関: mosapride citrate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2019/09/29 12:25:48」(JST)

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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]

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

^ ^a ^b Tack, J.; Camilleri, M.; Chang, L.; Chey, WD.; Galligan, JJ.; Lacy, BE.; Müller-Lissner, S.; Quigley, EM.; Schuurkes, J. (Apr 2012). "Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders". Aliment Pharmacol Ther. 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)]". Nippon Rinsho (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.
^ Mizuta, Y; Shikuwa, S; Isomoto, H; Mishima, R; Akazawa, Y; Masuda, J; Omagari, K; Takeshima, F; Kohno, S (Nov 2006). "Recent insights into digestive motility in functional dyspepsia". Journal of Gastroenterology. 41 (11): 1025–40. doi:10.1007/s00535-006-1966-z.
^ Kato, S; Morie, T; Yoshida, N (Apr 1995). "Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent". Chemical and Pharmaceutical Bulletin (Tokyo). 43 (4): 699–702. doi:10.1248/cpb.43.699.
^ Tsuchida Y, Hatao F, Fujisawa M, 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.
^ Kawahara I, Kuniyasu H, Matsuyoshi 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". Am. J. Physiol. Gastrointest. Liver Physiol. 302 (6): G588–97. doi:10.1152/ajpgi.00284.2011. PMID 22194416.
^ Matsuyoshi H, Kuniyasu H, Okumura M, et al. (July 2010). "A 5-HT(4)-receptor activation-induced neural plasticity enhances in vivo reconstructs of enteric nerve circuit insult". Neurogastroenterol. Motil. 22 (7): 806–13, e226. doi:10.1111/j.1365-2982.2010.01474.x. PMID 20146727.
^ Goto, K.; Kato, G.; Kawahara, I.; Luo, Y.; Obata, K.; Misawa, H.; Ishikawa, T.; Kuniyasu, H.; Nabekura, J.; Takaki, M (2013). "In vivo imaging of enteric neurogenesis in the deep tissue of mouse small intestine". PLOS ONE. 8 (1): e54814. 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". J Cardiovasc Pharmacol. 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". Pharmacol Toxicol. 90 (5): 246–53. doi:10.1034/j.1600-0773.2002.900504.x. PMID 12076305.

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1. 長期にわたる術後イレウスに対する予防策measures to prevent prolonged postoperative ileus [show details]
… Mosapride and prucalopride are 5-hydroxytryptamine 4 (5HT₄) receptor agonists that have been proposed to enhance bowel motility through prokinetic and anti-inflammatory actions. Mosapride has…
2. 成人における機能性胃腸症functional dyspepsia in adults [show details]
…meta-analysis that included 29 trials of six individual agents (cisapride, acotiamide, itopride, tegaserod, mosapride, and ABT-229) in patients with functional dyspepsia, overall, global symptom improvement was greater…

English Journal

Effect of mosapride on ruminal motility in cattle.

Arai S, Haritani M, Sawada H, Kimura K.
The Journal of veterinary medical science. 2019 Jul;81(7)1017-1020.
This study aimed to assess the effects of mosapride at various dosages on ruminal motility in cattle and the absorption kinetics of mosapride in cattle. Mosapride was rapidly absorbed after oral administration in cattle. Oral administration at dosages of 1, 3, and 10 mg/kg resulted in a dose-depende
PMID 31155551

Evaluation of the antianxiety and antidepressant activities of mosapride in Wistar albino rats.

Krishna V, Bairy KL, Patil N, Sunny SV.
Journal of basic and clinical physiology and pharmacology. 2019 Jul;30(4).
Background The 5HT4 receptor agonists are antidepressants with a unique mode of action. Many studies have been done on investigational drugs, and mosapride has been shown to have a 5HT3 antagonistic property. In this study, we assessed the potential anxiolytic and antidepressant effects of mosapride
PMID 31318691

High-content analysis of constitutive androstane receptor (CAR) translocation identifies mosapride citrate as a CAR agonist that represses gluconeogenesis.

Mackowiak B, Li L, Lynch C, Ziman A, Heyward S, Xia M, Wang H.
Biochemical pharmacology. 2019 Jul;168()224-236.
The constitutive androstane receptor (CAR) plays an important role in hepatic drug metabolism and detoxification but has recently been projected as a potential drug target for metabolic disorders due to its repression of lipogenesis and gluconeogenesis. Thus, identification of physiologically-releva
PMID 31306645

Japanese Journal

Drug-induced Liver Injury Associated with Mosapride Citrate: A Report of Two Cases

Internal Medicine 56(1), 41-45, 2017
NAID 130005239488

Activation of 5-HT<sub>4</sub> receptors facilitates neurogenesis of injured enteric neurons at an anastomosis in the lower gut

Journal of Smooth Muscle Research 51(0), 82-94, 2015
NAID 130005130210

The Effect of Mosapride Citrate on Patients with Non-Erosive Reflux Disease (NERD)

耳鼻咽喉科臨床　補冊 144(0), 72-73, 2015
NAID 130005110189

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★リンクテーブル★

リンク元	「モサプリド」
拡張検索	「mosapride citrate」

「モサプリド」

Mosapride
Clinical data
AHFS/Drugs.com	International Drug Names
ATC code	none;
Identifiers
	IUPAC name 4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide;
CAS Number	112885-41-3 ;
PubChem CID	119584;
IUPHAR/BPS	242;
ChemSpider	106780 ;
UNII	I8MFJ1C0BY;
KEGG	D08236 ;
ChEMBL	ChEMBL60889 ;
CompTox Dashboard (EPA)	DTXSID2048408 ;
ECHA InfoCard	100.127.999
Chemical and physical data
Formula	C21H25ClFN3O3
Molar mass	421.893 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc1cc(c(OCC)cc1N)C(=O)NCC3OCCN(Cc2ccc(F)cc2)C3;
	InChI 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) ; Key:YPELFRMCRYSPKZ-UHFFFAOYSA-N ;
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