VINPOCETINE IS AS POTENT AS PHENYTOIN TO BLOCK VOLTAGE-GATED NA+ CHANNELS IN RAT CORTICAL-NEURONS

被引：60

作者：

MOLNAR, P

ERDO, SL

机构：

[1] CNS Pharmacology Laboratory, Chinoin Co. Ltd., H-1045 Budapest

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 273卷 / 03期

关键词：

VINPOCETINE; PHENYTOIN; NA+; CHANNEL; VOLTAGE-GATED; ANTICONVULSANT; NEUROPROTECTION; CORTICAL NEURON; (RAT);

D O I：

10.1016/0014-2999(94)00755-V

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of vinpocetine and phenytoin on voltage-gated Na+ channels were examined on cultured cerebrocortical neurones of the rat using a conventional whole-cell patch-clamp method. Vinpocetine and phenytoin decreased Na+ currents in a concentration-dependent manner, with IC50 values of 44.2 +/- 14.6 and 50.5 +/- 17.4 mu M, respectively. Both compounds shifted the voltage dependence of the steady-state inactivation of the channel in the hyperpolarising direction. This pronounced Na+ channel blocking activity may contribute to the neuroprotective and anticonvulsant effects of vinpocetine.

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页码：303 / 306

页数：4

相关论文

共 14 条

[1] A DOUBLE-BLIND PLACEBO CONTROLLED EVALUATION OF THE SAFETY AND EFFICACY OF VINPOCETINE IN THE TREATMENT OF PATIENTS WITH CHRONIC VASCULAR SENILE CEREBRAL-DYSFUNCTION [J].

BALESTRERI, R ;

FONTANA, L ;

ASTENGO, F .

JOURNAL OF THE AMERICAN GERIATRICS SOCIETY, 1987, 35 (05) :425-430

[2] VINPOCETIN PROTECTS AGAINST EXCITOTOXIC CELL-DEATH IN PRIMARY CULTURES OF RAT CEREBRAL-CORTEX [J].

ERDO, SL ;

NINGSHENG, C ;

WOLFF, JR ;

KISS, B .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 187 (03) :551-553

[3] LACK OF EXCITOTOXIC CELL-DEATH IN SERUM-FREE CULTURES OF RAT CEREBRAL-CORTEX [J].

ERDO, SL ;

MICHLER, A ;

WOLFF, JR ;

TYTKO, H .

BRAIN RESEARCH, 1990, 526 (02) :328-332

[4]

FROSTL W, 1989, PHARMACOPSYCHIATRY S, V22, P51

[5] SELECTIVE INHIBITORS OF 3 FORMS OF CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES [J].

HIDAKA, H ;

TANAKA, T ;

ITOH, H .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1984, 5 (06) :237-239

[6] THE USE OF XENOPUS OOCYTES TO EVALUATE DRUGS AFFECTING BRAIN CA2+ CHANNELS - EFFECTS OF BIFEMELANE AND SEVERAL NOOTROPIC AGENTS [J].

KANEKO, S ;

TAKAHASHI, H ;

SATOH, M .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1990, 189 (01) :51-58

[7] EFFECTS OF SEVERAL CEREBROPROTECTIVE DRUGS ON NMDA CHANNEL FUNCTION - EVALUATION USING XENOPUS OOCYTES AND [H-3] MK-801 BINDING [J].

KANEKO, S ;

SUGIMURA, M ;

INOUE, T ;

SATOH, M .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1991, 207 (02) :119-128

[8]

KARPATI E, 1976, ARZNEIMITTEL-FORSCH, V26, P1908

[9] VINPOCETINE PREFERENTIALLY ANTAGONIZES QUISQUALATE AMPA RECEPTOR RESPONSES - EVIDENCE FROM RELEASE AND LIGAND-BINDING STUDIES [J].

KISS, B ;

CAI, NS ;

ERDO, SL .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 209 (1-2) :109-112

[10] VINPOCETINE INCREASES THE NEUROPROTECTIVE EFFECT OF ADENOSINE INVITRO [J].

KRIEGLSTEIN, J ;

RISCHKE, R .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 205 (01) :7-10