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MMPIP
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。
MMPIP图片
CAS NO:479077-02-6
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
MMPIP 是一种变构的选择性代谢型谷氨酸受体7 (mGluR7) 拮抗剂 (KB 值范围为 24-30 nM)。 MMPIP 可用于研究 mGluR7 对中枢神经系统功能的作用。MMPIP 可减轻神经病小鼠的疼痛并使其情感和认知行为正常化。
Cas No.479077-02-6
分子式C19H15N3O3
分子量333.34
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

MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1][2].

MMPIP inhibits L-(+)-2-amino-4-phosphonobutyric acid (L-AP4; 0.5 mM)-induced intracellular Ca2+ mobilization in Chinese hamster ovary (CHO) cells coexpressing rat mGluR7 with Gα15 (IC550=26 nM) [1]. In CHO cells expressing rat mGluR7, MMPIP inhibits L-AP4-induced inhibition of forskolin-stimulated cAMP accumulation (IC50 220 nM)[1].MMPIP also antagonizes L-AP4-induced inhibition of cAMP accumulation with an IC50 of 610 nM in CHO-human mGluR7/Gα15[1].

MMPIP (10 mg/kg) attenuates the amplitude of the acoustic startle response and markedly enhances the prepulse-induced inhibition of the acoustic startle response (up to 137% of control)[2].MMPIP (10 mg/kg) rescues the MK-801 (0.1 mg/kg)-induced cognitive impairments, by improving the choice accuracy[2].Zamifenacin exhibits short elimination half-lives (plasma 1.16 h, brain 1.75 h) following i.p. administration (10 mg/kg) in mice[2].

[1]. Gentaroh Suzuki, et al. In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists. J Pharmacol Exp Ther. 2007 Oct;323(1):147-56.
[2]. Paulina Cie?lik, et al. Negative Allosteric Modulators of mGlu 7 Receptor as Putative Antipsychotic Drugs. Front Mol Neurosci. 2018 Sep 20;11:316.