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Lerisetron
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lerisetron图片
CAS NO:143257-98-1
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
Lerisetron 是5-HT3拮抗剂,与 5-HT3受体具有高亲和力(pKi:9.2)。它对尿烷麻醉大鼠的 5-HT 引发的反射性心率过缓具有抑制作用。

产品描述

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

体内活性

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.

动物实验

Fischer 344 rats (n = 44) were divided into three groups, depending on their age: 5, 13, and 25 months. Blood samples were collected before administration of 200 micro g/kg of lerisetron for measurements of albumin, alpha(1)-acid glycoprotein, and unbound fraction of lerisetron. The lerisetron plasma concentrations were measured by high-performance liquid chromatography. A two-compartment model was fitted to the data using the nonlinear mixed-effects computer program WinNonMix. The population analysis was performed with the complete set of the collected data, and the potential sources of variability in the population parameters were investigated. Additionally, a pharmacodynamic study was performed. The effect of lerisetron (inhibition of the von Bezold-Jarisch reflex) was evaluated in young, adult, and senescent Fischer 344 rats.

Cas No.

143257-98-1

分子式

C18H20N4

分子量

292.386

别名

Lerisetron

储存和溶解度

DMSO:53 mg/ml(181.27 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years