您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Fenobam
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Fenobam
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。
Fenobam图片
CAS NO:57653-26-6
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Fenobam 是一种选择性、口服活性和脑渗透性 mGluR5 拮抗剂,作用于变构调节位点(大鼠和人重组 mGlu5 受体的 Kd 分别为 54 和 31 nM)。
Cas No.57653-26-6
别名非诺班
化学名1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)urea
Canonical SMILESClC1=CC(NC(NC(N(C)C2)=NC2=O)=O)=CC=C1
分子式C11H11N4O2Cl
分子量266.69
溶解度<26.67mg/ml in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity[1][2].

References:
[1]. Porter RH, et al. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther. 2005 Nov;315(2):711-21.
[2]. Laura F, et al. The Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Fenobam: Pharmacokinetics, Side Effects, and Analgesic Effects in Healthy Human Subjects.bioRxiv 391383;