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NS-638

CAS No. : 150493-34-8

MCE 站：NS-638

产品活性：NS-638是具有阻断Ca²⁺-离子通道性质的非肽类小分子。细胞内阻断由K⁺激活的Ca²⁺浓度升高的IC₅₀值为3.4 μM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: NS-638 dose dependently inhibits K⁺-stimulated [45 Ca²⁺]-uptake in chick cortical synaptosomes and 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA)- stimulated [³H]GABA-release from cultured cortical neurons with IC₅₀ values of 2.3 and 4.3 μM, respectively. K⁺-stimulated intracellular Ca²⁺-elevation in cultured cerebellar granule cells is equipotently blocked with an IC₅₀ value of 3.4 μM. At this concentration no effect on Ca²⁺-induced contractions in K⁺-depolarized guinea pig taenia coli is observed. NS-638 reversibly blocks N- and L-type Ca²⁺-channels in cultured chick dorsal root ganglion cells in the concentration range of 1-30 μM.

In Vivo: In the mouse middle cerebral artery occlusion model, NS-638 administered i.p. (50 mg kg-1) at 1 h and 6 h post-ischemia, and once a day for the next two days, results in a 48% reduction in total infarct volume. It does not show protection against ischemic neuronal damage in the gerbil model of bilateral carotid artery occlusion.

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