An N- and L-type calcium channel inhibitor
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 ?M) and AMPA-induced GABA release from primary chick cortical neurons (IC50 = 4.3 ?M), effects that can be blocked by the N-type calcium channel inhibitor ω-conotoxin GVIA but not the L-type calcium channel inhibitor nifedipine . It also inhibits potassium-induced calcium level increases in primary chick cerebellar granule cells (IC50 = 3.4 ?M), 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).
1.M?ller, A., Christophersen, P., Drejer, J., et al.Pharmacological profile and anti-ischemic properties of the Ca2+-channel blocker NS-638Neurol. Res.17(5)353-360(1995)
Cell experiment: | The effect of NS-638 on neuronal Ca2+-channels is evaluated using whole cell patch clamp techniques[1]. |
Animal experiment: | Mice: In the mouse middle cerebral artery occlusion model, NS-638 is administered i.p. (50 mg kg-1) at 1 h and 6 h post-ischemia, and once a day for the next two days[1]. |
参考文献: [1]. M?ller A, et al. Pharmacological profile and anti-ischemic properties of the Ca(2+)-channel blocker NS-638. Neurol Res. 1995 Oct;17(5):353-60. | |
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