ, Huston JP, De Souza Silva MA (February 2007). "Serotonin and psychostimulant addiction: focus on 5-HT1A-receptors". Progress in Neurobiology. 81 (3): 133–178. doi:10.1016/j.pneurobio.2007.01.001. PMID 17316955. S2CID 42788995.
  17. ^ Carey RJ, DePalma G, Damianopoulos E, Shanahan A, Müller CP, Huston JP (February 2005). "Evidence that the 5-HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects". Brain Research. 1034 (1–2): 162–171. doi:10.1016/j.brainres.2004.12.012. PMID 15713268. S2CID 28356741.
  18. ^ a b de Boer SF, Koolhaas JM (December 2005). "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". European Journal of Pharmacology. 526 (1–3): 125–139. doi:10.1016/j.ejphar.2005.09.065. PMID 16310183.
  19. ^ Parks CL, Robinson PS, Sibille E, Shenk T, Toth M (September 1998). "Increased anxiety of mice lacking the serotonin1A receptor". Proceedings of the National Academy of Sciences of the United States of America. 95 (18): 10734–10739. Bibcode:1998PNAS...9510734P. doi:10.1073/pnas.95.18.10734. PMC 27964. PMID 9724773.
  20. ^ Ebenezer IS, Arkle MJ, Tite RM (May 2007). "8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A receptors". Methods and Findings in Experimental and Clinical Pharmacology. 29 (4): 269–272. doi:10.1358/mf.2007.29.4.1075362. PMID 17609739.
  21. ^ a b Wouters W, Tulp MT, Bevan P (May 1988). "Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors". European Journal of Pharmacology. 149 (3): 213–223. doi:10.1016/0014-2999(88)90651-6. PMID 2842163.
  22. ^ a b Horiuchi J, McDowall LM, Dampney RA (November 2008). "Role of 5-HT(1A) receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation". Autonomic Neuroscience. 142 (1–2): 71–76. doi:10.1016/j.autneu.2008.06.004. PMID 18667366. S2CID 20878941.
  23. ^ Nalivaiko E, Ootsuka Y, Blessing WW (August 2005). "Activation of 5-HT1A receptors in the medullary raphe reduces cardiovascular changes elicited by acute psychological and inflammatory stresses in rabbits". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. 289 (2): R596–R604. doi:10.1152/ajpregu.00845.2004. PMID 15802554. S2CID 17426759.
  24. ^ a b Lucot JB (February 1994). "Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin". European Journal of Pharmacology. 253 (1–2): 53–60. doi:10.1016/0014-2999(94)90756-0. PMID 8013549.
  25. ^ Winstanley CA, Theobald DE, Dalley JW, Robbins TW (April 2005). "Interactions between serotonin and dopamine in the control of impulsive choice in rats: therapeutic implications for impulse control disorders". Neuropsychopharmacology. 30 (4): 669–682. doi:10.1038/sj.npp.1300610. PMID 15688093.
  26. ^ Ogren SO, Eriksson TM, Elvander-Tottie E, D'Addario C, Ekström JC, Svenningsson P, et al. (December 2008). "The role of 5-HT(1A) receptors in learning and memory". Behavioural Brain Research. 195 (1): 54–77. doi:10.1016/j.bbr.2008.02.023. PMID 18394726. S2CID 140205386.
  27. ^ Yasuno F, Suhara T, Nakayama T, Ichimiya T, Okubo Y, Takano A, et al. (February 2003). "Inhibitory effect of hippocampal 5-HT1A receptors on human explicit memory". The American Journal of Psychiatry. 160 (2): 334–340. doi:10.1176/appi.ajp.160.2.334. PMID 12562581.
  28. ^ Kennett GA, Dourish CT, Curzon G (February 1987). "Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression". European Journal of Pharmacology. 134 (3): 265–274. doi:10.1016/0014-2999(87)90357-8. PMID 2883013.
  29. ^ Bardin L, Tarayre JP, Malfetes N, Koek W, Colpaert FC (April 2003). "Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain". Pharmacology. 67 (4): 182–194. doi:10.1159/000068404. PMID 12595749. S2CID 25882138.
  30. ^ a b Millan MJ, Perrin-Monneyron S (March 1997). "Potentiation of fluoxetine-induced penile erections by combined blockade of 5-HT1A and 5-HT1B receptors". European Journal of Pharmacology. 321 (3): R11–R13. doi:10.1016/S0014-2999(97)00050-2. PMID 9085055.
  31. ^ Prow MR, Martin KF, Heal DJ (December 1996). "8-OH-DPAT-induced mydriasis in mice: a pharmacological characterisation". European Journal of Pharmacology. 317 (1): 21–28. doi:10.1016/S0014-2999(96)00693-0. PMID 8982715.
  32. ^ a b Meyer LC, Fuller A, Mitchell D (February 2006). "Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats". American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. 290 (2): R405–R413. doi:10.1152/ajpregu.00440.2005. PMID 16166206. S2CID 224414.
  33. ^ a b Popova NK, Amstislavskaya TG (July 2002). "Involvement of the 5-HT(1A) and 5-HT(1B) serotonergic receptor subtypes in sexual arousal in male mice". Psychoneuroendocrinology. 27 (5): 609–618. doi:10.1016/S0306-4530(01)00097-X. PMID 11965359. S2CID 25269315.
  34. ^ Monti JM, Jantos H (September 1992). "Dose-dependent effects of the 5-HT1A receptor agonist 8-OH-DPAT on sleep and wakefulness in the rat". Journal of Sleep Research. 1 (3): 169–175. doi:10.1111/j.1365-2869.1992.tb00033.x. PMID 10607047.
  35. ^ Thompson MR, Callaghan PD, Hunt GE, Cornish JL, McGregor IS (May 2007). "A role for oxytocin and 5-HT(1A) receptors in the prosocial effects of 3,4 methylenedioxymethamphetamine ("ecstasy")". Neuroscience. 146 (2): 509–514. doi:10.1016/j.neuroscience.2007.02.032. PMID 17383105. S2CID 15617471.
  36. ^ Gudelsky GA, Koenig JI, Meltzer HY (December 1986). "Thermoregulatory responses to serotonin (5-HT) receptor stimulation in the rat. Evidence for opposing roles of 5-HT2 and 5-HT1A receptors". Neuropharmacology. 25 (12): 1307–1313. doi:10.1016/0028-3908(86)90101-2. PMID 2951611. S2CID 2547042.
  37. ^ Ootsuka Y, Blessing WW (February 2006). "Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits". Brain Research. 1073–1074: 252–261. doi:10.1016/j.brainres.2005.12.031. PMID 16455061. S2CID 23178233.
  38. ^ a b c d e f g h i j k l m n o p q r s t u Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09
  39. ^ a b c d e "BRINTELLIX (vortioxetine) tablets for oral use. Full Prescribing Information, Section 12.2 (Pharmacodynamics)." Takeda Pharmaceuticals America Inc. and Lundbeck, 2013. Revised September 2013. [1] 2019-09-18 at the Wayback Machine
  40. ^ Saxena PR, Lawang A (October 1985). "A comparison of cardiovascular and smooth muscle effects of 5-hydroxytryptamine and 5-carboxamidotryptamine, a selective agonist of 5-HT1 receptors". Archives Internationales de Pharmacodynamie et de Therapie. 277 (2): 235–252. PMID 2933009.
  41. ^ Cao BJ, Rodgers RJ (October 1998). "Comparative effects of novel 5-HT1A receptor ligands, LY293284, LY315712 and LY297996, on plus-maze anxiety in mice". Psychopharmacology. 139 (3): 185–194. doi:10.1007/s002130050703. PMID 9784072. S2CID 9466299.
  42. ^ Harrison AA, Parsons LH, Koob GF, Markou A (January 1999). "RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist". Psychopharmacology. 141 (3): 242–250. doi:10.1007/s002130050831. PMID 10027505. S2CID 19974789.
  43. ^ Chojnacka-Wójcik E, Kłodzińska A, Tatarczyńska E (February 2005). "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". The Journal of Pharmacy and Pharmacology. 57 (2): 253–257. doi:10.1211/0022357055399. PMID 15720791. S2CID 20743875.
  44. ^ Lin D, Parsons LH (April 2002). "Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze". Pharmacology, Biochemistry, and Behavior. 71 (4): 581–587. doi:10.1016/S0091-3057(01)00712-2. PMID 11888549. S2CID 21610537.
  45. ^ a b Tatarczyńska E, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E (December 2004). "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behavioural Pharmacology. 15 (8): 523–534. doi:10.1097/00008877-200412000-00001. PMID 15577451. S2CID 6940756.
  46. ^ a b Eriksson TM, Madjid N, Elvander-Tottie E, Stiedl O, Svenningsson P, Ogren SO (June 2008). "Blockade of 5-HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission". Neuropharmacology. 54 (7): 1041–1050. doi:10.1016/j.neuropharm.2008.02.007. hdl:10616/40922. PMID 18394658. S2CID 207223573.
  47. ^ a b McCreary AC, Bankson MG, Cunningham KA (September 1999). "Pharmacological studies of the acute and chronic effects of (+)-3, 4-methylenedioxymethamphetamine on locomotor activity: role of 5-hydroxytryptamine(1A) and 5-hydroxytryptamine(1B/1D) receptors". The Journal of Pharmacology and Experimental Therapeutics. 290 (3): 965–973. PMID 10454466.
