WordNet

a salt or ester of citric acid
cause to form a salt or ester of citric acid

PrepTutorEJDIC

クエン酸塩

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/22 02:27:52」(JST)

wiki en

[Wiki en表示]

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, gastro-oesophageal 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, diarrhoea 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.; 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. 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. PMID 18457463.
^ Mizuta Y, Shikuwa S, Isomoto H, Mishima R, Akazawa Y, Masuda J, Omagari K, Takeshima F, Kohno S. Recent insights into digestive motility in functional dyspepsia. Journal of Gastroenterology. 2006 Nov;41(11):1025-40.
^ Kato S, Morie T, Yoshida N. Synthesis and biological activities of metabolites of mosapride, a new gastroprokinetic agent.Chemical and Pharmaceutical Bulletin (Tokyo). 1995 Apr;43(4):699-702.
^ 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. et al. (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. PMID 23382976. |displayauthors= suggested (help)
^ 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. 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. PMID 12076305.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 大量輸血 massive blood transfusion
2. 慢性腎疾患における高リン血症の治療 treatment of hyperphosphatemia in chronic kidney disease
3. 持続的腎代替療法中の抗凝固療法 anticoagulation for continuous renal replacement therapy
4. Therapeutic plasma exchange: Complications
5. クエン酸クロミフェンによる排卵誘発 ovulation induction with clomiphene citrate

English Journal

Effect of DA-9701, a novel prokinetic agent, on stress-induced delayed gastric emptying and hormonal changes in rats.

Jung YS, Kim MY, Lee HS, Park SL, Lee KJ.SourceCollege of Pharmacy, Ajou University, Suwon, Korea Department of Gastroenterology, Ajou University School of Medicine, Suwon, Korea.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society.Neurogastroenterol Motil.2013 Mar;25(3):254-e166. doi: 10.1111/nmo.12053. Epub 2012 Dec 6.
Background DA-9701 is a novel prokinetic agent formulated with Pharbitis Semen and Corydalis Tuber. This study aimed to evaluate the effect of DA-9701 on stress-induced delay in gastric emptying and changes in plasma adrenocorticotropic hormone and ghrelin levels in rats. Methods Changes in ga
PMID 23216854

Metabolic and toxicological considerations for the latest drugs used to treat irritable bowel syndrome.

Mozaffari S, Nikfar S, Abdollahi M.SourceDepartment of Toxicology and Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences , Tehran 1417614411 , Iran Mohammad.Abdollahi@UToronto.Ca ; Mohammad@TUMS.Ac.Ir.
Expert opinion on drug metabolism & toxicology.Expert Opin Drug Metab Toxicol.2013 Jan 19. [Epub ahead of print]
Introduction: The high prevalence of irritable bowel syndrome (IBS), a chronic gastrointestinal (GI) disorder, its lack of satisfactory effective drugs and its complicated pathophysiology lead to the demand of new therapeutic agents. During a new drug development process, the pharmacokinetic profil
PMID 23330973

Japanese Journal

Anti-emetic Effect of Mosapride Citrate Hydrate, a 5-HT? Receptor Agonist, on Selective Serotonin Reuptake Inhibitors (SSRIs)-Induced Emesis in Experimental Animals

Mine Yukiko,Oku Seiko,Yoshida Naoyuki
Journal of pharmacological sciences 121(1), 58-66, 2013-01
NAID 40019554461

Anti-emetic Effect of Mosapride Citrate Hydrate, a 5-HT4 Receptor Agonist, on Selective Serotonin Reuptake Inhibitors (SSRIs)-Induced Emesis in Experimental Animals

Mine Yukiko,Oku Seiko,Yoshida Naoyuki
Journal of Pharmacological Sciences, 2012
… In the present study, we investigated the anti-emetic effect of mosapride, a 5-HT4 … We also examined the effect of mosapride on SSRIs-induced delay in gastric emptying and increase in gastric vagal afferent activity in rats. … Mosapride inhibited paroxetine-induced emesis in Suncus murinus … The anti-emetic effect of mosapride was partially inhibited by SB207266, a selective 5-HT4 …
NAID 130002507900

Related Pictures

★リンクテーブル★

リンク元	「モサプリド」「クエン酸モサプリド」
関連記事	「mosapride」

「モサプリド」

Mosapride
Systematic (IUPAC) name
	(RS)-4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobenzyl)morpholin-2-yl]methyl}benzamide
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	?
Identifiers
CAS number	112885-41-3
ATC code	None
PubChem	CID 119584
IUPHAR ligand	242
ChemSpider	106780
UNII	I8MFJ1C0BY
KEGG	D08236
ChEMBL	CHEMBL60889
Chemical data
Formula	C21H25ClFN3O3
Mol. mass	421.893 g/mol
	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 ;
(what is this?) (verify)