LY393615 (NCC1048) is a novel blocker of both neuronal Ca²⁺ (calcium) and Na⁺ (sodium) channels, exhibiting half-maximal inhibitory concentrations (IC₅₀) of 1.9 µM and 5.2 µM against α1A and α1B calcium channel subunits, respectively. This compound demonstrates effective brain penetration and has shown neuroprotective effects in cerebral ischemia models, suggesting its utility in neurological disease research [1].

Ca2+ channel, P/Q-type:4 μM

LY393615 (0-10 μM) inhibits calcium flux in HEK293 cells with IC50 values of 1.9 μM and 5.2 μM against α1A and α1B calcium channel subunits, respectively, and exhibits an IC50 of 4.0 μM for the inhibition of P-type calcium channels in isolated Purkinje cells [1].

LY393615, administered intraperitoneally at doses of 12.5 or 15 mg/kg in a single injection, provided neuroprotection against hypoglycemic hypoxic injury and significantly protected against hippocampal damage caused by global cerebral ischemia in gerbils [1]. The compound exhibited favorable brain penetration, with half-lives of 2.04 hours following intravenous administration and 2.5 hours after intraperitoneal injection [1]. Pharmacokinetic parameters for LY393615 in gerbils indicated a half-life (T 1/2) of 2.04 hours for the 1 mg/kg intravenous dose and 2.5 hours for the 15 mg/kg intraperitoneal dose [1].