  48. ^ Amital D, Fostick L, Sasson Y, Kindler S, Amital H, Zohar J (May 2005). "Anxiogenic effects of Sumatriptan in panic disorder: a double-blind, placebo-controlled study". European Neuropsychopharmacology. 15 (3): 279–282. doi:10.1016/j.euroneuro.2004.12.002. PMID 15820416. S2CID 8382188.
  49. ^ Feuerstein TJ, Hüring H, van Velthoven V, Lücking CH, Landwehrmeyer GB (May 1996). "5-HT1D-like receptors inhibit the release of endogenously formed [3H]GABA in human, but not in rabbit, neocortex". Neuroscience Letters. 209 (3): 210–214. doi:10.1016/0304-3940(96)12637-9. PMID 8736648. S2CID 27376524.
  50. ^ Najjar SA, Hung LY, Margolis KG (June 2023). "Serotonergic Control of Gastrointestinal Development, Motility, and Inflammation". Comprehensive Physiology. 13 (3): 4851–4868. doi:10.1002/cphy.c220024. ISBN 9780470650714. PMC 10373054. PMID 37358510.
  51. ^ Branchek TA, Mawe GM, Gershon MD (July 1988). "Characterization and localization of a peripheral neural 5-hydroxytryptamine receptor subtype (5-HT1P) with a selective agonist, 3H-5-hydroxyindalpine". The Journal of Neuroscience. 8 (7): 2582–2595. doi:10.1523/JNEUROSCI.08-07-02582.1988. PMC 6569501. PMID 3249244.
  52. ^ Mawe GM, Branchek TA, Gershon MD (December 1986). "Peripheral neural serotonin receptors: identification and characterization with specific antagonists and agonists". Proceedings of the National Academy of Sciences of the United States of America. 83 (24): 9799–9803. Bibcode:1986PNAS...83.9799M. doi:10.1073/pnas.83.24.9799. PMC 387229. PMID 3467338.
  53. ^ Annaházi, Anita; Berger, Thomas Erwin; Demir, Ihsan Ekin; Zeller, Florian; Müller, Michael; Anneser, Markus; Skerra, Arne; Michel, Klaus; Schemann, Michael (April 2022). "Metabotropic 5-HT receptor-mediated effects in the human submucous plexus". Neurogastroenterology & Motility. 34 (10): e14380. doi:10.1111/nmo.14380. ISSN 1350-1925. PMID 35438222. S2CID 248241342.
  54. ^ a b Bubar MJ, Cunningham KA (2006). "Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence". Current Topics in Medicinal Chemistry. 6 (18): 1971–1985. doi:10.2174/156802606778522131. PMID 17017968.
  55. ^ Schreiber R, Melon C, De Vry J (February 1998). "The role of 5-HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test". Psychopharmacology. 135 (4): 383–391. doi:10.1007/s002130050526. PMID 9539263. S2CID 22677071.
  56. ^ a b Popova NK, Amstislavskaya TG (July 2002). "5-HT2A and 5-HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo-pituitary-testicular response to the presence of a female". Neuroendocrinology. 76 (1): 28–34. doi:10.1159/000063681. PMID 12097814. S2CID 42319246.
  57. ^ a b Popa D, Léna C, Fabre V, Prenat C, Gingrich J, Escourrou P, et al. (December 2005). "Contribution of 5-HT2 receptor subtypes to sleep-wakefulness and respiratory control, and functional adaptations in knock-out mice lacking 5-HT2A receptors". The Journal of Neuroscience. 25 (49): 11231–11238. doi:10.1523/JNEUROSCI.1724-05.2005. PMC 6725907. PMID 16339018.
  58. ^ a b Mazzola-Pomietto P, Aulakh CS, Tolliver T, Murphy DL (March 1997). "Functional subsensitivity of 5-HT2A and 5-HT2C receptors mediating hyperthermia following acute and chronic treatment with 5-HT2A/2C receptor antagonists". Psychopharmacology. 130 (2): 144–151. doi:10.1007/s002130050222. PMID 9106912. S2CID 22432569.
  59. ^ Blessing WW, Seaman B (2003). "5-hydroxytryptamine(2A) receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats". Neuroscience. 117 (4): 939–948. doi:10.1016/S0306-4522(02)00810-2. PMID 12654345. S2CID 53251590.
  60. ^ a b c McCall RB, Franklin SR, Hyslop DK, Knauer CS, Chio CL, Haber CL, Fitzgerald LW (2001). PNU-22394, a 5-HT2C receptor agonist, reduced feeding in rodents and produces weight loss in humans (Online). Society for Neuroscience. Vol. 27. Presentation Number 309.2. San Diego, CA: Society for Neuroscience Abstracts. p. TT-45. Retrieved 18 July 2014.
  61. ^ a b c Garfield AS, Heisler LK (January 2009). "Pharmacological targeting of the serotonergic system for the treatment of obesity". The Journal of Physiology. 587 (1): 49–60. doi:10.1113/jphysiol.2008.164152. PMC 2670022. PMID 19029184.
  62. ^ a b c Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, et al. (February 2013). "Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties". Journal of Medicinal Chemistry. 56 (3): 1211–1227. CiteSeerX 10.1.1.691.154. doi:10.1021/jm301656h. PMID 23301527.
  63. ^ Kennett GA, Bright F, Trail B, Baxter GS, Blackburn TP (April 1996). "Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety". British Journal of Pharmacology. 117 (7): 1443–1448. doi:10.1111/j.1476-5381.1996.tb15304.x. PMC 1909458. PMID 8730737.
  64. ^ Duxon MS, Kennett GA, Lightowler S, Blackburn TP, Fone KC (1997). "Activation of 5-HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat". Neuropharmacology. 36 (4–5): 601–608. doi:10.1016/S0028-3908(97)00042-7. PMID 9225285. S2CID 41471226.
  65. ^ Kennett GA, Trail B, Bright F (December 1998). "Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated". Neuropharmacology. 37 (12): 1603–1610. doi:10.1016/S0028-3908(98)00115-4. PMID 9886683. S2CID 7310462.
  66. ^ Kennett GA, Ainsworth K, Trail B, Blackburn TP (February 1997). "BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats". Neuropharmacology. 36 (2): 233–239. doi:10.1016/S0028-3908(96)00171-2. PMID 9144661. S2CID 23583570.
  67. ^ Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, et al. (March 2002). "5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro". British Journal of Pharmacology. 135 (5): 1144–1151. doi:10.1038/sj.bjp.0704571. PMC 1573235. PMID 11877320.
  68. ^ Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, et al. (1997). "SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist". Neuropharmacology. 36 (4–5): 609–620. doi:10.1016/S0028-3908(97)00038-5. PMID 9225286. S2CID 23032157.
  69. ^ a b Millan MJ, Brocco M, Gobert A, Dekeyne A (February 2005). "Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade". Psychopharmacology. 177 (4): 448–458. doi:10.1007/s00213-004-1962-z. PMID 15289999. S2CID 20866665.
  70. ^ a b Dekeyne A, Mannoury la Cour C, Gobert A, Brocco M, Lejeune F, Serres F, et al. (September 2008). "S32006, a novel 5-HT2C receptor antagonist displaying broad-based antidepressant and anxiolytic properties in rodent models". Psychopharmacology. 199 (4): 549–568. doi:10.1007/s00213-008-1177-9. PMID 18523738. S2CID 25063495.
  71. ^ Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, et al. (May 2009). "Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin". Biological Psychiatry. 65 (9): 748–759. doi:10.1016/j.biopsych.2008.10.031. PMID 19058784. S2CID 22053616.
  72. ^ Millan MJ, Peglion JL, Lavielle G, Perrin-Monneyron S (April 1997). "5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists". European Journal of Pharmacology. 325 (1): 9–12. doi:10.1016/S0014-2999(97)89962-1. PMID 9151932.
  73. ^ Stancampiano R, Melis MR, Argiolas A (August 1994). "Penile erection and yawning induced by 5-HT1C receptor agonists in male rats: relationship with dopaminergic and oxytocinergic transmission". European Journal of Pharmacology. 261 (1–2): 149–155. doi:10.1016/0014-2999(94)90313-1. PMID 8001637.
  74. ^ Frank MG, Stryker MP, Tecott LH (November 2002). "Sleep and sleep homeostasis in mice lacking the 5-HT2c receptor". Neuropsychopharmacology. 27 (5): 869–873. doi:10.1016/S0893-133X(02)00353-6. PMC 2452994. PMID 12431861.
  75. ^ Villalobos CA, Bull P, Sáez P, Cassels BK, Huidobro-Toro JP (April 2004). "4-Bromo-2,5-dimethoxyphenethylamine (2C-B) and structurally related phenylethylamines are potent 5-HT2A receptor antagonists in Xenopus laevis oocytes". British Journal of Pharmacology. 141 (7): 1167–1174. doi:10.1038/sj.bjp.0705722. PMC 1574890. PMID 15006903.
  76. ^ Rang HP (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 978-0-443-07145-4. Page 187
  77. ^ Michel K, Zeller F, Langer R, Nekarda H, Kruger D, Dover TJ, et al. (May 2005). "Serotonin excites neurons in the human submucous plexus via 5-HT3 receptors". Gastroenterology. 128 (5): 1317–1326. doi:10.1053/j.gastro.2005.02.005. PMID 15887114.
  78. ^ a b Pitsikas N, Brambilla A, Borsini F (January 1994). "Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine-induced amnesia in the rat in a spatial learning task". Pharmacology, Biochemistry, and Behavior. 47 (1): 95–99. doi:10.1016/0091-3057(94)90116-3. PMID 8115433. S2CID 21800364.
