Lerisetron

Names

[ Name ]:
Lerisetron

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.22g/cm3

[ Boiling Point ]:
502ºC at 760mmHg

[ Molecular Formula ]:
C₁₈H₂₀N₄

[ Molecular Weight ]:
292.37800

[ Flash Point ]:
257.4ºC

[ Exact Mass ]:
292.16900

[ PSA ]:
33.09000

[ LogP ]:
2.88800

[ Vapour Pressure ]:
3.31E-10mmHg at 25°C

[ Index of Refraction ]:
1.669

[ Storage condition ]:
-20°C