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Mosapride

January 01, 1970

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist,[1] which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans,[2] and is used for the treatment of gastritis, gastroesophageal reflux disease, functional dyspepsia[3] and irritable bowel syndrome.[4] It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food).[5]

Mosapride
Clinical data
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
  • 4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide
CAS Number
  • 112885-41-3 N
PubChem CID
  • 119584
IUPHAR/BPS
  • 242
DrugBank
  • DB11675 Y
ChemSpider
  • 106780 Y
UNII
  • I8MFJ1C0BY
KEGG
  • D08236 Y
ChEBI
  • CHEBI:94373
ChEMBL
  • ChEMBL60889 Y
CompTox Dashboard (EPA)
  • DTXSID2048408
ECHA InfoCard100.127.999
Chemical and physical data
FormulaC21H25ClFN3O3
Molar mass421.90 g·mol−1
3D model (JSmol)
  • Interactive image
  • Clc1cc(c(OCC)cc1N)C(=O)NCC3OCCN(Cc2ccc(F)cc2)C3
  • InChI=1S/C21H25ClFN3O3/c1-2-28-20-10-19(24)18(22)9-17(20)21(27)25-11-16-13-26(7-8-29-16)12-14-3-5-15(23)6-4-14/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27) Y
  • Key:YPELFRMCRYSPKZ-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

In addition to its prokinetic properties, mosapride also exerts anti-inflammatory effects on the gastrointestinal tract which may contribute to some of its therapeutic effects.[6] Mosapride also promotes neurogenesis in the gastrointestinal tract which may prove useful in certain bowel disorders.[7][8] The neurogenesis is due to mosapride's effect on the 5-HT4 receptor where it acts as an agonist.[9]

Its common side effects include dry mouth, abdominal pain, dizziness, headache, insomnia, malaise, nausea, diarrhea and sometimes constipation.[3][10] Unlike some other prokinetic agents, mosapride has little effect on potassium channels, no effect on hERG transfected cells, and no effect on cardiovascular function that could be detected in tests on humans.[1][11] Due to the pharmacokinetics of mosapride, it would take 1,000–3,000 times the therapeutic dose to elicit cardiovascular effects.[12]

References edit

  1. ^ a b Tack J, Camilleri M, Chang L, Chey WD, Galligan JJ, Lacy BE, et al. (April 2012). "Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders". Alimentary Pharmacology & Therapeutics. 35 (7): 745–67. doi:10.1111/j.1365-2036.2012.05011.x. PMC 3491670. PMID 22356640.
  2. ^ Odaka T, Suzuki T, Seza A, Yamaguchi T, Saisho H (August 2006). "[Serotonin 5- HT4 receptor agonist (mosapride citrate)]". Nihon Rinsho. Japanese Journal of Clinical Medicine (in Japanese). 64 (8): 1491–4. PMID 16898619.
  3. ^ a b Curran MP, Robinson DM (2008). "Mosapride in gastrointestinal disorders". Drugs. 68 (7): 981–91. doi:10.2165/00003495-200868070-00007. PMID 18457463. S2CID 195686202.
  4. ^ Mizuta Y, Shikuwa S, Isomoto H, Mishima R, Akazawa Y, Masuda J, et al. (November 2006). "Recent insights into digestive motility in functional dyspepsia". Journal of Gastroenterology. 41 (11): 1025–40. doi:10.1007/s00535-006-1966-z. PMID 17160514. S2CID 13353302.
  5. ^ Kato S, Morie T, Yoshida N (April 1995). "Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent". Chemical & Pharmaceutical Bulletin. 43 (4): 699–702. doi:10.1248/cpb.43.699. PMID 7600620.
  6. ^ Tsuchida Y, Hatao F, Fujisawa M, Murata T, Kaminishi M, Seto Y, et al. (May 2011). "Neuronal stimulation with 5-hydroxytryptamine 4 receptor induces anti-inflammatory actions via α7nACh receptors on muscularis macrophages associated with postoperative ileus". Gut. 60 (5): 638–47. doi:10.1136/gut.2010.227546. PMC 3071096. PMID 21115544.
  7. ^ Kawahara I, Kuniyasu H, Matsuyoshi H, Goto K, Obata K, Misawa H, et al. (March 2012). "Comparison of effects of a selective 5-HT reuptake inhibitor versus a 5-HT4 receptor agonist on in vivo neurogenesis at the rectal anastomosis in rats". American Journal of Physiology. Gastrointestinal and Liver Physiology. 302 (6): G588-97. doi:10.1152/ajpgi.00284.2011. hdl:10564/2701. PMID 22194416.
  8. ^ Matsuyoshi H, Kuniyasu H, Okumura M, Misawa H, Katsui R, Zhang GX, et al. (July 2010). "A 5-HT(4)-receptor activation-induced neural plasticity enhances in vivo reconstructs of enteric nerve circuit insult". Neurogastroenterology and Motility. 22 (7): 806–13, e226. doi:10.1111/j.1365-2982.2010.01474.x. PMID 20146727. S2CID 36819102.
  9. ^ Goto K, Kato G, Kawahara I, Luo Y, Obata K, Misawa H, et al. (2013). "In vivo imaging of enteric neurogenesis in the deep tissue of mouse small intestine". PLOS ONE. 8 (1): e54814. Bibcode:2013PLoSO...854814G. doi:10.1371/journal.pone.0054814. PMC 3561410. PMID 23382976.
  10. ^ Mosapride drug information – Drugs Update India
  11. ^ Kii Y, Ito T (May 1997). "Effects of 5-HT4-receptor agonists, cisapride, mosapride citrate, and zacopride, on cardiac action potentials in guinea pig isolated papillary muscles". Journal of Cardiovascular Pharmacology. 29 (5): 670–5. doi:10.1097/00005344-199705000-00016. PMID 9213211.
  12. ^ Kii Y, Ito T (May 2002). "Drug-induced ventricular tachyarrhythmia in isolated rabbit hearts with atrioventricular block". Pharmacology & Toxicology. 90 (5): 246–53. doi:10.1034/j.1600-0773.2002.900504.x. PMID 12076305.

