5-HT₆ receptor

The 5HT₆ receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT).^[5] It is a G protein-coupled receptor (GPCR) that is coupled to G_s and mediates excitatory neurotransmission.^[5] HTR6 denotes the human gene encoding for the receptor.^[6]

HTR6
Identifiers
Aliases	HTR6, 5-HT6, 5-HT6R, 5-HT6 receptor, 5-hydroxytryptamine receptor 6
External IDs	OMIM: 601109 MGI: 1196627 HomoloGene: 673 GeneCards: HTR6
Gene location (Human) Chr. Chromosome 1 (human)^[1] Band 1p36.13 Start 19,664,875 bp^[1] End 19,680,966 bp^[1]
Gene location (Mouse) Chr. Chromosome 4 (mouse)^[2] Band 4 D3|4 70.57 cM Start 138,788,419 bp^[2] End 138,802,881 bp^[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in Brodmann area 10 pancreatic ductal cell frontal pole mucosa of urinary bladder middle frontal gyrus external globus pallidus body of tongue pericardium inferior ganglion of vagus nerve Brodmann area 46 Top expressed in superior frontal gyrus cerebellar cortex hippocampus proper neck digastric muscle olfactory bulb thoracic diaphragm carotid body submandibular gland neural tube More reference expression data BioGPS More reference expression data
Gene ontology Molecular function histamine receptor activity protein binding G protein-coupled receptor activity signal transducer activity neurotransmitter receptor activity G protein-coupled serotonin receptor activity Cellular component integral component of membrane plasma membrane integral component of plasma membrane cilium membrane dendrite Biological process G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger cerebral cortex cell migration positive regulation of TOR signaling signal transduction chemical synaptic transmission G protein-coupled serotonin receptor signaling pathway G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 3362 15565 Ensembl ENSG00000158748 ENSMUSG00000028747 UniProt P50406 Q9R1C8 RefSeq (mRNA) NM_000871 NM_021358 NM_001377096 RefSeq (protein) NP_000862 NP_067333 NP_001364025 Location (UCSC) Chr 1: 19.66 – 19.68 Mb Chr 4: 138.79 – 138.8 Mb PubMed search ^[3] ^[4]
Wikidata
View/Edit Human View/Edit Mouse

Distribution

The 5HT₆ receptor is expressed almost exclusively in the brain.^[7] It is distributed in various areas including, but not limited to, the olfactory tubercle, cerebral cortex (frontal and entorhinal regions), nucleus accumbens, striatum, caudate nucleus, hippocampus, and the molecular layer of the cerebellum.^[5][8][9] Based on its abundance in extrapyramidal, limbic, and cortical regions it can be suggested that the 5HT₆ receptor plays a role in functions like motor control, emotionality, cognition, and memory.^[7][9][10]

Function

Blockade of central 5HT₆ receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas,^{[11][12][13][14]} whereas activation enhances GABAergic signaling in a widespread manner.^[15] Antagonism of 5HT₆ receptors also facilitates dopamine and norepinephrine release in the frontal cortex,^[14][16] while stimulation has the opposite effect.^[15]

As a drug target for antagonists

Despite the 5HT₆ receptor having a functionally excitatory action, it is largely co-localized with GABAergic neurons and therefore produces an overall inhibition of brain activity.^[15] In parallel with this, 5HT₆ antagonists are hypothesized to improve cognition, learning, and memory.^[17] Agents such as latrepirdine, idalopirdine (Lu AE58054), and intepirdine (SB-742,457/RVT-101) were evaluated as novel treatments for Alzheimer's disease and other forms of dementia.^[14][18][19] However, phase III trials of latrepirdine, idalopirdine, and intepirdine have failed to demonstrate efficacy.

5HT₆ antagonists have also been shown to reduce appetite and produce weight loss, and as a result, PRX-07034, BVT-5,182, and BVT-74,316 are being investigated for the treatment of obesity.^[20][21]

As a drug target for agonists

Recently, the 5HT₆ agonists WAY-181,187 and WAY-208,466 have been demonstrated to be active in rodent models of depression, anxiety, and obsessive-compulsive disorder (OCD), and such agents may be useful treatments for these conditions.^[15][22] Additionally, indirect 5HT₆ activation may play a role in the therapeutic benefits of serotonergic antidepressants like the selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants (TCAs).^{[citation needed]}

Ligands

A large number of selective 5HT₆ ligands have now been developed.^{[23][24][25][26][27][28][29][30][31]}

Agonists

Full agonists

• 2-Ethyl-5-methoxy-N,N-dimethyltryptamine (EMDT)^[32]
• WAY-181,187
• WAY-208,466
• N-(inden-5-yl)imidazothiazole-5-sulfonamide (43): K_i = 4.5nM, EC₅₀ = 0.9nM, E_max = 98%^[33]
• E-6837 – Full agonist at human 5HT₆ receptors

Partial agonists

• E-6801^[34]
• E-6837 – partial agonist at rat 5-HT₆ receptors. Orally active in rats, and caused weight loss with chronic administration^[35]
• EMD-386,088 – potent partial agonist (EC₅₀ = 1 nM) but non-selective^[36][37]
• LSD – E_max = 60%^[38]

