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The naphthalenesulphonamide calmodulin antagonist W7 and its 5-iodo-1-C8 analogue inhibit potassium and calcium currents in NG108-15 neuroblastoma x glioma cells in a manner possibly unrelated to their antagonism of calmodulin.

作者信息

Caulfield M P, Robbins J, Sim J A, Brown D A, Mac Neil S, Blackburn G M

机构信息

Department of Pharmacology, University College London, U.K.

出版信息

Neurosci Lett. 1991 Apr 15;125(1):57-61. doi: 10.1016/0304-3940(91)90130-l.

DOI:10.1016/0304-3940(91)90130-l
PMID:1649984
Abstract

Patch clamp techniques were used to record voltage-sensitive calcium and potassium currents from NG108-15 cells. N-(6-aminohexyl)-5-chloro-1-naphthalene- sulphonamide (W7), a calmodulin (CaM) antagonist and its more potent (10 times) 5-iodo-1-C8 analogue (J8) inhibited these currents in a dose-dependent manner. The inhibition was not dependent on internal or external Ca2+. W7 was about four times more potent as an inhibitor of the transient potassium current (IC50 = 8 microM) than of the M-current or of the calcium current. J8 was also selective for the potassium currents (IC50 values: transient current 4 microM, M-current 11 microM) compared to the calcium current (IC50 36 microM). It is suggested that the inhibition does not result from an anti-CaM action of the compounds.

摘要

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