| 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 |
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| Target |
pKi: 9.2 (5-HT3)[1]
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| 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
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| 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.
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