  79. ^ a b Smriga M, Torii K (December 2003). "L-Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin-mediated intestinal pathologies and anxiety in rats". Proceedings of the National Academy of Sciences of the United States of America. 100 (26): 15370–15375. Bibcode:2003PNAS..10015370S. doi:10.1073/pnas.2436556100. PMC 307574. PMID 14676321.
  80. ^ Kennett GA, Bright F, Trail B, Blackburn TP, Sanger GJ (1997). "Anxiolytic-like actions of the selective 5-HT4 receptor antagonists SB 204070A and SB 207266A in rats". Neuropharmacology. 36 (4–5): 707–712. doi:10.1016/S0028-3908(97)00037-3. PMID 9225297. S2CID 40341646.
  81. ^ Jean A, Conductier G, Manrique C, Bouras C, Berta P, Hen R, et al. (October 2007). "Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens". Proceedings of the National Academy of Sciences of the United States of America. 104 (41): 16335–16340. Bibcode:2007PNAS..10416335J. doi:10.1073/pnas.0701471104. PMC 2042207. PMID 17913892.
  82. ^ Compan V, Charnay Y, Dusticier N, Daszuta A, Hen R, Bockaert J (2004). "[Feeding disorders in 5-HT4 receptor knockout mice]". Journal de la Société de Biologie. 198 (1): 37–49. doi:10.1051/jbio/2004198010037. PMID 15146954. S2CID 90408378.
  83. ^ a b Meneses A, Hong E (March 1997). "Effects of 5-HT4 receptor agonists and antagonists in learning". Pharmacology, Biochemistry, and Behavior. 56 (3): 347–351. doi:10.1016/S0091-3057(96)00224-9. PMID 9077568. S2CID 11866740.
  84. ^ a b Fontana DJ, Daniels SE, Wong EH, Clark RD, Eglen RM (1997). "The effects of novel, selective 5-hydroxytryptamine (5-HT)4 receptor ligands in rat spatial navigation". Neuropharmacology. 36 (4–5): 689–696. doi:10.1016/S0028-3908(97)00055-5. PMID 9225295. S2CID 46510811.
  85. ^ Galeotti N, Ghelardini C, Bartolini A (September 1998). "Role of 5-HT4 receptors in the mouse passive avoidance test". The Journal of Pharmacology and Experimental Therapeutics. 286 (3): 1115–1121. PMID 9732367.
  86. ^ Lucas G, Rymar VV, Du J, Mnie-Filali O, Bisgaard C, Manta S, et al. (September 2007). "Serotonin(4) (5-HT(4)) receptor agonists are putative antidepressants with a rapid onset of action". Neuron. 55 (5): 712–725. doi:10.1016/j.neuron.2007.07.041. PMID 17785179. S2CID 14558104.
  87. ^ Duman RS (September 2007). "A silver bullet for the treatment of depression?". Neuron. 55 (5): 679–681. doi:10.1016/j.neuron.2007.08.011. PMID 17785173.
  88. ^ Manzke T, Guenther U, Ponimaskin EG, Haller M, Dutschmann M, Schwarzacher S, Richter DW (July 2003). "5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia". Science. 301 (5630): 226–229. Bibcode:2003Sci...301..226M. doi:10.1126/science.1084674. PMID 12855812. S2CID 13641423.
  89. ^ Nelson DL (February 2004). "5-HT5 receptors". Current Drug Targets. CNS and Neurological Disorders. 3 (1): 53–58. doi:10.2174/1568007043482606. PMID 14965244.
  90. ^ a b Dietz BM, Mahady GB, Pauli GF, Farnsworth NR (August 2005). "Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro". Brain Research. Molecular Brain Research. 138 (2): 191–197. doi:10.1016/j.molbrainres.2005.04.009. PMC 5805132. PMID 15921820.
  91. ^ a b c Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, et al. (July 2022). "Inactive and active state structures template selective tools for the human 5-HT5A receptor". Nature Structural & Molecular Biology. 29 (7): 677–687. doi:10.1038/s41594-022-00796-6. PMC 9299520. PMID 35835867.
  92. ^ Wesołowska A (February 2008). "The anxiolytic-like effect of the selective 5-HT6 receptor antagonist SB-399885: the impact of benzodiazepine receptors". European Journal of Pharmacology. 580 (3): 355–360. doi:10.1016/j.ejphar.2007.11.022. PMID 18096153.
  93. ^ a b Wesołowska A, Nikiforuk A (April 2007). "Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression". Neuropharmacology. 52 (5): 1274–1283. doi:10.1016/j.neuropharm.2007.01.007. PMID 17320917. S2CID 22664564.
  94. ^ Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, et al. (December 2006). "SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models". European Journal of Pharmacology. 553 (1–3): 109–119. doi:10.1016/j.ejphar.2006.09.049. PMID 17069795.
  95. ^ a b Perez-García G, Meneses A (July 2005). "Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task". Pharmacology, Biochemistry, and Behavior. 81 (3): 673–682. doi:10.1016/j.pbb.2005.05.005. PMID 15964617. S2CID 19789219.
  96. ^ Wesołowska A, Nikiforuk A (March 2008). "The selective 5-HT(6) receptor antagonist SB-399885 enhances anti-immobility action of antidepressants in rats". European Journal of Pharmacology. 582 (1–3): 88–93. doi:10.1016/j.ejphar.2007.12.013. PMID 18234190.
  97. ^ Alcalde E, Mesquida N, López-Pérez S, Frigola J, Mercè R (Feb 2009). "Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists". Journal of Medicinal Chemistry. 52 (3): 675–87. doi:10.1021/jm8009469. PMID 19159187.
  98. ^ . The Association of the British Pharmaceutical Industry. Archived from the original on 2008-06-12. Retrieved 2008-04-11.
  99. ^ a b c Hedlund PB, Huitron-Resendiz S, Henriksen SJ, Sutcliffe JG (November 2005). "5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern". Biological Psychiatry. 58 (10): 831–837. doi:10.1016/j.biopsych.2005.05.012. PMID 16018977. S2CID 10998014.
  100. ^ a b Wesołowska A, Nikiforuk A, Stachowicz K, Tatarczyńska E (September 2006). "Effect of the selective 5-HT7 receptor antagonist SB 269970 in animal models of anxiety and depression". Neuropharmacology. 51 (3): 578–586. doi:10.1016/j.neuropharm.2006.04.017. PMID 16828124. S2CID 39928418.
  101. ^ Gasbarri A, Cifariello A, Pompili A, Meneses A (December 2008). "Effect of 5-HT(7) antagonist SB-269970 in the modulation of working and reference memory in the rat". Behavioural Brain Research. 195 (1): 164–170. doi:10.1016/j.bbr.2007.12.020. PMID 18308404. S2CID 12910296.
  102. ^ Liy-Salmeron G, Meneses A (2008). "Effects of 5-HT drugs in prefrontal cortex during memory formation and the ketamine amnesia-model". Hippocampus. 18 (9): 965–974. doi:10.1002/hipo.20459. PMID 18570192. S2CID 20937527.
  103. ^ a b Bonaventure P, Kelly L, Aluisio L, Shelton J, Lord B, Galici R, et al. (May 2007). "Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents". The Journal of Pharmacology and Experimental Therapeutics. 321 (2): 690–698. doi:10.1124/jpet.107.119404. PMID 17314195. S2CID 14579645.
  104. ^ Thomas DR, Melotto S, Massagrande M, Gribble AD, Jeffrey P, Stevens AJ, et al. (June 2003). "SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats". British Journal of Pharmacology. 139 (4): 705–714. doi:10.1038/sj.bjp.0705290. PMC 1573887. PMID 12812993.
  105. ^ León-Ponte, Matilde; Ahern, Gerard P.; O'Connell, Peta J. (2007-04-15). "Serotonin provides an accessory signal to enhance T-cell activation by signaling through the 5-HT7 receptor". Blood. 109 (8): 3139–3146. doi:10.1182/blood-2006-10-052787. ISSN 0006-4971. PMC 1852236. PMID 17158224.
  106. ^ Davies MA, Sheffler DJ, Roth BL. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):317–36. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf
  107. ^ "HTR2C 5-hydroxytryptamine receptor 2C [ Homo sapiens (human) ]". NCBI. 19 Mar 2017. Retrieved 26 Mar 2017.
  108. ^ Bar-Shira O, Maor R, Chechik G (December 2015). "Gene Expression Switching of Receptor Subunits in Human Brain Development". PLOS Computational Biology. 11 (12): e1004559. Bibcode:2015PLSCB..11E4559B. doi:10.1371/journal.pcbi.1004559. PMC 4670163. PMID 26636753.
  109. ^ Saxena PR, De Vries P, Villalón CM (August 1998). "5-HT1-like receptors: a time to bid goodbye". Trends in Pharmacological Sciences. 19 (8): 311–316. doi:10.1016/S0165-6147(98)01228-0. PMID 9745358.

External links edit

  • Serotonin+Receptors at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
  • "5-Hydroxytryptamine Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
  • Rubenstein LA, Lanzara RG (2005-02-16). "Activation of G protein-coupled receptors entails cysteine modulation of agonist binding". Cogprints. Retrieved 2008-04-11.
  • Paterson LM, Kornum BR, Nutt DJ, Pike VW, Knudsen GM (January 2013). "5-HT radioligands for human brain imaging with PET and SPECT". Medicinal Research Reviews. 33 (1): 54–111. doi:10.1002/med.20245. PMC 4188513. PMID 21674551.

