VOLTAGE DEPENDENCIES OF THE EFFECTS OF CHLORPROMAZINE ON THE NICOTINIC RECEPTOR-CHANNEL FROM MOUSE MUSCLE-CELL LINE SOL8

被引：29

作者：

BENOIT, P

CHANGEUX, JP

机构：

[1] CNRS UA D1284 'Neurobiologie Moléculaire', Département des Biotechnologies, Institut Pasteur, Paris

来源：

NEUROSCIENCE LETTERS | 1993年 / 160卷 / 01期

关键词：

NICOTINIC RECEPTOR; CHANNEL BLOCKER; NEUROLEPTICS; CHLORPROMAZINE;

D O I：

10.1016/0304-3940(93)90918-B

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

The effects of chlorpromazine (CPZ) on nicotinic acetylcholine receptor (nAChR) were re-investigated by patch-clamp recordings on a mouse muscle cell line: (1) CPZ decreased the channel-opening frequency and, thus, acted as a closed-channel blocker. This effect was independent of the membrane potential and was consistent with an enhanced desensitization of the nAChR. (2) In addition, CPZ decreased the mean channel open time of the nAChR in a concentration- and voltage-dependent manner and, thus, behaved as an open-channel blocker. The latter effect supports the notion that CPZ binds to a site within the nAChR ionic channel.

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页码：81 / 84

页数：4

相关论文

共 23 条

[1] ELECTRO-PHYSIOLOGICAL AND BIOCHEMICAL-STUDIES ON ENHANCEMENT OF DESENSITIZATION BY PHENOTHIAZINE NEUROLEPTICS [J].

CARP, JS ;

ARONSTAM, RS ;

WITKOP, B ;

ALBUQUERQUE, EX .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1983, 80 (01) :310-314

[2] EFFECTS OF CHLORPROMAZINE AND PHENCYCLIDINE ON MOUSE C2 ACETYLCHOLINE-RECEPTOR KINETICS [J].

CHANGEUX, JP ;

PINSET, C ;

RIBERA, AB .

JOURNAL OF PHYSIOLOGY-LONDON, 1986, 378 :497-513

[3]

CHANGEUX JP, 1990, FIDIA RES F NEUROSCI, V4, P21

[4] TRIFLUOPERAZINE REDUCES INWARD IONIC CURRENTS AND SECRETION BY SEPARATE MECHANISMS IN BOVINE CHROMAFFIN CELLS [J].

CLAPHAM, DE ;

NEHER, E .

JOURNAL OF PHYSIOLOGY-LONDON, 1984, 353 (AUG) :541-564

[5]

COX RN, 1985, J BIOL CHEM, V260, P7186

[6]

DIPAOLA M, 1990, J BIOL CHEM, V265, P11017

[7] STRUCTURE OF THE HIGH-AFFINITY BINDING-SITE FOR NONCOMPETITIVE BLOCKERS OF THE ACETYLCHOLINE-RECEPTOR - SERINE-262 OF THE DELTA-SUBUNIT IS LABELED BY [H-3] CHLORPROMAZINE [J].

GIRAUDAT, J ;

DENNIS, M ;

HEIDMANN, T ;

CHANG, JY ;

CHANGEUX, JP .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (08) :2719-2723

[8] THE NONCOMPETITIVE BLOCKER [H-3] CHLORPROMAZINE LABELS SEGMENT M2 BUT NOT SEGMENT M1 OF THE NICOTINIC ACETYLCHOLINE-RECEPTOR ALPHA-SUBUNIT [J].

GIRAUDAT, J ;

GALZI, JL ;

REVAH, F ;

CHANGEUX, JP ;

HAUMONT, PY ;

LEDERER, F .

FEBS LETTERS, 1989, 253 (1-2) :190-198

[9] CHARACTERIZATION OF THE TRANSIENT AGONIST-TRIGGERED STATE OF THE ACETYLCHOLINE-RECEPTOR RAPIDLY LABELED BY THE NONCOMPETITIVE BLOCKER [H-3] CHLORPROMAZINE - ADDITIONAL EVIDENCE FOR THE OPEN CHANNEL CONFORMATION [J].

HEIDMANN, T ;

CHANGEUX, JP .

BIOCHEMISTRY, 1986, 25 (20) :6109-6113

[10] TIME-RESOLVED PHOTOLABELING BY THE NONCOMPETITIVE BLOCKER CHLORPROMAZINE OF THE ACETYLCHOLINE-RECEPTOR IN ITS TRANSIENTLY OPEN AND CLOSED ION CHANNEL CONFORMATIONS [J].

HEIDMANN, T ;

CHANGEUX, JP .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1984, 81 (06) :1897-1901