【摘 要】
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The first-generation antihistamines are widely prescribed medications to relieve allergic reactions and urticaria by blocking the peripheral histamine H1 re
【机 构】
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Department of Pharmacology, Hebei Medical University
【出 处】
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中国神经科学学会第四次会员代表大会暨第七届全国学术会议(The 7th Biennial Meeting and the
论文部分内容阅读
The first-generation antihistamines are widely prescribed medications to relieve allergic reactions and urticaria by blocking the peripheral histamine H1 receptor.Overdose of these drugs often results in serious neuronal toxic effects,including seizures,convulsions and worsening of epileptic symptoms.Till now,the molecular mechanism underlying these adverse effects has not been fully understood.KCNQ/M K+ channel plays a crucial role in controlling neuron excitability.Here,we demonstrate that mepyramine and diphenhydrarnine,two structurally related first-generation antihistamines,can act as potent KCNQ/M channel blockers.Extracellular application of these drugs quickly and reversibly reduced KCNQ2/Q3 currents heterologously expressed in HEK293 cells.The current inhibition was concentration and voltage dependent.The estimated IC50 (12.5 and 48.1 μmol/L,respectively) is within the scope of drug concentrations detected in poisoned patients (30 to 300 μmol/L).Both drugs shifted the Ⅰ-Ⅴ curve of KCNQ2/Q3 channel to more depolarized potentials,and altered channel gating property by prolonging activation and shortening deactivation kinetics.
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