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MPEP
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。
MPEP图片
CAS NO:96206-92-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
MPEP 是一种有效的、选择性的、非竞争性的、具有口服活性和全身活性的 mGlu5 受体拮抗剂,其 IC50 为 36 nM,可完全抑制 quisqualate 刺激的磷酸肌醇 (PI) 水解。
Cas No.96206-92-7
化学名2-methyl-6-(2-phenylethynyl)pyridine
Canonical SMILESCC1=CC=CC(=N1)C#CC2=CC=CC=C2
分子式C14H11N
分子量193.24
溶解度≥ 9.95mg/mL in DMSO
储存条件Store at -20°C
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

MPEP is a selective and systemically active antagonist of metabotropic glutamate receptor subtype 5 (mGlu5 receptor) with IC50 value of 36nM [1].

MPEP is an antagonist of mGlu5 receptor. It is used as a valuable pharmacological tool to explore the function of its target receptor due to its high selectivity. In L (tk-) cells expressing human mGlu1b receptors, MPEP completely inhibits quisqualate-induced PI hydrolysis with IC50 value of 36nM. MPEP shows no effect in CHO-K1 cells expressing mGlu1b receptor or in L (tk-) mGlu5a cell line. In addition, 100μM MPEP also has no effect on group II and III mGlu receptor subtypes. Moreover, MPEP inhibits the DHPG induced PI hydrolysis in hippocampal, striatal and cortical slices with IC50 values of 8nM, 20.5nM and 17.9nM, respectively. Furthermore, microiontophoretical delivery of MPEP reduces DHPG-induced excitations in vivo. MPEP also shows anxiolytic-or antidepressant-like effects in the Vogel test in rats and in the tail suspension test in mice [1, 2].

References:
[1] Gasparini F, Lingenhohl K, Stoehr N, et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology, 1999, 38(10): 1493-1503.
[2] Tatarczyńska E, Klodzińska A, Chojnacka-Wójcik E, et al. Potential anxiolytic-and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. British journal of pharmacology, 2001, 132(7): 1423-1430.