LY2794193

LY2794193 is a highly potent and selective mGlu3 receptor agonist ( hmGlu3 K i =0.927 nM， EC 50 =0.47 nM; hmGlu2 K i =412 nM， EC 50 =47.5 nM) In Vitro LY2794193 exhihits inhibition of spontaneous Ca 2+ oscillations in cultured rat cortical neurons with an EC 50 of 43.6 nM. In the rat cortical neuron Ca 2+ oscillation assay, LY2794193 exhibits a biphasic inhibition of spontaneous Ca 2+ transients (high affinity EC 50 =0.44 nM; 48% of the total agonist response; low affinity EC 50 =43.6 nM; 52% of the total agonist response) with combined maximal agonist efficacy (E max ) of 66%. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo LY2794193 (1-30 mg/kg, s.c.), given 30 min prior to PCP (5 mg/kg, s.c.) leads a dose-related reduction in ambulations . LY2794193 (1 mg/kg; i.v.) exhibits moderate clearance (18.3 mL/min per kg) and volume of distribution (1.17 L/kg) with a calculated plasma half-life (T 1/2 ) of 3.1 h in Male Sprague-Dawley rats . LY2794193 (3 mg/kg; s.c.) leads to the rapid appearance in the plasma (AUC=9.9 μM; C max =6.78 μM; T max =0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats Dosage: 1, 3, 10, or 30 mg/kg Administration: Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.) Result: A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant. Form:Solid IC50& Target:mGluR3 0.47 nM (EC 50 ) mGluR3 0.927 nM (Ki) mGluR2 47.5 (EC 50 ) mGluR2 412 (Ki)

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