ТЭЦ

Описание

(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. 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. It reduced oxidative stress and inflammatory markers in cultured BV-2 microglial cells. 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.

Использование

CHPG is a selective mGluR-5 agonist.

Биологическая активность

A selective mGlu 5 metabotropic glutamate receptor agonist, completely inactive at mGlu 1a receptors expressed in CHO cells. Active in vivo .