Home Neuronal Signaling 5-HT Receptor antagonist Ramosetron Hydrochloride

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Ramosetron Hydrochloride 5-HT Receptor antagonist

Cat.No.S3723

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

Chemical Structure

Molecular Weight: 315.8

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (199.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 63 mg/mL

Ethanol : 1 mg/mL

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In vivo
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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.
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Chemical Information, Storage & Stability

Molecular Weight 315.8 Formula

C17H17N3O.HCl

 Storage (From the date of receipt)
CAS No. 132907-72-3 Download SDF Storage of Stock Solutions

Synonyms YM-060 Smiles CN1C=C(C2=CC=CC=C21)C(=O)C3CCC4=C(C3)NC=N4.Cl

Mechanism of Action

Targets/IC50/Ki
5-HT3 receptor
(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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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