您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > MTEP hydrochloride
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:
 
MTEP hydrochloride
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。
MTEP hydrochloride图片
CAS NO:1186195-60-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
MTEP hydrochloride 是一种有效的、选择性的、非竞争性的 mGlu5 拮抗剂,IC50 为 5 nM,Ki 为 16 nM。
Cas No.1186195-60-7
别名3-[2-(2-甲基-4-噻唑基)乙炔基]吡啶盐酸盐
化学名2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole;hydrochloride
Canonical SMILESCC1=NC(=CS1)C#CC2=CN=CC=C2.Cl
分子式C11H9ClN2S
分子量236.72
溶解度DMF: 3 mg/ml,DMSO: 15 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 10 mg/ml
储存条件Store at -20℃
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

IC50: 5 nM

MTEP is a selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonist.

The mGluRs are classified into three groups: group I (mGluR1 and 5), group II (mGluR2 and 3) and group III (mGluR4, 6, 7 and 8). mGluR5 belonging to group I is excitatory, mainly localized at the edge of axo-spinous and axodendritic synaptic junctions.

In vitro: Like MPEP, MTEP showed a nanomolar affinity for mGluR5, but seemed to be superior to MPEP in term of specificity. MTEP did not influence mGluR2, mGluR7, NMDA, AMPA or kainate receptors, while inhibited MAOA at a concentration three times higher than MPEP. Moreover, recent study indicated that MTEP was five times stronger that MPEP as an anxiolytic compound [1].

In vivo: MTEP with doses between 0.5 and 3 mg/kg was found to decrease the haloperidol-induced muscle rigidity, which was measured as an increased muscle resistance of the rat hind leg. The longest and strongest effect was observed with the dose of 1 mg/kg. MTEP was also found to reduce the haloperidol-induced increase in electromyographic activity recorded in the tibialis anterior and gastrocnemius muscles. 3 and 5 mg/kg of MTEP could inhibit the haloperidol- induced catalepsy [1].

Clinical trial: N/A

Reference:
[1] Ossowska K,Konieczny J,Wolfarth S,Pilc A.  MTEP, a new selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), produces antiparkinsonian-like effects in rats. Neuropharmacology.2005 Sep;49(4):447-55.