January 01, 1970
receptor, hydroxytryptamine, receptors, serotonin, receptors, group, protein, coupled, receptor, ligand, gated, channels, found, central, peripheral, nervous, systems, they, mediate, both, excitatory, inhibitory, neurotransmission, serotonin, hydroxytryptamine. 5 HT receptors 5 hydroxytryptamine receptors or serotonin receptors are a group of G protein coupled receptor and ligand gated ion channels found in the central and peripheral nervous systems 1 2 3 They mediate both excitatory and inhibitory neurotransmission The serotonin i e 5 hydroxytryptamine hence 5 HT receptors are activated by the neurotransmitter serotonin which acts as their natural ligand The 5 HT1B receptor as an example of a metabotropic serotonin receptor Its crystallographic structure in ribbon representation The serotonin receptors modulate the release of many neurotransmitters including glutamate GABA dopamine epinephrine norepinephrine and acetylcholine as well as many hormones including oxytocin prolactin vasopressin cortisol corticotropin and substance P among others Serotonin receptors influence various biological and neurological processes such as aggression anxiety appetite cognition learning memory mood nausea sleep and thermoregulation They are the target of a variety of pharmaceutical and recreational drugs including many antidepressants antipsychotics anorectics antiemetics gastroprokinetic agents antimigraine agents hallucinogens and entactogens 4 Serotonin receptors are found in almost all animals and are even known to regulate longevity and behavioral aging in the primitive nematode Caenorhabditis elegans 5 6 Contents 1 Classification 1 1 Families 1 2 Subtypes 2 Expression patterns 3 5 HT1 like 4 References 5 External linksClassification edit5 hydroxytryptamine receptors or 5 HT receptors or serotonin receptors are found in the central and peripheral nervous systems 1 2 They can be divided into 7 families of G protein coupled receptors which activate an intracellular second messenger cascade to produce an excitatory or inhibitory response The exception to this is the 5 HT3 receptor which is a ligand gated ion channel In 2014 a novel 5 HT receptor was isolated from the small white butterfly Pieris rapae and named pr5 HT8 It does not occur in mammals and shares relatively low similarity to the known 5 HT receptor classes 7 Families edit Family Type Mechanism Potential 5 HT1 Gi Go protein coupled Decreasing cellular levels of cAMP Inhibitory 5 HT2 Gq G11 protein coupled Increasing cellular levels of IP3 and DAG Excitatory 5 HT3 Ligand gated Na and K cation channel Depolarizing plasma membrane Excitatory 5 HT4 Gs protein coupled Increasing cellular levels of cAMP Excitatory 5 HT5 Gi Go protein coupled 8 Decreasing cellular levels of cAMP Inhibitory 5 HT6 Gs protein coupled Increasing cellular levels of cAMP Excitatory 5 HT7 Gs protein coupled Increasing cellular levels of cAMP Excitatory Subtypes edit The 7 general serotonin receptor classes include a total of 14 known serotonin receptors 9 The 15th receptor 5 HT1P has been distinguished on the basis of functional and radioligand binding studies its existence has never been definitely affirmed or refuted 10 11 The specific types have been characterized as follows 12 13 14 Information on serotonin receptors human isoforms if nothing else is stated Receptor First cloned PDB entries Gene s Distribution Function Agonists Antagonists Uses of drugs that act on this receptor Blood vessels CNS GI Tract Platelets PNS Smooth Muscle 5 HT1A 1987 7e2x 7e2y 7e2z nbsp HTR1A Yes Yes No No No No Addiction 15 16 17 Aggression 18 Anxiety 19 Appetite 20 Autoreceptor Blood Pressure 21 22 Cardiovascular Function 23 Emesis 24 Heart Rate 21 22 Impulsivity 25 Memory 26 27 Mood 28 Nausea 24 Nociception 29 Penile Erection 30 Pupil Dilation 31 Respiration 32 Sexual Behavior 33 Sleep 34 Sociability 35 Thermoregulation 36 Vasoconstriction 37 Selective for 5 HT1A over other 5 HT receptors Vilazodone Viibryd F 15 599 research compound highly potent and selective for 5 HT1A Flesinoxan potent EC50 24 nM Gepirone partial agonist Ki 70 nM Haloperidol Ipsapirone partial agonist Ki 12 1 nM Quetiapine Trazodone SARI selective in the sense that on all other 5 HT receptors it acts as either an antagonist or has no action Kd 78 nM Yohimbine unselective partial agonist Tandospirone potent and selective partial agonist Nonselective 5 CT potent Ki 250 50 pM 8 OH DPAT potent Aripiprazole atypical antipsychotic Asenapine atypical antipsychotic Buspirone 38 partial agonist Vortioxetine high efficacy partial agonist 39 Ziprasidone partial agonist Ki 3 4 nM Methylphenidate weak agonist BMY 7378 Cyanopindolol Iodocyanopindolol Lecozotan Methiothepin Methysergide 40 NAN 190 Nebivolol Nefazodone WAY 100 135 WAY 100 635 Mefway Analgesics agonists Antidepressants post synaptic receptor agonists and pre synaptic autoreceptor antagonists serve as antidepressants Anxiolytics 41 agonist and antagonist 5 HT1B 1992 6g79 HTR1B Yes Yes No No No No Addiction 42 Aggression 18 Anxiety 43 44 45 Autoreceptor Learning 46 Locomotion 47 Memory 46 Mood 45 Penile Erection 30 Sexual Behavior 33 Vasoconstriction 5 CT CGS 12066A CP 93 129 CP 94 253 Dihydroergotamine Eltoprazine Ergotamine Methysergide RU 24969 TFMPP Triptans 38 antimigraine 38 Zolmitriptan Eletriptan Sumatriptan Vortioxetine partial agonist Ki 33 nM 39 Alprenolol AR A000002 Asenapine Cyanopindolol GR 127 935 Iodocyanopindolol Isamoltane Metergoline Methiothepin Oxprenolol Pindolol Propranolol SB 216 641 Yohimbine Migraines e g triptans 5 HT1D 1991 7e32 nbsp HTR1D Yes Yes No No No No Anxiety 48 49 Autoreceptor Locomotion 47 Vasoconstriction 5 CT CP 135 807 Dihydroergotamine Ergotamine Methysergide Triptans 38 antimigraine 38 Almotriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan Yohimbine BRL 15572 GR 127 935 Ketanserin Metergoline Methiothepin Rauwolscine Ritanserin Vortioxetine Ki 54 nM 39 Ziprasidone Migraines e g triptans 5 HT1E 1992 7e33 nbsp HTR1E Yes Yes No No No No BRL 54443 None known 5 HT1F 1993 7exd nbsp HTR1F No Yes No No No No Migraine BRL 54443 Lasmiditan LY 334 370 Naratriptan Eletriptan None known 5 HT1P Not cloned No No Yes No No No Peristalsis 11 50 5 OHIP 11 51 2 Methyl 5 HT 52 5 BOHIP 53 5 HTP DP 11 None known 5 HT2A 1988 HTR2A Yes Yes Yes Yes Yes Yes Addiction potentially modulating 54 Anxiety 55 Appetite Cognition Imagination Learning Memory Mood Perception Sexual Behavior 56 Sleep 57 Thermoregulation 58 Vasoconstriction 59 25I NBOMe Full agonist 5 MeO DMT BZP Bufotenin DMT DOM Ergonovine Lisuride LSD Mescaline PNU 22394 partial agonist 60 61 62 Psilocin Psilocybin TFMPP partial agonist or antagonist Atypical antipsychotics Aripiprazole Clozapine 38 Olanzapine Quetiapine Risperidone Ziprasidone Asenapine Amitriptyline Clomipramine Cyproheptadine Doxepin Eplivanserin Etoperidone Haloperidol Hydroxyzine Iloperidone Ketanserin 38 antihypertensive 38 Methysergide Mianserin Mirtazapine Nefazodone Pimavanserin Pizotifen Ritanserin Trazodone Yohimbine Atypical antipsychotics antagonist Psychedelics agonists NaSSAs antidepressants and anxiolytics they serve as antagonists at this site Treating serotonin syndrome antagonists e g cyproheptadine Sleeping aid antagonists e g trazodone 5 HT2B 1992 HTR2B Yes Yes Yes Yes Yes Yes Anxiety 63 64 65 Appetite 66 Cardiovascular Function GI Motility 67 Sleep 57 Vasoconstriction 6 APB full agonist BW 723C86 Fenfluramine MDMA Norfenfluramine PNU 22394 partial agonist 60 61 62 Ro60 0175 Methylphenidate weak agonist Agomelatine Asenapine BZP Ketanserin Methysergide Ritanserin RS 127 445 Tegaserod Yohimbine Migraines antagonists 5 HT2C 1988 HTR2C Yes Yes Yes Yes Yes Yes Addiction potentially modulating 54 Anxiety 68 69 70 Appetite GI Motility 71 Heteroreceptor for norepinephrine and dopamine Locomotion Mood 69 70 Penile Erection 72 73 Sexual Behavior 56 Sleep 74 Thermoregulation 58 Vasoconstriction 2C B partial agonist 75 A 372 159 AL 38022A Aripiprazole Ergonovine Lorcaserin PNU 22394 full agonist 60 61 62 Ro60 0175 TFMPP Trazodone 38 hypnotic 38 YM 348 Agomelatine 