Mosapride Citrate | CAS#112885-42-4 | SR-4 Agonist

MedKoo Cat#: 527090 | Name: Mosapride Citrate

Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Mosapride Citrate is a selective 5-HT4 agonist, SR-4 agonist, and SR-3 antagonist. Mosapride Citrate has been shown to increase gastric emptying in rats and stimulates gastric motor activity in conscious dogs.

Chemical Structure

Mosapride Citrate

CAS#112885-42-4

Theoretical Analysis

MedKoo Cat#: 527090

Name: Mosapride Citrate

CAS#: 112885-42-4

Chemical Formula: C27H33ClFN3O10

Exact Mass: 613.1839

Molecular Weight: 614.02

Elemental Analysis: C, 52.82; H, 5.42; Cl, 5.77; F, 3.09; N, 6.84; O, 26.06

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 285.00
50mg	USD 855.00

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

Mosapride Citrate

IUPAC/Chemical Name

4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide citrate

InChi Key

HUZTYZBFZKRPFG-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H25ClFN3O3.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)

SMILES Code

O=C(NCC1CN(CC2=CC=C(F)C=C2)CCO1)C3=CC(Cl)=C(N)C=C3OCC.OC(C(O)=O)(CC(O)=O)CC(O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Mosapride Citrate is a selective 5-HT4 agonist, SR-4 agonist, and SR-3 antagonist.

In vitro activity:

This study tested the effect of mosapride on 5-hydroxytryptamine type 3 (5-HT3) receptor currents because the 5-HT3 receptors are also known to be expressed in the GI system and have an important role in the regulation of GI functions. The 5-HT3 receptor current amplitudes were inhibited by mosapride in a concentration-dependent manner. Mosapride blocked the peak currents evoked by the application of 5-HT in a competitive manner because the EC50 shifted to the right without changing the maximal effect. Reference: Korean J Physiol Pharmacol. 2019 Sep;23(5):419-426. https://pubmed.ncbi.nlm.nih.gov/31496879/

In vivo activity:

Forty-five healthy male Sprague-Dawley rats that were pathogen-free (weight 200-220 g) were randomly divided into a control group (n = 15), model group (n = 15) and mosapride group (n = 15). There was a significant decline in the rate of gut microbiota translocation in the mosapride group compared with the model group. There were intestinal microbiota changes in the mosapride group compared with that of the model group, including Bacteroidetes, Prevotellaceae, Alloprevotella, Ruminiclostridium, Negativicutes, Selenomonadales, Veillonellaceae, Anaerovibrio, Campylobacterales, Epsilonbacteraeota, Helicobacter, Oscillibacter, Verrucomicrobiales, Akkermansia, Intestinimonas, Eubacterium, Clostridiaceae, Clostridium, Bacteroides, Tyzzerella, Actinobacteria, and Bifidobacteriales. Among these bacteria, Alloprevotella showed a strong correlation with the other bacteria. Reference: Adv Clin Exp Med. 2022 Jun;31(6):623-633. https://pubmed.ncbi.nlm.nih.gov/35275452/

	Solvent	mg/mL	mM
Solubility
	DMF:PBS (pH 7.2) (1:4)	0.2	0.33
	DMSO	68.3	111.29

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 614.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Park YS, Sung KW. Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells. Korean J Physiol Pharmacol. 2019 Sep;23(5):419-426. doi: 10.4196/kjpp.2019.23.5.419. Epub 2019 Aug 26. PMID: 31496879; PMCID: PMC6717790. 2. Mine Y, Yoshikawa T, Oku S, Nagai R, Yoshida N, Hosoki K. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J Pharmacol Exp Ther. 1997 Dec;283(3):1000-8. PMID: 9399969. 3. Chen D, Xiong J, Feng H, Liu Y, Xu J, Xu H. The influence of mosapride on gut microbiota of carbon tetrachloride-induced cirrhosis rats based on 16S rRNA gene sequencing. Adv Clin Exp Med. 2022 Jun;31(6):623-633. doi: 10.17219/acem/146320. PMID: 35275452. 4. Krishna V, Bairy KL, Patil N, Sunny SV. Evaluation of the antianxiety and antidepressant activities of mosapride in Wistar albino rats. J Basic Clin Physiol Pharmacol. 2019 Jul 18;30(4). doi: 10.1515/jbcpp-2018-0089. PMID: 31318691.

