Foliglurax monohydrochloride (PXT002331 monohydrochloride) 是一种可渗透脑的,有效的选择性mGluR4 正变构调节剂 (PAM),EC50 为 79±19 nM。抗帕金森病。
Foliglurax monohydrochloride (PXT002331 monohydrochloride) 分子图Foliglurax monohydrochlorideChemical Structure
CAS No. : 2133294-96-7
分子量:457.97
分子式:C₂₃H₂₄ClN₃O₃S
CAS No.:2133294-96-7
描述:Foliglurax monohydrochloride(PXT002331monohydrochloride)是一种高选择性和有效的脑渗透性mGluR4正变构调节剂(PAM),EC50为79±19 nM [1]。抗帕金森病的作用[1]。
IC50 & Target[1]:mGlu479 nM (EC50)
体外:Foliglurax是一种高选择性和有效的mGlu4受体PAM,具有明显的脑外显能特征,可能彻底改变中枢神经系统疾病中mGlu4受体药物靶向的领域[2]。
相关文献:
[1]. Charvin D, et al. Discovery, Structure-Activity Relationship, andAntiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series ofPositive Allosteric Modulators of Metabotropic Glutamate Receptor 4. J Med Chem.2017 Oct 26;60(20):8515-8537.
[2]. Volpi C, et al. Opportunities and challenges in drug discoverytargeting metabotropic glutamate receptor 4. Expert Opin Drug Discov. 2018May;13(5):411-423.
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