Foliglurax monohydrochloride (PXT002331 (monohydrochloride)) (PXT002331 monohydrochloride) 是一种高选择性和有效的脑渗透性代谢型谷氨酸受体 4 正变构调节剂 (mGluR4 PAM)，EC50 为 79 nM。
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant mGluR4 positive allosteric modulator (PAM), with an EC50 of 79±19 nM[1]. Antiparkinsonian effect[1].
Foliglurax, a highly selective and potent mGlu4 receptor PAM with a marked brain-penetrance feature, might revolutionize the field of mGlu4 receptor drug targeting in CNS disorders[2].
[1]. Charvin D, et al. Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive 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 discovery targeting metabotropic glutamate receptor 4. Expert Opin Drug Discov. 2018 May;13(5):411-423.
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