CHARACTERIZATION OF ADENOSINE RECEPTORS IN THE RAT ISOLATED AORTA

被引:58
作者
LEWIS, CD
HOURANI, SMO
LONG, CJ
COLLIS, MG
机构
[1] UNIV SURREY,SCH BIOL SCI,GUILDFORD GU2 5XH,SURREY,ENGLAND
[2] PFIZER LTD,CENT RES,SANDWICH CT13 9NJ,KENT,ENGLAND
来源
GENERAL PHARMACOLOGY | 1994年 / 25卷 / 07期
关键词
RAT AORTA; ADENOSINE; PURINOCEPTORS; ENDOTHELIUM;
D O I
10.1016/0306-3623(94)90162-7
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. Adenosine and its analogues relaxed the isolated rat aorta by an endothelium-dependent mechanism with an order of potency of 5'-N-ethylcarboxamidoadenosine (NECA) > 2-(p-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine (CGS 21680) > adenosine = N-6-(2-(4-aminophenyl)ethyl)adenosine (APNEA) = N-6-cyclopentyladenosine (CPA) > 5'-methylthioadenosine (MTA), although the maximal response achieved by CGS 21680 was less than that achieved by NECA. 2. Both 8-sulphophenyltheophylline (8-SPT) and MTA antagonized responses to the adenosine analogues, but there were some anomolous features of this antagonism and NECA was inhibited more powerfully than the other agonists. This suggests that as well as A(2a) receptors mediating relaxation, the rat aorta may relax to adenosine analogues by other mechanisms.
引用
收藏
页码:1381 / 1387
页数:7
相关论文
共 37 条
[1]  
AGARWAL KC, 1980, BIOCHEM PHARMACOL, V29, P1529
[2]   COMPARATIVE EFFECTS OF A SELECTIVE ADENOSINE A2-RECEPTOR AGONIST, CGS-21680, AND NITROPRUSSIDE IN VASCULAR SMOOTH-MUSCLE [J].
BALWIERCZAK, JL ;
SHARIF, R ;
KRULAN, CM ;
FIELD, FP ;
WEISS, GB ;
MILLER, MJS .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1991, 196 (02) :117-123
[3]  
BRACKETT LE, 1991, J PHARMACOL EXP THER, V257, P205
[4]  
BRUNS RF, 1986, MOL PHARMACOL, V29, P331
[5]   ADENOSINE RELAXES THE AORTA BY INTERACTING WITH AN A2-RECEPTOR AND AN INTRACELLULAR SITE [J].
COLLIS, MG ;
BROWN, CM .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1983, 96 (1-2) :61-69
[6]   APPARENT AFFINITY OF SOME 8-PHENYL-SUBSTITUTED XANTHINES AT ADENOSINE RECEPTORS IN GUINEA-PIG AORTA AND ATRIA [J].
COLLIS, MG ;
JACOBSON, KA ;
TOMKINS, DM .
BRITISH JOURNAL OF PHARMACOLOGY, 1987, 92 (01) :69-75
[7]  
COLLIS MG, 1993, TRENDS PHARMACOL SCI, V14, P360
[8]   APPARENT AFFINITY OF 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE FOR ADENOSINE-A1 AND ADENOSINE-A2 RECEPTORS IN ISOLATED-TISSUES FROM GUINEA-PIGS [J].
COLLIS, MG ;
STOGGALL, SM ;
MARTIN, FM .
BRITISH JOURNAL OF PHARMACOLOGY, 1989, 97 (04) :1274-1278
[9]  
COLLIS MG, 1990, PURINES IN CELLULAR SIGNALLING, P48
[10]   ADENOSINE RECEPTORS IN ISOLATED TISSUE PREPARATIONS [J].
COLLIS, MG .
NUCLEOSIDES & NUCLEOTIDES, 1991, 10 (05) :1057-1066