Cayman (R,S)-CHPG

(R,S)-CHPG is a potent and selective agonist at metabotropic glutamate receptor 5 (mGluR5). In CHO Cells, it had an EC₅₀ of 750 µM for calcium mobilization in mGluR5a-expressing cells but was inactive in mGluR1a-expressing cells.¹ In transfected HEK293 cells, (R,S)-CHPG bound mGluR1a and mGluR5a (K_is = 0.9 and 3.9 µM, respectively) but not ionotropic glutamate receptors.² It reduced oxidative stress and inflammatory markers in cultured BV-2 microglial cells.³ In mouse models of traumatic brain injury, it reduced lesion volume, improved sensorimotor deficits in the beam walk test, and improved spatial memory in the Morris water maze.⁴

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