Name | 1-benzyl-2-piperazin-1-ylbenzimidazole |
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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]. |
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Related Catalog | |
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 |
Density | 1.22g/cm3 |
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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 |