Basimglurant sulfate (RG 7090; RO 491752)

Description: Basimglurant sulfate (RG7090; RO491752) is apotent, selective and orally bioavailable mGlu5 negative allostericmodulator with a Kd of 1.1 nM. It is under Phase 2 clinical trial fortreating MDD and Fragile X syndrome(FXS). Basimglurant is a promising novel medicine for psychiatricdiseases. Basimglurant has favorable drug-like properties, adifferentiated molecular mechanism of action, and antidepressant-likefeatures which suggest the possibility of also addressing importantcomorbidities of MDD including anxiety and pain as well as daytimesleepiness and apathy or lethargy.

References:

1. LindemannL, et al. Pharmacology of basimglurant (RO4917523, RG7090), a uniquemetabotropic glutamate receptor 5 negative allosteric modulator inclinical development for depression. J Pharmacol Exp Ther. 2015Apr; 353(1):213-33.

2. JaeschkeG, et al. Metabotropic glutamate receptor 5 negative allostericmodulators: discovery of2-chloro-4-1-(4-fluorophenyl)-2, 5-dimethyl-1H-imidazol-4-ylethynylpyridine(basimglurant, RO4917523), a promising novel medicine for psychiatricdiseases.

Related CAS #: 802906-73-6 (Sulfate) 1034442-21-1 (free base)