January 01, 1970
mosapride, gastroprokinetic, agent, that, acts, selective, 5ht4, agonist, major, active, metabolite, mosapride, known, additionally, acts, 5ht3, antagonist, which, accelerates, gastric, emptying, throughout, whole, gastrointestinal, tract, humans, used, treatm. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist The major active metabolite of mosapride known as M1 additionally acts as a 5HT3 antagonist 1 which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans 2 and is used for the treatment of gastritis gastroesophageal reflux disease functional dyspepsia 3 and irritable bowel syndrome 4 It is recommended to be taken on an empty stomach i e at least one hour before food or two hours after food 5 MosaprideClinical dataAHFS Drugs comInternational Drug NamesATC codeA03FA09 WHO IdentifiersIUPAC name 4 Amino 5 chloro 2 ethoxy N 4 4 fluorophenyl methyl morpholin 2 yl methyl benzamideCAS Number112885 41 3 NPubChem CID119584IUPHAR BPS242DrugBankDB11675 YChemSpider106780 YUNIII8MFJ1C0BYKEGGD08236 YChEBICHEBI 94373ChEMBLChEMBL60889 YCompTox Dashboard EPA DTXSID2048408ECHA InfoCard100 127 999Chemical and physical dataFormulaC 21H 25Cl F N 3O 3Molar mass421 90 g mol 13D model JSmol Interactive imageSMILES Clc1cc c OCC cc1N C O NCC3OCCN Cc2ccc F cc2 C3InChI InChI 1S C21H25ClFN3O3 c1 2 28 20 10 19 24 18 22 9 17 20 21 27 25 11 16 13 26 7 8 29 16 12 14 3 5 15 23 6 4 14 h3 6 9 10 16H 2 7 8 11 13 24H2 1H3 H 25 27 YKey YPELFRMCRYSPKZ UHFFFAOYSA N Y N Y what is this verify In addition to its prokinetic properties mosapride also exerts anti inflammatory effects on the gastrointestinal tract which may contribute to some of its therapeutic effects 6 Mosapride also promotes neurogenesis in the gastrointestinal tract which may prove useful in certain bowel disorders 7 8 The neurogenesis is due to mosapride s effect on the 5 HT4 receptor where it acts as an agonist 9 Its common side effects include dry mouth abdominal pain dizziness headache insomnia malaise nausea diarrhea and sometimes constipation 3 10 Unlike some other prokinetic agents mosapride has little effect on potassium channels no effect on hERG transfected cells and no effect on cardiovascular function that could be detected in tests on humans 1 11 Due to the pharmacokinetics of mosapride it would take 1 000 3 000 times the therapeutic dose to elicit cardiovascular effects 12 References edit a b Tack J Camilleri M Chang L Chey WD Galligan JJ Lacy BE et al April 2012 Systematic review cardiovascular safety profile of 5 HT 4 agonists developed for gastrointestinal disorders Alimentary Pharmacology amp Therapeutics 35 7 745 67 doi 10 1111 j 1365 2036 2012 05011 x PMC 3491670 PMID 22356640 Odaka T Suzuki T Seza A Yamaguchi