| Description: |
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 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. |
