LY2794193

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%. < /p>

LY2794193 (1-30 mg/kg, sc), given 30 min prior to PCP (5 mg/kg, sc) leads a dose-related reduction in ambulations.
LY2794193 (1 mg/ kg; iv) 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; sc) 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.