Lerisetron ( —— )

产品货号. M21941 CAS No. 143257-98-1

Lerisetron 是 3 型血清素 (5-HT3) 受体拮抗剂，具有止吐活性。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥1007	有现货
10MG	￥1568	有现货
25MG	￥2623	有现货
50MG	￥3692	有现货
100MG	￥5292	有现货
500MG	获取报价	有现货
1G	获取报价	有现货
1 mL x 10 mM in DMSO	￥943	有现货

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生物学信息

产品名称

Lerisetron
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

Lerisetron 是 3 型血清素 (5-HT3) 受体拮抗剂，具有止吐活性。
产品描述

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.
体外实验

——
体内实验

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.
同义词

——
通路

Endocrinology/Hormones
靶点

5-HT Receptor
受体

5-HT3
研究领域

——
适应症

——

化学信息

CAS Number

143257-98-1
分子量

292.38
分子式

C18H20N4
纯度

>98% (HPLC)
溶解度

DMSO:53 mg/ml(181.27 mM)
SMILES

C(c1ccccc1)n1c(nc2ccccc12)N1CCNCC1
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1. Nerea, Jauregizar, Antonio, et al. Age-Related Changes in Pharmacokinetics and Pharmacodynamics of Lerisetron in the Rat: A Population Pharmacokinetic Model[J]. Gerontology, 2003 2. Strenge H , Goebel S , Kowalski J , et al. Effects of Lerisetron, a New 5-HT3 Receptor Antagonist, on Ipecacuanha- induced Emesis in Healthy Volunteers[J]. Arzneimittelforschung, 2002, 52(09):689-694.

计算器

浓度计算器

摩尔计算器

分子量计算器

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