EVANS BLUE BLOCKS P(2X)-PURINOCEPTORS IN RAT VAS-DEFERENS

被引:31
作者
BULTMANN, R
STARKE, K
机构
[1] Pharmakologisches Institut, Universität Freiburg, Freiburg i. Br., D-79104
关键词
RAT VAS DEFERENS; EVANS BLUE; ALPHA; BETA-METHYLENE ATP; SURAMIN; P(2X)-PURINOCEPTORS; P(2)-PURINOCEPTOR ANTAGONIST;
D O I
10.1007/BF00167248
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In rat vas deferens, Evans blue 100 muM increased contractions elicited by high K+ and by noradrenaline but markedly reduced contractions elicited by the P2X-purinoceptor-selective agonist alpha,beta-methylene ATP (3 muM). The concentration-response curve of alpha,beta-methylene ATP was shifted to the right by Evans blue 30 muM and the maximal contraction was increased. In tissues incubated with nifedipine 10 muM, Evans blue 100 muM tended to increase the residual contraction elicited by noradrenaline and abolished the residual response to alpha,beta-methylene ATP (3 muM). The concentration-response curve of alpha,beta-methylene ATP was progressively shifted to the right by increasing concentrations of Evans blue in the presence of nifedipine; maximal contractions were increased by Evans blue 10 and 30 but not 100 muM. From the shifts to the right caused by Evans blue 30 muM, apparent pK(B) values of 5.9 (no nifedipine) and 6.0 (nifedipine present) were calculated. It is concluded that Evans blue blocks P2X-purinoceptors in rat vas deferens and in addition causes a non-receptor-specific enhancement of contractions.
引用
收藏
页码:684 / 687
页数:4
相关论文
共 17 条
[1]   SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].
ARUNLAKSHANA, O ;
SCHILD, HO .
BRITISH JOURNAL OF PHARMACOLOGY AND CHEMOTHERAPY, 1959, 14 (01) :48-58
[2]   INHIBITION BY ETHANOL OF CONTRACTIONS OF RAT VAS-DEFERENS - NO EVIDENCE FOR SELECTIVE BLOCKADE OF P(2X)-PURINOCEPTORS [J].
BULTMANN, R ;
SZABO, B ;
STARKE, K .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1993, 347 (05) :527-533
[3]  
BULTMANN R, IN PRESS NAUNYNSCHMI, P349
[4]   P2-PURINOCEPTORS OF 2 SUBTYPES IN THE RABBIT MESENTERIC-ARTERY - REACTIVE BLUE-2 SELECTIVELY INHIBITS RESPONSES MEDIATED VIA THE P2Y-PURINOCEPTOR BUT NOT THE P2X-PURINOCEPTOR [J].
BURNSTOCK, G ;
WARLAND, JJI .
BRITISH JOURNAL OF PHARMACOLOGY, 1987, 90 (02) :383-391
[5]   IS THERE A BASIS FOR DISTINGUISHING 2 TYPES OF P2-PURINOCEPTOR [J].
BURNSTOCK, G ;
KENNEDY, C .
GENERAL PHARMACOLOGY, 1985, 16 (05) :433-440
[6]   P-2 RECEPTOR - SUBCLASSIFICATION AND STRUCTURE-ACTIVITY-RELATIONSHIPS [J].
CUSACK, NJ .
DRUG DEVELOPMENT RESEARCH, 1993, 28 (03) :244-252
[7]   SURAMIN - A REVERSIBLE P2-PURINOCEPTOR ANTAGONIST IN THE MOUSE VASDEFERENS [J].
DUNN, PM ;
BLAKELEY, AGH .
BRITISH JOURNAL OF PHARMACOLOGY, 1988, 93 (02) :243-245
[8]  
FURCHGOTT RF, 1972, HDB EXPT PHARM, V33, P283
[9]   CO-TRANSMISSION IN THE RAT VAS-DEFERENS - POSTJUNCTIONAL SYNERGISM OF NORADRENALINE AND ADENOSINE 5'-TRIPHOSPHATE [J].
HUIDOBROTORO, JP ;
PARADA, S .
NEUROSCIENCE LETTERS, 1988, 85 (03) :339-344
[10]  
KENNEDY C, 1990, ARCH INT PHARMACOD T, V303, P30