In vitro protocol:

In vivo protocol:

1. Chen D, Xiong J, Feng H, Liu Y, Xu J, Xu H. The influence of mosapride on gut microbiota of carbon tetrachloride-induced cirrhosis rats based on 16S rRNA gene sequencing. Adv Clin Exp Med. 2022 Jun;31(6):623-633. doi: 10.17219/acem/146320. PMID: 35275452. 2. Krishna V, Bairy KL, Patil N, Sunny SV. Evaluation of the antianxiety and antidepressant activities of mosapride in Wistar albino rats. J Basic Clin Physiol Pharmacol. 2019 Jul 18;30(4). doi: 10.1515/jbcpp-2018-0089. PMID: 31318691.

1: Yang XY, Guo CY, Zhang X, Zhong YQ, Tian C. [Effect analysis on Deanxit combined with Shuganjieyu capsule in the treatment of refractory gastroesophageal reflux disease]. Zhonghua Yi Xue Za Zhi. 2017 Nov 28;97(44):3475-3479. doi: 10.3760/cma.j.issn.0376-2491.2017.44.008. Chinese. PubMed PMID: 29275582. 2: Li DY, Dai YK, Zhang YZ, Huang MX, Li RL, Ou-Yang J, Chen WJ, Hu L. Systematic review and meta-analysis of traditional Chinese medicine in the treatment of constipation-predominant irritable bowel syndrome. PLoS One. 2017 Dec 18;12(12):e0189491. doi: 10.1371/journal.pone.0189491. eCollection 2017. PubMed PMID: 29253850; PubMed Central PMCID: PMC5734785. 3: Wang B, Chen Y, Chen S. [Clinical observation of slow transit constipation treated with acupuncture and modified weitong xiaopi formula]. Zhongguo Zhen Jiu. 2017 Feb 12;37(2):130-134. doi: 10.13703/j.0255-2930.2017.02.006. Chinese. PubMed PMID: 29231473. 4: Jeong EJ, Chung SY, Hong HN, Oh SW, Sim JY. The novel, potent and highly selective 5-HT(4) receptor agonist YH12852 significantly improves both upper and lower gastrointestinal motility. Br J Pharmacol. 2017 Nov 15. doi: 10.1111/bph.14096. [Epub ahead of print] PubMed PMID: 29139561. 5: Xu H, Xiong J, Xu J, Li S, Zhou Y, Chen D, Cai X, Ping J, Deng M, Chen J. Mosapride Stabilizes Intestinal Microbiota to Reduce Bacterial Translocation and Endotoxemia in CCl(4)-Induced Cirrhotic Rats. Dig Dis Sci. 2017 Oct;62(10):2801-2811. doi: 10.1007/s10620-017-4704-x. Epub 2017 Aug 16. PubMed PMID: 28815345. 6: Zhou J, Tang X, Wang J, Chen Z, Wang X, Jiang B. Feasibility of a novel low-volume and sodium phosphate-free bowel preparation regimen for colon capsule endoscopy. Exp Ther Med. 2017 Aug;14(2):1739-1743. doi: 10.3892/etm.2017.4664. Epub 2017 Jun 23. PubMed PMID: 28810644; PubMed Central PMCID: PMC5525907. 7: Wang B, Sun X, Wang S, Guo P, Li S, Zhang M, Zhao L, Chen X. Comparative pharmacokinetics of (S)-MP3950, a novel 5-HT4 receptor agonist, in normal and atropine-induced gastrointestinal motility disorders rats. Xenobiotica. 2017 Aug 30:1-7. doi: 10.1080/00498254.2017.1365974. [Epub ahead of print] PubMed PMID: 28786731. 8: Iida H, Kaai M, Inoh Y, Kanoshima K, Ohkuma K, Nonaka T, Fujita K, Ida T, Kusakabe A, Maeda S, Nakajima A, Inamori M. Early effect on intragastric pH of oral administration of rabeprazole with mosapride compared with rabeprazole alone. Ann Gastroenterol. 2017;30(4):424-428. doi: 10.20524/aog.2017.0161. Epub 2017 May 19. PubMed PMID: 28655978; PubMed Central PMCID: PMC5479994. 9: Lei L, Yang H, Zhang X, Ren J. Comparison of the effects of esomeprazole plus mosapride citrate and botulinum toxin A on vocal process granuloma. Am J Otolaryngol. 2017 Sep - Oct;38(5):593-597. doi: 10.1016/j.amjoto.2017.01.039. Epub 2017 Jun 21. PubMed PMID: 28655420. 