LY354740

LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively). It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM). LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Cay-14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM). LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm. It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg. LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.Formal Name: (1S,2S,5R,6S)-2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid. CAS Number: 176199-48-7. Molecular Formula: C8H11NO4. Formula Weight: 185.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. SMILES: OC([C@H]1[C@@]2([H])[C@]1([H])[C@@](C(O)=O)(N)CC2)=O. InChi Code: InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1. InChi Key: VTAARTQTOOYTES-RGDLXGNYSA-N.