Characterization of alpha(1)-adrenoceptor subtypes in rat spinal cord

被引:34
作者
Wada, T
Otsu, T
Hasegawa, Y
Mizuchi, A
Ono, H
机构
[1] SCI UNIV TOKYO,FAC PHARMACEUT SCI,DEPT PHARMACOL,SHINJUKU KU,TOKYO 162,JAPAN
[2] UNIV TOKYO,DEPT PHARM,BRANCH HOSP,FAC MED,BUNKYO KU,TOKYO 112,JAPAN
[3] MITSUI PHARMACEUT INC,INST BIOL SCI,MOBARA,CHIBA 297,JAPAN
关键词
spinal cord; alpha(1)-adrenoceptor subtype; BMY; 7378; 5-methyl-urapidil; H-3]prazosin; (rat);
D O I
10.1016/0014-2999(96)00570-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The a, adrenoceptor subtypes in ventral and dorsal horns of rat lumbar spinal cord were studied. High concentrations of the alpha(1D)-adrenoceptor antagonist, BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]-ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride), displaced bound [H-3]prazosin in a single-site manner and the binding affinity was close to those for alpha(1A)- and alpha(1B)-adrenoceptor binding sites. 5-Methyl-urapidil displaced bound [H-3]prazosin in a two-site manner and the high and low affinities were close to those of alpha(1A)- and alpha(1B)-adrenoceptor binding sites, respectively. The alpha(1)-adrenoceptor subtype populations of ventral and dorsal horns did not differ. The alpha(1A)- and alpha(1B)-adrenoceptor populations comprised 70% and 30%, respectively, of the total and very few alpha(1D)-adrenoceptors and a were detected.
引用
收藏
页码:263 / 266
页数:4
相关论文
共 12 条
[1]  
ALONSOLLAMAZARES A, 1995, J NEUROCHEM, V65, P2387
[2]  
BERVOETS K, 1994, J PHARMACOL EXP THER, V269, P110
[3]  
CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
[4]   BMY-7378 IS A SELECTIVE ANTAGONIST OF THE D-SUBTYPE OF ALPHA(1)-ADRENOCEPTORS [J].
GOETZ, AS ;
KING, HK ;
WARD, SDC ;
TRUE, TA ;
RIMELE, TJ ;
SAUSSY, DL .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1995, 272 (2-3) :R5-R6
[5]  
HIEBLE JP, 1995, PHARMACOL REV, V47, P267
[6]  
MICHEL MC, 1995, N-S ARCH PHARMACOL, V352, P1
[7]  
MICHEL MC, 1993, MOL PHARMACOL, V44, P1165
[8]  
MINNEMAN KP, 1994, ANNU REV PHARMACOL, V34, P117
[9]   PHARMACOLOGY OF DESCENDING NORADRENERGIC SYSTEMS IN RELATION TO MOTOR FUNCTION [J].
ONO, H ;
FUKUDA, H .
PHARMACOLOGY & THERAPEUTICS, 1995, 68 (01) :105-112
[10]  
PEREZ DM, 1991, MOL PHARMACOL, V40, P876