| Bioactivity | 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]. |
| Target | pKi: 9.2 (5-HT3) |
| 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]. |
| Name | Lerisetron |
| CAS | 143257-98-1 |
| Formula | C18H20N4 |
| Molar Mass | 292.38 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |