Home Neuronal Signaling 5-HT Receptor antagonist Ramosetron Hydrochloride For research use only.

Ramosetron Hydrochloride

Synonyms: YM-060

Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.

Ramosetron Hydrochloride Chemical Structure

Ramosetron Hydrochloride Chemical Structure

CAS No. 132907-72-3

Purity & Quality Control

Batch: S372301 DMSO]63 mg/mL]false]Water]63 mg/mL]false]Ethanol]1 mg/mL]false Purity: 99.95%
99.95

Ramosetron Hydrochloride Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Ramosetron Hydrochloride (YM-060) 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
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
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].
Animal Research Animal Models Sprague-Dawley rats
Dosages 0.01, 0.03, 0.1 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01870895 Completed
Diarrhea-predominant Irritable Bowel Syndrome
Astellas Pharma Inc
 February 2013 Phase 3
NCT01394653 Completed
Healthy|Plasma Concentration of YM060
Astellas Pharma Inc
 July 2011 Phase 1
NCT01392794 Completed
Healthy|Plasma Concentration of YM060
Astellas Pharma Inc
 April 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 315.8 Formula

C17H17N3O.HCl
CAS No. 132907-72-3 SDF Download Ramosetron Hydrochloride SDF
Smiles CN1C=C(C2=CC=CC=C21)C(=O)C3CCC4=C(C3)NC=N4.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.49 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 63 mg/mL

Ethanol : 1 mg/mL


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

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