38 antidepressant 38 Amitriptyline Asenapine Clomipramine Clozapine 38 antipsychotic 38 Cyproheptadine Dimebolin Eltoprazine Etoperidone Fluoxetine Haloperidol Iloperidone Ketanserin 38 antihypertensive 38 Lisuride Methysergide 76 Mianserin Mirtazapine Nefazodone Olanzapine Paroxetine Quetiapine Risperidone Ritanserin SB 242084 Tramadol Trazodone Ziprasidone Antidepressant antagonists e g agomelatine fluoxetine mirtazapine Orexigenic e g mirtazapine clozapine and olanzapine antagonists Anorectic Lorcaserin agonist Antipsychotic Vabicaserin agonists 5 HT3 1993 HTR3A HTR3B HTR3C HTR3D HTR3E No Yes Yes No Yes No Addiction Anxiety Emesis GI Motility 77 Learning 78 Memory 78 Nausea 2 Methyl 5 HT BZP Quipazine RS 56812 Alosetron Several antiemetics 38 Dolasetron Ondansetron 38 Granisetron Tropisetron Clozapine Memantine Metoclopramide Mianserin Mirtazapine Olanzapine Quetiapine Vortioxetine Ki 3 7 nM 39 Antiemetic Antidepressant e g mirtazpine antipsychotic e g olanzapine quetiapine 5 HT4 1995 HTR4 No Yes Yes No Yes No Anxiety 79 80 Appetite 81 82 GI Motility Learning 83 84 Memory 83 84 85 Mood 86 87 Respiration 88 5 MT BIMU 8 Cinitapride Cisapride 38 gastroprokinetic Dazopride Metoclopramide Mosapride Prucalopride RS 67333 Renzapride Tegaserod Zacopride L Lysine 79 Piboserod Gastroprokinetics e g Tegaserod 5 HT5A 1994 7UM4 7UM5 7UM6 7UM7 HTR5A No Yes No No No No Autoreceptor Locomotion 89 Sleep 90 5 CT Ergotamine Lisuride partial 91 Methylergometrine full 91 Valerenic Acid partial agonist 90 Asenapine Dimebolin Methiothepin Ritanserin SB 699 551 SB 699 551 A MS112 91 None thus far 5 HT5B 1993 HTR5BP No No No No No No Functions in rodents pseudogene in humans None thus far 5 HT6 1993 HTR6 No Yes No No No No Anxiety 92 93 Cognition 94 Learning 95 Memory 95 Mood 93 96 EMD 386 088 EMDT WAY 181 187 WAY 208 466 E 6837 N inden 5 yl imidazothiazole 5 sulfonamide 43 97 Amitriptyline Aripiprazole Asenapine Clomipramine Clozapine Dimebolin EGIS 12233 Haloperidol Iloperidone MS 245 Olanzapine Ro04 6790 SB 258 585 SB 271 046 98 SB 357 134 SB 399 885 Antidepressant antagonists and agonists Anxiolytic antagonists and agonist Nootropic antagonists Anorectic antagonists 5 HT7 1993 HTR7 Yes Yes Yes No No No Anxiety 99 100 Autoreceptor Memory 101 102 Mood 99 100 Respiration 32 103 Sleep 99 103 104 Thermoregulation Vasoconstriction Immunostimulation 105 5 CT 8 OH DPAT Aripiprazole weak partial agonist 106 AS 19 E 55888 Amitriptyline Asenapine Clomipramine Clozapine EGIS 12233 Haloperidol Iloperidone Imipramine Ketanserin Mirtazapine Olanzapine RA 7 Ritanserin Risperidone SB 269 970 Vortioxetine Ki 19 nM 39 Antidepressant antagonists Anxiolytics antagonists Nootropic antagonists Note that there is no 5 HT1C receptor since after the receptor was cloned and further characterized it was found to have more in common with the 5 HT2 family of receptors and was redesignated as the 5 HT2C receptor 107 Very nonselective agonists of 5 HT receptor subtypes include ergotamine an antimigraine which activates 5 HT1A 5 HT1D 5 HT1B D2 and norepinephrine receptors 38 LSD a psychedelic is a 5 HT1A 5 HT2A 5 HT2C 5 HT5A and 5 HT6 agonist 38 Expression patterns editThe genes coding for serotonin receptors are expressed across the mammalian brain Genes coding for different receptors types follow different developmental curves Specifically there is a developmental increase of HTR5A expression in several subregions of the human cortex paralleled by a decreased expression of HTR1A from the embryonic period to the post natal one 108 5 HT1 like editA number of receptors were classed as 5 HT1 like by 1998 it was being argued that since these receptors were a heterogeneous population of 5 HT1B 5 HT1D and 5 HT7 receptors the classification was redundant 109 References edit a b Hoyer D Clarke DE Fozard JR Hartig PR Martin GR Mylecharane EJ et al June 1994 International Union of Pharmacology classification of receptors for 5 hydroxytryptamine Serotonin Pharmacological Reviews 46 2 157 203 PMID 7938165 a b Frazer A Hensler JG 1999 Chapter 13 Serotonin Receptors In Siegel GJ Agranoff BW Albers RW Fisher SK Uhler MD eds Basic Neurochemistry MolecularCellular and Medical Aspects Philadelphia Lippincott Raven pp 263 292 ISBN 978 0 397 51820 3 Beliveau V Ganz M Feng L Ozenne B Hojgaard L Fisher PM et al January 2017 A High Resolution In Vivo Atlas of the Human Brain s Serotonin System The Journal of Neuroscience 37 1 120 128 doi 10 1523 jneurosci 2830 16 2016 PMC 5214625 PMID 28053035 Nichols DE Nichols CD May 2008 Serotonin receptors Chemical Reviews 108 5 1614 1641 doi 10 1021 cr078224o PMID 18476671 Murakami H Murakami S August 2007 Serotonin receptors antagonistically modulate Caenorhabditis elegans longevity Aging Cell 6 4 483 488 doi 10 1111 j 1474 9726 2007 00303 x PMID 17559503 S2CID 8345654 Murakami H Bessinger K Hellmann J Murakami S July 2008 Manipulation of serotonin signal suppresses early phase of behavioral aging in Caenorhabditis elegans Neurobiology of Aging 29 7 1093 1100 doi 10 1016 j neurobiolaging 2007 01 013 PMID 17336425 S2CID 37671716 Qi YX Xia RY Wu YS Stanley D Huang J Ye GY December 2014 Larvae of the small white butterfly Pieris rapae express a novel serotonin receptor Journal of Neurochemistry 131 6 767 777 doi 10 1111 jnc 12940 PMID 25187179 S2CID 21621635 Francken BJ Jurzak M Vanhauwe JF Luyten WH Leysen JE November 1998 The human 5 ht5A receptor couples to Gi Go proteins and inhibits adenylate cyclase in HEK 293 cells European Journal of Pharmacology 361 2 3 299 309 doi 10 1016 S0014 2999 98 00744 4 PMID 9865521 Malenka RC Nestler EJ Hyman SE 2009 Sydor A Brown RY eds Molecular Neuropharmacology A Foundation for Clinical Neuroscience 2nd ed New York McGraw Hill Medical p 4 ISBN 9780071481274 Similarly little is known about which of serotonin s 14 known receptors must be activated to achieve an antidepressant response Brady ST 2012 Basic Neurochemistry Principles of Molecular Cellular and Medical Neurobiology 8th ed Waltham MA USA Elsevier pp 320 321 ISBN 978 0 12 374947 5 a b c d Mitchell NA Pepperell E Ociepka S Brown JD Witherington J Tuladhar B et al July 2009 5 hydroxyindalpine an agonist at the putative 5 HT receptor has no activity on human recombinant monoamine receptors but accelerates distension induced peristalsis in mouse isolated colon Neurogastroenterology and Motility 21 7 760 e48 doi 10 1111 j 1365 2982 2009 01275 x PMID 19309442 S2CID 9532359 Glennon RA Dukat M Westkaemper RB 2000 01 01 Serotonin Receptor Subtypes and Ligands American College of Neurophyscopharmacology Archived from the original on 21 April 2008 Retrieved 2008 04 11 5 Hydroxytryptamine Receptors IUPHAR Receptor Database International Union of Basic and Clinical Pharmacology Retrieved 2008 04 11 Wesolowska A 2002 In the search for selective ligands of 5 HT5 5 HT6 and 5 HT7 serotonin receptors PDF Polish Journal of Pharmacology 54 4 327 341 PMID 12523486 Tomkins DM Higgins GA Sellers EM June 1994 Low doses of the 5 HT1A agonist 8 hydroxy 2 di n propylamino tetralin 8 OH DPAT increase ethanol intake Psychopharmacology 115 1 2 173 179 doi 10 1007 BF02244769 PMID 7862892 S2CID 38012716 Muller CP Carey RJ Huston JP De Souza Silva MA February 2007 Serotonin and psychostimulant addiction focus on 5 HT1A receptors Progress in Neurobiology 81 3 133 178 doi 10 1016 j pneurobio 2007 01 001 PMID 17316955 S2CID 42788995 Carey RJ DePalma G Damianopoulos E Shanahan A Muller CP Huston JP February 2005 Evidence that the 5 HT1A autoreceptor is an important pharmacological target for the modulation of cocaine behavioral stimulant effects Brain Research 1034 1 2 162 171 doi 10 1016 j brainres 2004 12 012 PMID 15713268 S2CID 28356741 a b de Boer SF Koolhaas JM December 2005 5 HT1A and 5 HT1B receptor agonists and aggression a pharmacological challenge of the serotonin deficiency hypothesis European Journal of Pharmacology 526 1 3 125 139 doi 10 1016 j ejphar 2005 09 065 PMID 16310183 Parks CL Robinson PS Sibille E Shenk T Toth M September 1998 Increased anxiety of mice lacking the serotonin1A receptor Proceedings of the National Academy of Sciences of the United States of America 95 18 10734 10739 Bibcode 1998PNAS 9510734P doi 10 1073 pnas 95 18 10734 PMC 27964 PMID 9724773 Ebenezer IS Arkle MJ Tite RM May 2007 8 Hydroxy 2 di n propylamino tetralin inhibits food intake in fasted rats by an action at 5 HT1A receptors Methods and Findings in Experimental and Clinical Pharmacology 29 4 269 272 doi 10 1358 mf 2007 29 4 1075362 PMID 17609739 a b Wouters W Tulp MT Bevan P May 1988 Flesinoxan lowers blood pressure and heart rate in cats via 5 HT1A receptors European Journal of Pharmacology 149 3 213 223 doi 10 1016 0014 2999 88 90651 6 PMID 2842163 a b Horiuchi J McDowall LM Dampney RA November 2008 Role of 5 HT 1A receptors in the lower brainstem on the cardiovascular response to dorsomedial hypothalamus activation Autonomic Neuroscience 142 1 2 71 76 doi 10 1016 j autneu 2008 06 004 PMID 18667366 S2CID 20878941 Nalivaiko E Ootsuka Y Blessing WW August 2005 Activation of 5 HT1A receptors in the medullary raphe reduces cardiovascular changes elicited by acute psychological and inflammatory stresses in rabbits American Journal of Physiology Regulatory Integrative and Comparative Physiology 289 2 R596 R604 doi 10 1152 ajpregu 00845 2004 PMID 15802554 S2CID 17426759 a b Lucot JB February 1994 Antiemetic effects of flesinoxan in cats comparisons with 8 hydroxy 2 di n propylamino tetralin European Journal of Pharmacology 253 1 2 53 60 doi 10 1016 0014 2999 94 90756 0 PMID 8013549 Winstanley CA Theobald DE Dalley JW Robbins TW April 2005 Interactions between serotonin and dopamine in the control of impulsive choice in rats therapeutic implications for impulse control disorders Neuropsychopharmacology 30 4 669 682 doi 10 1038 sj npp 1300610 PMID 15688093 Ogren SO Eriksson TM Elvander Tottie E D Addario C Ekstrom JC Svenningsson P et al December 2008 The role of 5 HT 1A receptors in learning and memory Behavioural Brain Research 195 1 54 77 doi 10 1016 j bbr 2008 02 023 PMID 18394726 S2CID 140205386 Yasuno F Suhara T Nakayama T Ichimiya T Okubo Y Takano A et al February 2003 Inhibitory effect of hippocampal 5 HT1A receptors on human explicit memory The American Journal of Psychiatry 160 2 334 340 doi 10 1176 appi ajp 160 2 334 PMID 12562581 Kennett GA Dourish CT Curzon G February 1987 Antidepressant like action of 5 HT1A agonists and conventional antidepressants in an animal model of depression European Journal of Pharmacology 134 3 265 274 doi 10 1016 0014 2999 87 90357 8 PMID 2883013 Bardin L Tarayre JP Malfetes N Koek W Colpaert FC April 2003 Profound non opioid analgesia produced by the high efficacy 5 HT 1A agonist F 13640 in the formalin model of tonic nociceptive pain Pharmacology 67 4 182 194 doi 10 1159 000068404 PMID 12595749 S2CID 25882138 a b Millan MJ Perrin Monneyron S March 1997 Potentiation of fluoxetine induced penile erections by combined blockade of 5 HT1A and 5 HT1B receptors European Journal of Pharmacology 321 3 R11 R13 doi 10 1016 S0014 2999 97 00050 2 PMID 9085055 Prow MR Martin KF Heal DJ December 1996 8 OH DPAT induced mydriasis in mice a pharmacological characterisation European Journal of Pharmacology 317 1 21 28 doi 10 1016 S0014 2999 96 00693 0 PMID 8982715 a b Meyer LC Fuller A Mitchell D February 2006 Zacopride and 8 OH DPAT reverse opioid induced respiratory depression and hypoxia but not catatonic immobilization in goats American Journal of Physiology Regulatory Integrative and Comparative Physiology 290 2 R405 R413 doi 10 1152 ajpregu 00440 2005 PMID 16166206 S2CID 224414 a b Popova NK Amstislavskaya TG July 2002 Involvement of the 5 HT 1A and 5 HT 1B serotonergic receptor subtypes in sexual arousal in male mice Psychoneuroendocrinology 27 5 609 618 doi 10 1016 S0306 4530 01 00097 X PMID 11965359 S2CID 25269315 Monti JM Jantos H September 1992 Dose dependent effects of the 5 HT1A receptor agonist 8 OH DPAT on sleep and wakefulness in the rat Journal of Sleep Research 1 3 169 175 doi 10 1111 j 1365 2869 1992 tb00033 x PMID 10607047 Thompson MR Callaghan PD Hunt GE Cornish JL McGregor IS May 2007 A role for oxytocin and 5 HT 1A receptors in the prosocial effects of 3 4 methylenedioxymethamphetamine ecstasy Neuroscience 146 2 509 514 doi 10 1016 j neuroscience 2007 02 032 PMID 17383105 S2CID 15617471 Gudelsky GA Koenig JI Meltzer HY December 1986 Thermoregulatory responses to serotonin 5 HT receptor stimulation in the rat Evidence for opposing roles of 5 HT2 and 5 HT1A receptors Neuropharmacology 25 12 1307 1313 doi 10 1016 0028 3908 86 90101 2 PMID 2951611 S2CID 2547042 Ootsuka Y Blessing WW February 2006 Activation of 5 HT1A receptors in rostral medullary raphe inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits Brain Research 1073 1074 252 261 doi 10 1016 j brainres 2005 12 031 PMID 16455061 S2CID 23178233 a b c d e f g h i j k l m n o p q r s t u Pharmacology Corner gt Serotonin 5 HT receptors agonists and antagonists By Flavio Guzman M D on 9 08 09 a b c d e BRINTELLIX vortioxetine tablets for oral use Full Prescribing Information Section 12 2 Pharmacodynamics Takeda Pharmaceuticals America Inc and Lundbeck 2013 Revised September 2013 1 Archived 2019 09 18 at the Wayback Machine Saxena PR Lawang A October 1985 A comparison of cardiovascular and smooth muscle effects of 5 hydroxytryptamine and 5 carboxamidotryptamine a selective agonist of 5 HT1 receptors Archives Internationales de Pharmacodynamie et de Therapie 277 2 235 252 PMID 2933009 Cao BJ Rodgers RJ October 1998 Comparative effects of novel 5 HT1A receptor ligands LY293284 LY315712 and LY297996 on plus maze anxiety in mice Psychopharmacology 139 3 185 194 doi 10 1007 s002130050703 PMID 9784072 S2CID 9466299 Harrison AA Parsons LH Koob GF Markou A January 1999 RU 24969 a 5 HT1A 1B agonist elevates brain stimulation reward thresholds an effect reversed by GR 127935 a 5 HT1B 1D antagonist Psychopharmacology 141 3 242 250 doi 10 1007 s002130050831 PMID 10027505 S2CID 19974789 Chojnacka Wojcik E Klodzinska A Tatarczynska E February 2005 The anxiolytic like effect of 5 HT1B receptor ligands in rats a possible mechanism of action The Journal of Pharmacy and Pharmacology 57 2 253 257 doi 10 1211 0022357055399 PMID 15720791 S2CID 20743875 Lin D Parsons LH April 2002 Anxiogenic like effect of serotonin 1B receptor stimulation in the rat elevated plus maze Pharmacology Biochemistry and Behavior 71 4 581 587 doi 10 1016 S0091 3057 01 00712 2 PMID 11888549 S2CID 21610537 a b Tatarczynska E Klodzinska A Stachowicz K Chojnacka Wojcik E December 2004 Effects of a selective 5 HT1B receptor agonist and antagonists in animal models of anxiety and depression Behavioural Pharmacology 15 8 523 534 doi 10 1097 00008877 200412000 00001 PMID 15577451 S2CID 6940756 a b Eriksson TM Madjid N Elvander Tottie E Stiedl O Svenningsson P Ogren SO June 2008 Blockade of 5 HT 1B receptors facilitates contextual aversive learning in mice by disinhibition of cholinergic and glutamatergic neurotransmission Neuropharmacology 54 7 1041 1050 doi 10 1016 j neuropharm 2008 02 007 hdl 10616 40922 PMID 18394658 S2CID 207223573 a b McCreary AC Bankson MG Cunningham KA September 1999 Pharmacological studies of the acute and chronic effects of 3 4 methylenedioxymethamphetamine on locomotor activity role of 5 hydroxytryptamine 1A and 5 hydroxytryptamine 1B 1D receptors The Journal of Pharmacology and Experimental Therapeutics 290 3 965 973 PMID 10454466 Amital D Fostick L Sasson Y Kindler S Amital H Zohar J May 2005 Anxiogenic effects of Sumatriptan in panic disorder a double blind placebo controlled study European Neuropsychopharmacology 15 3 279 282 doi 10 1016 j euroneuro 2004 12 002 PMID 15820416 S2CID 8382188 Feuerstein TJ Huring H van Velthoven V Lucking CH Landwehrmeyer GB May 1996 5 HT1D like receptors inhibit the release of endogenously formed 3H GABA in human but not in rabbit neocortex Neuroscience Letters 209 3 210 214 doi 10 1016 0304 3940 96 12637 9 PMID 8736648 S2CID 27376524 Najjar SA Hung LY Margolis KG June 2023 Serotonergic Control of Gastrointestinal Development Motility and Inflammation Comprehensive Physiology 13 