(+/-)-LY367385

(±)-LY367385 is an antagonist of metabotropic glutamate receptor 1α (mGluR1α).¹ It inhibits phosphoinositide (PI) hydrolysis selectively in AV-12 cells expressing mGluR1α over those expressing mGluR5a (IC₅₀s = 19 and >300 μM, respectively).

(±)-LY367385 is the racemate of LY367385. LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis，compared with > 100 μM for mGlu5a[1][2].

1. Salt, T.E., Jones, H.E., Copeland, C.S., et al. Function of mGlu1 receptors in the modulation of nociceptive processing in the thalamus Neuropharmacology 79(100),405-411(2014).