• Metabotropic Glutamate Receptors
• mGlu2/3 Receptor and MDD
• mGlu2/3 Receptor and TRD
• mGlu2/3 Receptor and AD

 

mGlu2/3 Receptor and MDD

In 2007, BCI licensed BCI-632 (MGS0039) and its oral prodrug BCI-838 (MGS0210) from Taisho Pharmaceutical Co. Ltd.

Functionally, BCI-632 is a competitive antagonist with a high potency to both mGlu2 and mGlu3. BCI-632 is robustly active in acute as well as chronic rodent models of depression including Forced Swim, Tail Suspension, Learned Helplessness, Novelty Suppression of Feeding, Chronic Corticosterone and in isolation reared animals. In addition, BCI-632 robustly triggers serotonin release in the medial prefrontal cortex as well as neurogenesis in the dentate gyrus after chronic dosing in rats and mice. Taken together, these data suggest that blocking mGlu2/3 may confer anti-depressive activity in patients suffering from major depressive disorder (MDD).