Lerisetron

Research use only, not for human use.

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.showed a decrease in total clearance and distribution volume of the central compartment in old rats. The lerisetron free (unbound) fraction remained unchanged among the groups, and there were no significant differences in alpha(1)-acid glycoprotein levels. The concentration-effect relationship was best described by a sigmoid E(max) model. Since the drug concentration in plasma at half-maximal effect (EC(50)) decreased in old rats, an increased sensitivity to the effect of lerisetron in old animals could be expected.

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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.Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia.Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats.

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Endocrinology/Hormones

5-HT Receptor

5-HT3

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143257-98-1

292.38

C18H20N4

>98% (HPLC)

DMSO:53 mg/ml(181.27 mM)

C(c1ccccc1)n1c(nc2ccccc12)N1CCNCC1

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(-20℃)

With Ice Pack

≥ 2 years