mGluR2antagonist1是一种口服有效的，可透过血脑屏障的选择性mGluR2负变构调节剂(IC50为9nM)。
货号:ajcx31060
CAS:1432728-49-8
分子式:C21H16FN3O3
分子量：377.37
溶解度:DMSO: 100 mg/mL (264.99 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability[1].

In vivo, mGluR2 antagonist 1 (Compound 25) reverses the effect of mGluR2 agonist LY379268 in amphetamine-induced hyperlocomotion and shows good efficacy in the mouse delayed non-match to position assay at 10 mg/kg.

[1]. Youheng Shu,et al. Discovery of 4-arylquinoline-2-carboxamides, Highly Potent and Selective Class of mGluR2 Negative Allosteric Modulators: From HTS to Activity in Animal Models. Bioorg Med Chem Lett. 2020 May 1;30(9):127066.