Antagonists and inverse agonists

• ALX-1161
• AVN-211
• BVT-5182^[39]
• BVT-74316^[20]
• Cerlapirdine – selective
• EGIS-12233 – mixed 5HT₆ / 5HT₇ antagonist
• Idalopirdine (Lu AE58054) – selective
• Intepirdine (SB-742,457/RVT-101) – selective antagonist
• Landipirdine (RO-5025181, SYN-120)
• Latrepirdine^[40] (non-selective) and analogues^[41]
• MS-245
• PRX-07034
• SB-258,585
• SB-271,046
• SB-357,134
• SB-399,885
• SGS 518 Fb: [445441-26-9]
• Ro 04-6790
• Ro-4368554^[42]
• Atypical antipsychotics (sertindole, olanzapine, asenapine, clozapine)
• WAY-255315 / SAM-315: K_i = 1.1 nM, IC₅₀ = 13 nM^[43]
• Rosa rugosa extract^[44]

Genetics

Polymorphisms in the HTR6 gene are associated with neuropsychiatric disorders. For example, an association between the C267T (rs1805054) polymorphism and Alzheimer's disease has been shown.^[45] Others have studied the polymorphism in relation to Parkinson's disease.^[46]

See also

• 5-HT receptor
• 5-HT₁ receptor
• 5-HT₂ receptor
• 5-HT₃ receptor
• 5-HT₄ receptor
• 5-HT₅ receptor

References

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2. GRCm38: Ensembl release 89: ENSMUSG00000028747 - Ensembl, May 2017
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Further reading

• Hoyer D, Hannon JP, Martin GR (April 2002). "Molecular, pharmacological and functional diversity of 5-HT receptors". Pharmacology Biochemistry and Behavior. 71 (4): 533–54. doi:10.1016/S0091-3057(01)00746-8. PMID 11888546. S2CID 25543069.
• Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, Grewal JS, Garnovskaya MN (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction". Pharmacology & Therapeutics. 92 (2–3): 179–212. doi:10.1016/S0163-7258(01)00169-3. PMID 11916537.
• Van Oekelen D, Luyten WH, Leysen JE (April 2003). "5-HT2A and 5-HT2C receptors and their atypical regulation properties". Life Sciences. 72 (22): 2429–49. doi:10.1016/S0024-3205(03)00141-3. PMID 12650852.
• Dubertret C, Hanoun N, Adès J, Hamon M, Gorwood P (April 2004). "Family-based association study of the serotonin-6 receptor gene (C267T polymorphism) in schizophrenia". American Journal of Medical Genetics Part B. 126B (1): 10–5. doi:10.1002/ajmg.b.20120. PMID 15048641. S2CID 24710946.
• Ullmer C, Schmuck K, Kalkman HO, Lübbert H (August 1995). "Expression of serotonin receptor mRNAs in blood vessels". FEBS Letters. 370 (3): 215–21. doi:10.1016/0014-5793(95)00828-W. PMID 7656980.
• Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW (January 1996). "Cloning, characterization, and chromosomal localization of a human 5-HT₆ serotonin receptor". Journal of Neurochemistry. 66 (1): 47–56. doi:10.1046/j.1471-4159.1996.66010047.x. PMID 8522988. S2CID 35874409.
• Orlacchio A, Kawarai T, Paciotti E, Stefani A, Orlacchio A, Sorbi S, St George-Hyslop PH, Bernardi G (May 2002). "Association study of the 5-hydroxytryptamine(6) receptor gene in Alzheimer's disease". Neuroscience Letters. 325 (1): 13–6. doi:10.1016/S0304-3940(02)00221-5. PMID 12023056. S2CID 45464124.
• Ham BJ, Kim YH, Choi MJ, Cha JH, Choi YK, Lee MS (January 2004). "Serotonergic genes and personality traits in the Korean population". Neuroscience Letters. 354 (1): 2–5. doi:10.1016/S0304-3940(03)00753-5. PMID 14698468. S2CID 22448256.
• Bernotas R, Lenicek S, Antane S, Zhang GM, Smith D, Coupet J, Harrison B, Schechter LE (November 2004). "1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT₆ receptor ligands". Bioorganic & Medicinal Chemistry Letters. 14 (22): 5499–502. doi:10.1016/j.bmcl.2004.09.003. PMID 15482912.
• Kang H, Lee WK, Choi YH, Vukoti KM, Bang WG, Yu YG (April 2005). "Molecular analysis of the interaction between the intracellular loops of the human serotonin receptor type 6 (5-HT₆) and the alpha subunit of GS protein". Biochemical and Biophysical Research Communications. 329 (2): 684–92. doi:10.1016/j.bbrc.2005.02.040. PMID 15737640.
• Tao WA, Wollscheid B, O'Brien R, Eng JK, Li XJ, Bodenmiller B, Watts JD, Hood L, Aebersold R (August 2005). "Quantitative phosphoproteome analysis using a dendrimer conjugation chemistry and tandem mass spectrometry". Nature Methods. 2 (8): 591–8. doi:10.1038/nmeth776. PMID 16094384. S2CID 20475874.
• Lorke DE, Lu G, Cho E, Yew DT (2006). "Serotonin 5-HT2A and 5-HT₆ receptors in the prefrontal cortex of Alzheimer and normal aging patients". BMC Neuroscience. 7: 36. doi:10.1186/1471-2202-7-36. PMC 1523198. PMID 16640790.
• Yun HM, Kim S, Kim HJ, Kostenis E, Kim JI, Seong JY, Baik JH, Rhim H (February 2007). "The novel cellular mechanism of human 5-HT₆ receptor through an interaction with Fyn". The Journal of Biological Chemistry. 282 (8): 5496–505. doi:10.1074/jbc.M606215200. PMID 17189269.

External links

• "5-HT₆". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
• serotonin+6+receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
• Human HTR6 genome location and HTR6 gene details page in the UCSC Genome Browser.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.