Ramosetron Hydrochloride

Catalog No.S3723 Synonyms: YM-060

Ramosetron Hydrochloride Chemical Structure

Molecular Weight(MW): 315.8

Ramosetron Hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.

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Biological Activity

Description Ramosetron Hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.
Targets
5-HT3 receptor [2]
(in N1E-15 cells)
0.091 nM(Ki)
In vitro

Ramosetron Hydrochloride (YM-060) has very low afinity for nicotinic and GABA receptors. In vitro studies have also demonstrated that YM060 shows low afinity for 5-HT1-like, 5-HT2, alpha-1, atpha-2, beta-1, beta-2, histamine H1 and H2 receptors. YM-060 is expected not to have 5-HT4 receptor blocking activity[2].

In vivo Ramosetron is known to potently inhibit stress-induced abnormal defecation in animals. Ramosetron has potent, rapid-onset, and long-lasting inhibitory effects on CFS-induced defecation in rats, without any influence on normal defecation. The inhibitory effect of ramosetron appeared immediately after dosing and lasted for many hours[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Sprague-Dawley rats
  • Formulation: dissolved in distilled water(DW) and diluted with 0.5% (w/v) MC solution
  • Dosages: 0.01, 0.03, 0.1 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (199.49 mM)
Water 63 mg/mL (199.49 mM)
Ethanol 1 mg/mL (3.16 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 315.8
Formula

C17H17N3O.HCl

CAS No. 132907-72-3
Storage powder
in solvent
Synonyms YM-060

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01870895 Completed Diarrhea-predominant Irritable Bowel Syndrome Astellas Pharma Inc February 2013 Phase 3
NCT01870895 Completed Diarrhea-predominant Irritable Bowel Syndrome Astellas Pharma Inc February 2013 Phase 3
NCT01736423 Completed Diarrhea-predominant Irritable Bowel Syndrome Astellas Pharma Inc September 2012 Phase 3
NCT01736423 Completed Diarrhea-predominant Irritable Bowel Syndrome Astellas Pharma Inc September 2012 Phase 3
NCT01394653 Completed Healthy|Plasma Concentration of YM060 Astellas Pharma Inc July 2011 Phase 1
NCT01394653 Completed Healthy|Plasma Concentration of YM060 Astellas Pharma Inc July 2011 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID