EVIDENCE THAT AN ATYPICAL BETA-ADRENOCEPTOR MEDIATES THE INHIBITION OF SPONTANEOUS RHYTHMICAL CONTRACTIONS OF RABBIT ISOLATED JEJUNUM INDUCED BY RITODRINE AND SALBUTAMOL

被引:31
作者
NORMAN, BJ [1 ]
LEATHARD, HL [1 ]
机构
[1] CHARING CROSS & WESTMINSTER MED SCH,DEPT PHARMACOL,LONDON W6 8RF,ENGLAND
关键词
D O I
10.1111/j.1476-5381.1990.tb12083.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. The nature of the adrenoceptors mediating the inhibitory action of noradrenaline, ritodrine and salbutamol on the spontaneous activity of longitudinal muscle of the rabbit jejunum in vitro was investigated by use of a range of adrenoceptor antagonists. 2. The actions of ritodrine and salbutamol were antagonized competitively by propranolol. The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for β1- and β2-adrenoceptors. 3. In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (>2.7 μM) of phentolamine and were unaffected by yohimbine (2.6 μM), mepyramine (2.5 μM) or cimetidine (4.0 μM). 4. Ritodrine which is less potent than salbutamol in tissues with typical β2-adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5. It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical β-adrenoceptor, at which propranolol is a competitive but not very potent antagonist.
引用
收藏
页码:27 / 30
页数:4
相关论文
共 26 条
[1]   ATYPICAL BETA-ADRENOCEPTOR ON BROWN ADIPOCYTES AS TARGET FOR ANTI-OBESITY DRUGS [J].
ARCH, JRS ;
AINSWORTH, AT ;
CAWTHORNE, MA ;
PIERCY, V ;
SENNITT, MV ;
THODY, VE ;
WILSON, C ;
WILSON, S .
NATURE, 1984, 309 (5964) :163-165
[2]   SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].
ARUNLAKSHANA, O ;
SCHILD, HO .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01) :48-58
[3]   AGONIST AND ANTAGONIST CHARACTERIZATION OF A PUTATIVE ADRENOCEPTOR WITH DISTINCT PHARMACOLOGICAL PROPERTIES FROM THE ALPHA-SUBTYPES AND BETA-SUBTYPES [J].
BOND, RA ;
CLARKE, DE .
BRITISH JOURNAL OF PHARMACOLOGY, 1988, 95 (03) :723-734
[4]   INHIBITION OF RABBIT INTESTINE MEDIATED BY ALPHA-ADRENOCEPTORS AND BETA-ADRENOCEPTORS [J].
BOWMAN, WC ;
HALL, MT .
BRITISH JOURNAL OF PHARMACOLOGY, 1970, 38 (02) :399-&
[5]   CIMETIDINE - NON-THIOUREA H2-RECEPTOR ANTAGONIST [J].
BRIMBLECOMBE, RW ;
DUNCAN, WAM ;
DURANT, GJ ;
EMMETT, JC ;
GANELLIN, CR ;
PARSONS, ME .
JOURNAL OF INTERNATIONAL MEDICAL RESEARCH, 1975, 3 (02) :86-92
[6]  
BRISTOW M, 1970, J PHARMACOL EXP THER, V171, P52
[7]   A PHYSIOLOGICAL-BASIS FOR SUBCLASSIFYING BETA-ADRENOCEPTORS EXAMINED BY CHEMICAL SYMPATHECTOMY OF GUINEA-PIGS [J].
BROADLEY, KJ ;
CHESSWILLIAMS, RG ;
GRASSBY, PF .
JOURNAL OF PHYSIOLOGY-LONDON, 1986, 373 :367-378
[8]  
COLEMAN R A, 1987, British Journal of Pharmacology, V90, p40P
[9]  
COLTON T, 1974, STAT MED, P194
[10]   DIFFERENTIATION OF BETA-ADRENORECEPTORS BY USE OF BLOCKING AGENTS [J].
FARMER, JB ;
LEVY, GP .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1970, 22 (02) :145-&