(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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1. Doherty, A.J., Palmer, M.J., Henley, J.M., et al. (RS)-2-chloro-5-hydroxyphenylglycine (CHPG) activates mGlu5, but no mGlu1, receptors expressed in CHO cells and potentiates NMDA responses in the hippocampus. Neuropharmacology 36(2), 265-267 (1997).

2. Mutel, V., Ellis, G.J., Adam, G., et al. Characterization of [³H]quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J. Neurochem. 75(6), 2590-2601 (2000).

3. Qiu, J.-L., Zhu, W.-L., Lu, Y.-J., et al. The selective mGluR5 agonist CHPG attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. Neurochem Int. 85-86, 46-52 (2015).

4. Loane, D.J., Stoica, B.A., Byrnes, K.R., et al. Activation of mGluR5 and inhibition of NADPH oxidase improves functional recovery after traumatic brain injury. J. Neurotrauma 30(5), 403-412 (2013).