3 4851 4868 doi 10 1002 cphy c220024 ISBN 9780470650714 PMC 10373054 PMID 37358510 Branchek TA Mawe GM Gershon MD July 1988 Characterization and localization of a peripheral neural 5 hydroxytryptamine receptor subtype 5 HT1P with a selective agonist 3H 5 hydroxyindalpine The Journal of Neuroscience 8 7 2582 2595 doi 10 1523 JNEUROSCI 08 07 02582 1988 PMC 6569501 PMID 3249244 Mawe GM Branchek TA Gershon MD December 1986 Peripheral neural serotonin receptors identification and characterization with specific antagonists and agonists Proceedings of the National Academy of Sciences of the United States of America 83 24 9799 9803 Bibcode 1986PNAS 83 9799M doi 10 1073 pnas 83 24 9799 PMC 387229 PMID 3467338 Annahazi Anita Berger Thomas Erwin Demir Ihsan Ekin Zeller Florian Muller Michael Anneser Markus Skerra Arne Michel Klaus Schemann Michael April 2022 Metabotropic 5 HT receptor mediated effects in the human submucous plexus Neurogastroenterology amp Motility 34 10 e14380 doi 10 1111 nmo 14380 ISSN 1350 1925 PMID 35438222 S2CID 248241342 a b Bubar MJ Cunningham KA 2006 Serotonin 5 HT2A and 5 HT2C receptors as potential targets for modulation of psychostimulant use and dependence Current Topics in Medicinal Chemistry 6 18 1971 1985 doi 10 2174 156802606778522131 PMID 17017968 Schreiber R Melon C De Vry J February 1998 The role of 5 HT receptor subtypes in the anxiolytic effects of selective serotonin reuptake inhibitors in the rat ultrasonic vocalization test Psychopharmacology 135 4 383 391 doi 10 1007 s002130050526 PMID 9539263 S2CID 22677071 a b Popova NK Amstislavskaya TG July 2002 5 HT2A and 5 HT2C serotonin receptors differentially modulate mouse sexual arousal and the hypothalamo pituitary testicular response to the presence of a female Neuroendocrinology 76 1 28 34 doi 10 1159 000063681 PMID 12097814 S2CID 42319246 a b Popa D Lena C Fabre V Prenat C Gingrich J Escourrou P et al December 2005 Contribution of 5 HT2 receptor subtypes to sleep wakefulness and respiratory control and functional adaptations in knock out mice lacking 5 HT2A receptors The Journal of Neuroscience 25 49 11231 11238 doi 10 1523 JNEUROSCI 1724 05 2005 PMC 6725907 PMID 16339018 a b Mazzola Pomietto P Aulakh CS Tolliver T Murphy DL March 1997 Functional subsensitivity of 5 HT2A and 5 HT2C receptors mediating hyperthermia following acute and chronic treatment with 5 HT2A 2C receptor antagonists Psychopharmacology 130 2 144 151 doi 10 1007 s002130050222 PMID 9106912 S2CID 22432569 Blessing WW Seaman B 2003 5 hydroxytryptamine 2A receptors regulate sympathetic nerves constricting the cutaneous vascular bed in rabbits and rats Neuroscience 117 4 939 948 doi 10 1016 S0306 4522 02 00810 2 PMID 12654345 S2CID 53251590 a b c McCall RB Franklin SR Hyslop DK Knauer CS Chio CL Haber CL Fitzgerald LW 2001 PNU 22394 a 5 HT2C receptor agonist reduced feeding in rodents and produces weight loss in humans Online Society for Neuroscience Vol 27 Presentation Number 309 2 San Diego CA Society for Neuroscience Abstracts p TT 45 Retrieved 18 July 2014 a b c Garfield AS Heisler LK January 2009 Pharmacological targeting of the serotonergic system for the treatment of obesity The Journal of Physiology 587 1 49 60 doi 10 1113 jphysiol 2008 164152 PMC 2670022 PMID 19029184 a b c Jensen AA Plath N Pedersen MH Isberg V Krall J Wellendorph P et al February 2013 Design synthesis and pharmacological characterization of N and O substituted 5 6 7 8 tetrahydro 4H isoxazolo 4 5 d azepin 3 ol analogues novel 5 HT 2A 5 HT 2C receptor agonists with pro cognitive properties Journal of Medicinal Chemistry 56 3 1211 1227 CiteSeerX 10 1 1 691 154 doi 10 1021 jm301656h PMID 23301527 Kennett GA Bright F Trail B Baxter GS Blackburn TP April 1996 Effects of the 5 HT2B receptor agonist BW 723C86 on three rat models of anxiety British Journal of Pharmacology 117 7 1443 1448 doi 10 1111 j 1476 5381 1996 tb15304 x PMC 1909458 PMID 8730737 Duxon MS Kennett GA Lightowler S Blackburn TP Fone KC 1997 Activation of 5 HT2B receptors in the medial amygdala causes anxiolysis in the social interaction test in the rat Neuropharmacology 36 4 5 601 608 doi 10 1016 S0028 3908 97 00042 7 PMID 9225285 S2CID 41471226 Kennett GA Trail B Bright F December 1998 Anxiolytic like actions of BW 723C86 in the rat Vogel conflict test are 5 HT2B receptor mediated Neuropharmacology 37 12 1603 1610 doi 10 1016 S0028 3908 98 00115 4 PMID 9886683 S2CID 7310462 Kennett GA Ainsworth K Trail B Blackburn TP February 1997 BW 723C86 a 5 HT2B receptor agonist causes hyperphagia and reduced grooming in rats Neuropharmacology 36 2 233 239 doi 10 1016 S0028 3908 96 00171 2 PMID 9144661 S2CID 23583570 Borman RA Tilford NS Harmer DW Day N Ellis ES Sheldrick RL et al March 2002 5 HT 2B receptors play a key role in mediating the excitatory effects of 5 HT in human colon in vitro British Journal of Pharmacology 135 5 1144 1151 doi 10 1038 sj bjp 0704571 PMC 1573235 PMID 11877320 Kennett GA Wood MD Bright F Trail B Riley G Holland V et al 1997 SB 242084 a selective and brain penetrant 5 HT2C receptor antagonist Neuropharmacology 36 4 5 609 620 doi 10 1016 S0028 3908 97 00038 5 PMID 9225286 S2CID 23032157 a b Millan MJ Brocco M Gobert A Dekeyne A February 2005 Anxiolytic properties of agomelatine an antidepressant with melatoninergic and serotonergic properties role of 5 HT2C receptor blockade Psychopharmacology 177 4 448 458 doi 10 1007 s00213 004 1962 z PMID 15289999 S2CID 20866665 a b Dekeyne A Mannoury la Cour C Gobert A Brocco M Lejeune F Serres F et al September 2008 S32006 a novel 5 HT2C receptor antagonist displaying broad based antidepressant and anxiolytic properties in rodent models Psychopharmacology 199 4 549 568 doi 10 1007 s00213 008 1177 9 PMID 18523738 S2CID 25063495 Fujitsuka N Asakawa A Hayashi M Sameshima M Amitani H Kojima S et al May 2009 Selective serotonin reuptake inhibitors modify physiological gastrointestinal motor activities via 5 HT2c receptor and acyl ghrelin Biological Psychiatry 65 9 748 759 doi 10 1016 j biopsych 2008 10 031 PMID 19058784 S2CID 22053616 Millan MJ Peglion JL Lavielle G Perrin Monneyron S April 1997 5 HT2C receptors mediate penile erections in rats actions of novel and selective agonists and antagonists European Journal of Pharmacology 325 1 9 12 doi 10 1016 S0014 2999 97 89962 1 PMID 9151932 Stancampiano R Melis MR Argiolas A August 1994 Penile erection and yawning induced by 5 HT1C receptor agonists in male rats relationship with dopaminergic and oxytocinergic transmission European Journal of Pharmacology 261 1 2 149 155 doi 10 1016 0014 2999 94 90313 1 PMID 8001637 Frank MG Stryker MP Tecott LH November 2002 Sleep and sleep homeostasis in mice lacking the 5 HT2c receptor Neuropsychopharmacology 27 5 869 873 doi 10 1016 S0893 133X 02 00353 6 PMC 2452994 PMID 12431861 Villalobos CA Bull P Saez P Cassels BK Huidobro Toro JP April 2004 4 Bromo 2 5 dimethoxyphenethylamine 2C B and structurally related phenylethylamines are potent 5 HT2A receptor antagonists in Xenopus laevis oocytes British Journal of Pharmacology 141 7 1167 1174 doi 10 1038 sj bjp 0705722 PMC 1574890 PMID 15006903 Rang HP 2003 Pharmacology Edinburgh Churchill Livingstone ISBN 978 0 443 07145 4 Page 187 Michel K Zeller F Langer R Nekarda H Kruger D Dover TJ et al May 2005 Serotonin excites neurons in the human submucous plexus via 5 HT3 receptors Gastroenterology 128 5 1317 1326 doi 10 1053 j gastro 2005 02 005 PMID 15887114 a b Pitsikas N Brambilla A Borsini F January 1994 Effect of DAU 6215 a novel 5 HT3 receptor antagonist on scopolamine induced amnesia in the rat in a spatial learning task Pharmacology Biochemistry and Behavior 47 1 95 99 doi 10 1016 0091 3057 94 90116 3 PMID 8115433 S2CID 21800364 a b Smriga M Torii K December 2003 L Lysine acts like a partial serotonin receptor 4 antagonist and inhibits serotonin mediated intestinal pathologies and anxiety in rats Proceedings of the National Academy of Sciences of the United States of America 100 26 15370 15375 Bibcode 2003PNAS 10015370S doi 10 1073 pnas 2436556100 PMC 307574 PMID 14676321 Kennett GA Bright F