T Saisho H August 2006 Serotonin 5 HT4 receptor agonist mosapride citrate Nihon Rinsho Japanese Journal of Clinical Medicine in Japanese 64 8 1491 4 PMID 16898619 a b Curran MP Robinson DM 2008 Mosapride in gastrointestinal disorders Drugs 68 7 981 91 doi 10 2165 00003495 200868070 00007 PMID 18457463 S2CID 195686202 Mizuta Y Shikuwa S Isomoto H Mishima R Akazawa Y Masuda J et al November 2006 Recent insights into digestive motility in functional dyspepsia Journal of Gastroenterology 41 11 1025 40 doi 10 1007 s00535 006 1966 z PMID 17160514 S2CID 13353302 Kato S Morie T Yoshida N April 1995 Synthesis and biological activities of metabolites of mosapride a new gastroprokinetic agent Chemical amp Pharmaceutical Bulletin 43 4 699 702 doi 10 1248 cpb 43 699 PMID 7600620 Tsuchida Y Hatao F Fujisawa M Murata T Kaminishi M Seto Y et al May 2011 Neuronal stimulation with 5 hydroxytryptamine 4 receptor induces anti inflammatory actions via a7nACh receptors on muscularis macrophages associated with postoperative ileus Gut 60 5 638 47 doi 10 1136 gut 2010 227546 PMC 3071096 PMID 21115544 Kawahara I Kuniyasu H Matsuyoshi H Goto K Obata K Misawa H et al March 2012 Comparison of effects of a selective 5 HT reuptake inhibitor versus a 5 HT4 receptor agonist on in vivo neurogenesis at the rectal anastomosis in rats American Journal of Physiology Gastrointestinal and Liver Physiology 302 6 G588 97 doi 10 1152 ajpgi 00284 2011 hdl 10564 2701 PMID 22194416 Matsuyoshi H Kuniyasu H Okumura M Misawa H Katsui R Zhang GX et al July 2010 A 5 HT 4 receptor activation induced neural plasticity enhances in vivo reconstructs of enteric nerve circuit insult Neurogastroenterology and Motility 22 7 806 13 e226 doi 10 1111 j 1365 2982 2010 01474 x PMID 20146727 S2CID 36819102 Goto K Kato G Kawahara I Luo Y Obata K Misawa H et al 2013 In vivo imaging of enteric neurogenesis in the deep tissue of mouse small intestine PLOS ONE 8 1 e54814 Bibcode 2013PLoSO 854814G doi 10 1371 journal pone 0054814 PMC 3561410 PMID 23382976 Mosapride drug information Drugs Update India Kii Y Ito T May 1997 Effects of 5 HT4 receptor agonists cisapride mosapride citrate and zacopride on cardiac action potentials in guinea pig isolated papillary muscles Journal of Cardiovascular Pharmacology 29 5 670 5 doi 10 1097 00005344 199705000 00016 PMID 9213211 Kii Y Ito T May 2002 Drug induced ventricular tachyarrhythmia in isolated rabbit hearts with atrioventricular block Pharmacology amp Toxicology 90 5 246 53 doi 10 1034 j 1600 0773 2002 900504 x PMID 12076305 Retrieved from https en wikipedia org w index php title Mosapride amp oldid 1194704661, wikipedia, wiki, book, books, library,

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