来立司琼 T8441

Product Introduction
Bioactivity


英文名: Lerisetron

描述: 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。

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 53 mg/ml(181.27 mM)


关键字: 5-HT Receptor | Serotonin Receptor | Serotonin | Bradycardia | Lerisetron | Inhibitor | 5-hydroxytryptamine Receptor | Pharmacokinetics | inhibit | SD rats

相关产品: AMI-193 | Buspirone hydrochloride | Metergoline | Buclizine dihydrochloride | 7-Desmethyl-3-hydroxyagomelatine | Iloperidone | NPS ALX Compound 4a | Methiothepin mesylate | 5-HT2 agonist-1 free base | Cinitapride Hydrogen Tartrate

相关库: Anti-Neurodegenerative Disease Compound Library | Anti-Parkinson's Disease Compound Library | ReFRAME Related Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Human Metabolite Library | GPCR Compound Library | Inhibitor Library | Serotonin Receptor-Targeted Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途