143257-98-1

143257-98-1 structure

Name: Lerisetron
Chemical Name: 1-benzyl-2-piperazin-1-ylbenzimidazole
CAS Number: 143257-98-1
Molecular Formula: C₁₈H₂₀N₄
Molecular Weight: 292.37800
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-08-31 18:09:32
Modify Date: 2024-01-11 10:04:33
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].

Name	1-benzyl-2-piperazin-1-ylbenzimidazole
Synonyms	Lerisetron lerisetron[inn] UNII-Q36R82SXRG 1-Benzyl-2-piperazin-1-yl-1H-benzoimidazole 1-benzyl-2-(piperazin-1-yl)-1H-benzimidazole 1-phenylmethyl-2-(1-piperazinyl)-1H-benzimidazole

Description	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].
Related Catalog	Research Areas >> Cardiovascular Disease Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	pKi: 9.2 (5-HT3)[1]
In Vivo	Lerisetron (50-200 μg/kg; IV; single) exhibits CL of 0.004-0.005 L/min, Vds of 0.88-0.96 L, MRT0-LAST of 224-337.1 min and AUC∞ of 57.7-66.1 μg·min/L in rats[2]. Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia[2]. Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats[2]. IV (50 μg/kg) IV (100 μg/kg) IV (200 μg/kg) CL (L/min) 0.005 0.004 0.004 Vds (L) 0.9 0.88 0.96 MRT0-LAST (min) 224 337.1 226.3 AUC∞ (μg·min/L) 66.1 57.7 58.1
References	[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.