Blocking of Cloned Low-Threshold Ca2+ Channels by Neuroleptic Drugs
作者： VN Osipenko , VG Naidenov , PG Kostyuk , Ya M Shuba
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摘要: We studied the blocking action of neuroleptic drugs, haloperidol, pimozide, and fluspirilene, on three types cloned low voltage-activated (T-type) Ca2+ channels, α1G, α1H, α1I, functionally expressed in Xenopus oocytes. Fluspirilene pimozide (members diphenylbutylpiperidine group) haloperidol (belonging to butyrophenones) inhibited currents with different values Kd constant maximum intensity blocking. Effects neuroleptics were voltage-dependent accompanied by slowing-down kinetics currents. The mechanism is probably based interaction between channels activated inactivated states. difference efficiency specificity blockade various T-channel subtypes should be considered when estimating therapeutic significance tested pharmacological agents.
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