Trail B Blackburn TP Sanger GJ 1997 Anxiolytic like actions of the selective 5 HT4 receptor antagonists SB 204070A and SB 207266A in rats Neuropharmacology 36 4 5 707 712 doi 10 1016 S0028 3908 97 00037 3 PMID 9225297 S2CID 40341646 Jean A Conductier G Manrique C Bouras C Berta P Hen R et al October 2007 Anorexia induced by activation of serotonin 5 HT4 receptors is mediated by increases in CART in the nucleus accumbens Proceedings of the National Academy of Sciences of the United States of America 104 41 16335 16340 Bibcode 2007PNAS 10416335J doi 10 1073 pnas 0701471104 PMC 2042207 PMID 17913892 Compan V Charnay Y Dusticier N Daszuta A Hen R Bockaert J 2004 Feeding disorders in 5 HT4 receptor knockout mice Journal de la Societe de Biologie 198 1 37 49 doi 10 1051 jbio 2004198010037 PMID 15146954 S2CID 90408378 a b Meneses A Hong E March 1997 Effects of 5 HT4 receptor agonists and antagonists in learning Pharmacology Biochemistry and Behavior 56 3 347 351 doi 10 1016 S0091 3057 96 00224 9 PMID 9077568 S2CID 11866740 a b Fontana DJ Daniels SE Wong EH Clark RD Eglen RM 1997 The effects of novel selective 5 hydroxytryptamine 5 HT 4 receptor ligands in rat spatial navigation Neuropharmacology 36 4 5 689 696 doi 10 1016 S0028 3908 97 00055 5 PMID 9225295 S2CID 46510811 Galeotti N Ghelardini C Bartolini A September 1998 Role of 5 HT4 receptors in the mouse passive avoidance test The Journal of Pharmacology and Experimental Therapeutics 286 3 1115 1121 PMID 9732367 Lucas G Rymar VV Du J Mnie Filali O Bisgaard C Manta S et al September 2007 Serotonin 4 5 HT 4 receptor agonists are putative antidepressants with a rapid onset of action Neuron 55 5 712 725 doi 10 1016 j neuron 2007 07 041 PMID 17785179 S2CID 14558104 Duman RS September 2007 A silver bullet for the treatment of depression Neuron 55 5 679 681 doi 10 1016 j neuron 2007 08 011 PMID 17785173 Manzke T Guenther U Ponimaskin EG Haller M Dutschmann M Schwarzacher S Richter DW July 2003 5 HT4 a receptors avert opioid induced breathing depression without loss of analgesia Science 301 5630 226 229 Bibcode 2003Sci 301 226M doi 10 1126 science 1084674 PMID 12855812 S2CID 13641423 Nelson DL February 2004 5 HT5 receptors Current Drug Targets CNS and Neurological Disorders 3 1 53 58 doi 10 2174 1568007043482606 PMID 14965244 a b Dietz BM Mahady GB Pauli GF Farnsworth NR August 2005 Valerian extract and valerenic acid are partial agonists of the 5 HT5a receptor in vitro Brain Research Molecular Brain Research 138 2 191 197 doi 10 1016 j molbrainres 2005 04 009 PMC 5805132 PMID 15921820 a b c Zhang S Chen H Zhang C Yang Y Popov P Liu J et al July 2022 Inactive and active state structures template selective tools for the human 5 HT5A receptor Nature Structural amp Molecular Biology 29 7 677 687 doi 10 1038 s41594 022 00796 6 PMC 9299520 PMID 35835867 Wesolowska A February 2008 The anxiolytic like effect of the selective 5 HT6 receptor antagonist SB 399885 the impact of benzodiazepine receptors European Journal of Pharmacology 580 3 355 360 doi 10 1016 j ejphar 2007 11 022 PMID 18096153 a b Wesolowska A Nikiforuk A April 2007 Effects of the brain penetrant and selective 5 HT6 receptor antagonist SB 399885 in animal models of anxiety and depression Neuropharmacology 52 5 1274 1283 doi 10 1016 j neuropharm 2007 01 007 PMID 17320917 S2CID 22664564 Hirst WD Stean TO Rogers DC Sunter D Pugh P Moss SF et al December 2006 SB 399885 is a potent selective 5 HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models European Journal of Pharmacology 553 1 3 109 119 doi 10 1016 j ejphar 2006 09 049 PMID 17069795 a b Perez Garcia G Meneses A July 2005 Oral administration of the 5 HT6 receptor antagonists SB 357134 and SB 399885 improves memory formation in an autoshaping learning task Pharmacology Biochemistry and Behavior 81 3 673 682 doi 10 1016 j pbb 2005 05 005 PMID 15964617 S2CID 19789219 Wesolowska A Nikiforuk A March 2008 The selective 5 HT 6 receptor antagonist SB 399885 enhances anti immobility action of antidepressants in rats European Journal of Pharmacology 582 1 3 88 93 doi 10 1016 j ejphar 2007 12 013 PMID 18234190 Alcalde E Mesquida N Lopez Perez S Frigola J Merce R Feb 2009 Indene based scaffolds 2 An indole indene switch discovery of novel indenylsulfonamides as 5 HT6 serotonin receptor agonists Journal of Medicinal Chemistry 52 3 675 87 doi 10 1021 jm8009469 PMID 19159187 Target Schizophrenia Possible future developments The Association of the British Pharmaceutical Industry Archived from the original on 2008 06 12 Retrieved 2008 04 11 a b c Hedlund PB Huitron Resendiz S Henriksen SJ Sutcliffe JG November 2005 5 HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern Biological Psychiatry 58 10 831 837 doi 10 1016 j biopsych 2005 05 012 PMID 16018977 S2CID 10998014 a b Wesolowska A Nikiforuk A Stachowicz K Tatarczynska E September 2006 Effect of the selective 5 HT7 receptor antagonist SB 269970 in animal models of anxiety and depression Neuropharmacology 51 3 578 586 doi 10 1016 j neuropharm 2006 04 017 PMID 16828124 S2CID 39928418 Gasbarri A Cifariello A Pompili A Meneses A December 2008 Effect of 5 HT 7 antagonist SB 269970 in the modulation of working and reference memory in the rat Behavioural Brain Research 195 1 164 170 doi 10 1016 j bbr 2007 12 020 PMID 18308404 S2CID 12910296 Liy Salmeron G Meneses A 2008 Effects of 5 HT drugs in prefrontal cortex during memory formation and the ketamine amnesia model Hippocampus 18 9 965 974 doi 10 1002 hipo 20459 PMID 18570192 S2CID 20937527 a b Bonaventure P Kelly L Aluisio L Shelton J Lord B Galici R et al May 2007 Selective blockade of 5 hydroxytryptamine 5 HT 7 receptors enhances 5 HT transmission antidepressant like behavior and rapid eye movement sleep suppression induced by citalopram in rodents The Journal of Pharmacology and Experimental Therapeutics 321 2 690 698 doi 10 1124 jpet 107 119404 PMID 17314195 S2CID 14579645 Thomas DR Melotto S Massagrande M Gribble AD Jeffrey P Stevens AJ et al June 2003 SB 656104 A a novel selective 5 HT7 receptor antagonist modulates REM sleep in rats British Journal of Pharmacology 139 4 705 714 doi 10 1038 sj bjp 0705290 PMC 1573887 PMID 12812993 Leon Ponte Matilde Ahern Gerard P O Connell Peta J 2007 04 15 Serotonin provides an accessory signal to enhance T cell activation by signaling through the 5 HT7 receptor Blood 109 8 3139 3146 doi 10 1182 blood 2006 10 052787 ISSN 0006 4971 PMC 1852236 PMID 17158224 Davies MA Sheffler DJ Roth BL Aripiprazole A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology CNS Drug Reviews Internet 2004 cited 2013 Aug 4 10 4 317 36 Available from http onlinelibrary wiley com doi 10 1111 j 1527 3458 2004 tb00030 x pdf HTR2C 5 hydroxytryptamine receptor 2C Homo sapiens human NCBI 19 Mar 2017 Retrieved 26 Mar 2017 Bar Shira O Maor R Chechik G December 2015 Gene Expression Switching of Receptor Subunits in Human Brain Development PLOS Computational Biology 11 12 e1004559 Bibcode 2015PLSCB 11E4559B doi 10 1371 journal pcbi 1004559 PMC 4670163 PMID 26636753 Saxena PR De Vries P Villalon CM August 1998 5 HT1 like receptors a time to bid goodbye Trends in Pharmacological Sciences 19 8 311 316 doi 10 1016 S0165 6147 98 01228 0 PMID 9745358 External links editSerotonin Receptors at the U S National Library of Medicine Medical Subject Headings MeSH 5 Hydroxytryptamine Receptors IUPHAR Database of Receptors and Ion Channels International Union of Basic and Clinical Pharmacology Rubenstein LA Lanzara RG 2005 02 16 Activation of G protein coupled receptors entails cysteine modulation of agonist binding Cogprints Retrieved 2008 04 11 Paterson LM Kornum BR Nutt DJ Pike VW Knudsen GM January 2013 5 HT radioligands for human brain imaging with PET and SPECT Medicinal Research Reviews 33 1 54 111 doi 10 1002 med 20245 PMC 4188513 PMID 21674551 Retrieved from https en wikipedia org w index php title 5 HT receptor amp oldid 1215963881, wikipedia, wiki, book, books, library,

article

, read, download, free, free download, mp3, video, mp4, 3gp, jpg, jpeg, gif, png, picture, music, song, movie, book, game, games.