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NS 638 is an inhibitor of the N-type voltage-gated calcium channel Cav2.2 and CNS L-type calcium channels.1 It inhibits potassium-induced calcium uptake in chick cortical synaptosomes (IC50 = 3.4 µM) and AMPA-induced GABA release from primary chick cortical neurons (IC50 = 4.3 µM), effects that can be blocked by the N-type calcium channel inhibitor ω-conotoxin GVIA (Item No. 24114) but not the L-type calcium channel inhibitor nifedipine (Item No. 11106). It also inhibits potassium-induced calcium level increases in primary chick cerebellar granule cells (IC50 = 3.4 µM), an effect that can be blocked by nifedipine but not ω-conotoxin GVIA. NS 638 (50 mg/kg) reduces infarct volume in a mouse model of focal ischemia induced by middle cerebral artery occlusion (MCAO) but not in a gerbil model of global ischemia induced by bilateral carotid artery occlusion (BCAO).
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1. Pharmacological profile and anti-