An N-type calcium channel blocker
PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
PD173212 (PD 173212, 300 nM) potently blocks recombinant B-class (N-type) calcium channel currents 78±7.8%, with an IC50 of 74 nM, by whole-cell voltage-clamp techniques. PD 173212 possesses selectivity for non L-type Ca2+ channels versus neuronal Na+, K+, and L-type Ca2+ channels[1].
PD173212 (30 mg/kg, i.v.) shows moderate efficacy in preventing tonic seizures in the audiogenic seizure model[1].
参考文献:
[1]. Hu LY, et al. Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2151-6.
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