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Basimglurant

CAS No. : 802906-73-6

MCE 站：Basimglurant

产品活性：Basimglurant (RG7090) 是高效，选择性有口服活性的mGlu5负变构调节剂，K_d值为1.1 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: [³H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with K_d of 1.1 nM. In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [³H]-MPEP with a K_i of 35.6 nM and [³H]-ABP688 with a K_i of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca²⁺ mobilization with an IC₅₀ of 7.0 nM and [³H]-inositolphosphate accumulation with an IC₅₀ of 5.9 nM. Basimglurant (RG7090) shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues.

In Vivo: Basimglurant (RG7090) 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 (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg).

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