Lerisetron

Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats[1].

Product Specifications

CAS Number

[143257-98-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cardiovascular Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/lerisetron.html

Purity

99.69

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

C1(N=C(N2CCNCC2)N3CC4=CC=CC=C4)=C3C=CC=C1

Molecular Formula

C18H20N4

Molecular Weight

292.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Orjales A, Mosquera R, Labeaga L, Rodes R. New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. J Med Chem. 1997;40 (4) :586-593.|[2]Jauregizar N, Calvo R, Suarez E, Quintana A, Raczka E, Lukas JC. Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. J Pharm Sci. 2002;91 (1) :41-52.