tcsc0343 LY341495

LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC₅₀s of 2.9 nM, 10 nM, 170 nM for mGluR-2, mGluR-3, mGluR-8, respectively.

IC50 & Target: IC50: 2.9 nM (mGluR-2, human), 10 nM (mGluR-3, human), 170 nM (mGluR-8, human)

In Vivo: LY341495 (0.3, 1, and 3 mg/kg, i.p.) displays a lower level of discrimination in rats^[1]. LY341495 (3.0 mg/kg) decreases Dvl-2, pGSK-3α/β and β-catenin protein levels but Dvl-1, Dvl-3 and GSK-3α/β are unaffected in both the PFC and STR. LY341495 has the generally the opposite effect following acute and chronic administration compared to mGlu2/3 agonist, LY379268^[2]. LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression is not altered in either KO brain. LY341495 is almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)] in mGluR3-KO mice^[3].