SPECIFIC LABELING OF POSTSYNAPTIC ALPHA-1 ADRENOCEPTORS IN RAT-HEART VENTRICLE BY H-3-WB 4101

被引:47
作者
RAISMAN, R [1 ]
BRILEY, M [1 ]
LANGER, SZ [1 ]
机构
[1] LERS, DEPT BIOL SYNTHELABO, 58 RUE GLACIERE, F-75013 PARIS, FRANCE
关键词
α-Adrenoceptors; 6-Hydroxydopamine; !sup]3[!/sup]H-WB 4101; Pre-and postsynaptic receptors; Receptor binding;
D O I
10.1007/BF00505937
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The α-adrenoceptor ligand, 3H-WB 4101 binds to a single population of independent sites in the rat heart ventricle. These sites are not affected by chemical sympathectomy with 6-hydroxydopamine and thus appear to be located postsynaptically. The relative order of potencies for displacement of 3H-WB 4101 binding: prazosin>phentolamine>yohimbine, is characteristic of that of the α1 type of adrenoceptors. In heart ventricle 3H WB-4101 thus seems to label specifically postsynaptically located α1-adrenoceptors. The significance of the specificity of this ligand is discussed with relevance to its use in the central nervous system. © 1979 Springer-Verlag.
引用
收藏
页码:223 / 226
页数:4
相关论文
共 23 条
[1]   IDENTIFICATION OF CARDIAC BETA-ADRENERGIC RECEPTORS BY (-) [H-3]ALPRENOLOL BINDING [J].
ALEXANDER, RW ;
WILLIAMS, LT ;
LEFKOWITZ, RJ .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1975, 72 (04) :1564-1568
[2]  
BRILEY MS, 1979, BRIT J PHARMACOL, V66, pP90
[3]   BLOCKADE BY WB 4101 OF ALPHA-ADRENOCEPTORS IN RAT VAS-DEFERENS AND GUINEA-PIG TAENIA CECI [J].
BUTLER, M ;
JENKINSON, DH .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1978, 52 (3-4) :303-311
[4]  
CUBEDDU L, 1974, J PHARMACOL EXP THER, V190, P431
[5]   BRAIN ALPHA-ADRENERGIC RECEPTORS - COMPARISON OF [H-3]WB 4101 BINDING WITH NOREPINEPHRINE-STIMULATED CYCLIC-AMP ACCUMULATION IN RAT CEREBRAL-CORTEX [J].
DAVIS, JN ;
ARNETT, CD ;
HOYLER, E ;
STALVEY, LP ;
DALY, JW ;
SKOLNICK, P .
BRAIN RESEARCH, 1978, 159 (01) :125-135
[6]   NEGATIVE FEEDBACK REGULATION OF NORADRENALINE RELEASE BY NERVE-STIMULATION IN PERFUSED CATS SPLEEN - DIFFERENCES IN POTENCY OF PHENOXYBENZAMINE IN BLOCKING PRESYNAPTIC AND POST-SYNAPTIC ADRENERGIC-RECEPTORS [J].
DUBOCOVICH, ML ;
LANGER, SZ .
JOURNAL OF PHYSIOLOGY-LONDON, 1974, 237 (03) :505-519
[7]   ALPHA-NORADRENERGIC RECEPTORS IN BRAIN - DIFFERENTIAL EFFECTS OF SODIUM ON BINDING OF [H-3]AGONISTS AND [H-3]ANTAGONISTS [J].
GREENBERG, DA ;
UPRICHARD, DC ;
SHEEHAN, P ;
SNYDER, SH .
BRAIN RESEARCH, 1978, 140 (02) :378-384
[8]   ALPHA-NORADRENERGIC RECEPTOR-BINDING IN MAMMALIAN BRAIN - DIFFERENTIAL LABELING OF AGONIST AND ANTAGONIST STATES [J].
GREENBERG, DA ;
UPRICHARD, DC ;
SNYDER, SH .
LIFE SCIENCES, 1976, 19 (01) :69-76
[9]   COMPARATIVE-STUDY ON PRE-SYNAPTIC AND POST-SYNAPTIC ALPHA-BLOCKING ACTIVITY OF A SERIES OF BENZODIOXANES [J].
KAPUR, H ;
MOTTRAM, DR .
BIOCHEMICAL PHARMACOLOGY, 1978, 27 (14) :1879-1880
[10]   PRESYNAPTIC REGULATION OF CATECHOLAMINE RELEASE [J].
LANGER, SZ .
BIOCHEMICAL PHARMACOLOGY, 1974, 23 (13) :1793-1800