mGluR

325.77

DMSO : ≥ 33.33 mg/mL (102.31 mM)

Pale Brown to Light Brown Powder

-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with Kd of 1.1 nM. In competition binding experiments on human recombinant mGlu5, basimglurant fully displaces -MPEP with a Ki of 35.6 nM and -ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, basimglurant inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and -inositolphosphate accumulation with an IC50 of 5.9 nM. Basimglurant shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues.

Basimglurant is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg).

C₁₈H₁₃ClFN₃

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