10: Uchida M, Kobayashi O, Shimizu K. Gastric emptying after artificial ulceration in rats: differences due to the site of the ulcer and the effects of prokinetic drugs. J Smooth Muscle Res. 2017;53(0):48-56. doi: 10.1540/jsmr.53.48. PubMed PMID: 28652516; PubMed Central PMCID: PMC5487827. 11: Yang YJ, Bang CS, Baik GH, Park TY, Shin SP, Suk KT, Kim DJ. Prokinetics for the treatment of functional dyspepsia: Bayesian network meta-analysis. BMC Gastroenterol. 2017 Jun 26;17(1):83. doi: 10.1186/s12876-017-0639-0. PubMed PMID: 28651565; PubMed Central PMCID: PMC5485548. 12: Morsi NM, Abdelbary GA, Elshafeey AH, Ahmed MA. Engineering of a novel optimized platform for sublingual delivery with novel characterization tools: in vitro evaluation and in vivo pharmacokinetics study in human. Drug Deliv. 2017 Nov;24(1):918-931. doi: 10.1080/10717544.2017.1334719. PubMed PMID: 28597700. 13: Zhang AM, Sun ZQ, Zhang LM. Mosapride combined with probiotics on gastrointestinal function and growth in premature infants. Exp Ther Med. 2017 Jun;13(6):2675-2680. doi: 10.3892/etm.2017.4340. Epub 2017 Apr 13. PubMed PMID: 28587329; PubMed Central PMCID: PMC5450587. 14: El Nashar RM, Abdel Ghani NT, El Gohary NA, Barhoum A, Madbouly A. Molecularly imprinted polymers based biomimetic sensors for mosapride citrate detection in biological fluids. Mater Sci Eng C Mater Biol Appl. 2017 Jul 1;76:123-129. doi: 10.1016/j.msec.2017.03.087. Epub 2017 Mar 14. PubMed PMID: 28482490. 15: Pan W, Wang Z, Tian F, Yan M, Lu Y. Electroacupuncture combined with mosapride alleviates symptoms in diabetic patients with gastroparesis. Exp Ther Med. 2017 Apr;13(4):1637-1643. doi: 10.3892/etm.2017.4139. Epub 2017 Feb 21. PubMed PMID: 28413522; PubMed Central PMCID: PMC5377548. 16: Wu X, Zheng C, Xu X, Ding P, Xiong F, Tian M, Wang Y, Dong H, Zhang M, Wang W, Xu S, Xie M, Huang G. Electroacupuncture for Functional Constipation: A Multicenter, Randomized, Control Trial. Evid Based Complement Alternat Med. 2017;2017:1428943. doi: 10.1155/2017/1428943. Epub 2017 Jan 31. PubMed PMID: 28250788; PubMed Central PMCID: PMC5307003. 17: Lee JY, Kim SK, Cho KB, Park KS, Kwon JG, Jung JT, Kim EY, Jang BI, Lee SH; Daegu-Gyeongbuk Gastrointestinal Study Group (DGSG). A Double-blind, Randomized, Multicenter Clinical Trial Investigating the Efficacy and Safety of Esomeprazole Single Therapy Versus Mosapride and Esomeprazole Combined Therapy in Patients with Esophageal Reflux Disease. J Neurogastroenterol Motil. 2017 Apr 30;23(2):218-228. doi: 10.5056/jnm16100. PubMed PMID: 28192647; PubMed Central PMCID: PMC5383116. 18: Sako A, Bae SK, Gushima T, Motoshita J, Bekki S, Abiru S, Komori A, Shimoda S, Ito M, Yatsuhashi H, Takahashi K. Drug-induced Liver Injury Associated with Mosapride Citrate: A Report of Two Cases. Intern Med. 2017;56(1):41-45. doi: 10.2169/internalmedicine.56.7374. Epub 2017 Jan 1. PubMed PMID: 28049998; PubMed Central PMCID: PMC5313423. 19: Yu H, Zheng BJ, Pan WK, Wang HJ, Xie C, Zhao YY, Chen XL, Liu Y, Gao Y. Combination of exogenous cell transplantation and 5-HT(4) receptor agonism induce endogenous enteric neural crest-derived cells in a rat hypoganglionosis model. Exp Cell Res. 2017 Feb 1;351(1):36-42. doi: 10.1016/j.yexcr.2016.12.022. Epub 2016 Dec 26. PubMed PMID: 28034674. 20: Hashizume N, Yagi M, Ushijima K, Seki Y, Fukahori S, Muto M, Matsufuji H, Taguchi T. Pharmacotherapy for pediatric chronic intestinal pseudo-obstruction: Nationwide survey in Japan. Pediatr Int. 2017 Apr;59(4):467-472. doi: 10.1111/ped.13201. Epub 2017 Feb 2. PubMed PMID: 27862707.