Digges K G, Summers R J
Br J Pharmacol. 1983 Jul;79(3):655-65. doi: 10.1111/j.1476-5381.1983.tb10002.x.
Postsynaptic alpha-adrenoceptors in rat isolated aortic strips and portal veins have been examined using a number of agonist and antagonist drugs which have varying selectivity for alpha 1- and alpha 2-adrenoceptors. In both tissues (-)-noradrenaline [-)-NA), (-)-adrenaline [-) Adr) (-)-alpha-methyl noradrenaline [-)-alpha-Me-NA) and (-)-phenylephrine [-)-PE) were full agonists, while clonidine, oxymetazoline and (2-(2,6-dichlorophenyl)-5,6-dihydroimidazo(2,1,b) thiazole (44,549) were partial agonists. Guanfacine was a full agonist in aortic strips but only a partial agonist in portal veins. In aortic strips, pA2 values for prazosin and yohimbine were not significantly different using (-)-NA, (-)-PE or guanfacine as the agonist, suggesting a single population of alpha-adrenoceptors. The order of potency of the antagonists, prazosin = 2-(beta-(4-hydroxyphenyl)-ethylaminomethyl)-tetralone (BE2254) greater than phentolamine greater than yohimbine greater than rauwolscine, is indicative of an alpha 1-type of receptor. In portal veins, the order of potency of the antagonists was prazosin greater than BE2254 greater than phentolamine greater than yohimbine greater than rauwolscine, again indicating an alpha 1-type of receptor. The mean pA2 value for yohimbine was not significantly different in either tissue. However, mean pA2 values for prazosin, BE-2254 and phentolamine were approximately one order of magnitude lower in portal veins than in aortic strips, suggesting that the receptors in the two tissues may not be identical.
利用多种对α1和α2肾上腺素能受体具有不同选择性的激动剂和拮抗剂药物,对大鼠离体主动脉条和门静脉中的突触后α-肾上腺素能受体进行了研究。在这两种组织中,(-)-去甲肾上腺素[(-)-NA]、(-)-肾上腺素[(-)-Adr]、(-)-α-甲基去甲肾上腺素[(-)-α-Me-NA]和(-)-去氧肾上腺素[(-)-PE]是完全激动剂,而可乐定、羟甲唑啉和(2-(2,6-二氯苯基)-5,6-二氢咪唑并[2,1,b]噻唑(44,549)是部分激动剂。胍法辛在主动脉条中是完全激动剂,但在门静脉中只是部分激动剂。在主动脉条中,以(-)-NA、(-)-PE或胍法辛为激动剂时,哌唑嗪和育亨宾的pA2值无显著差异,提示存在单一群体的α-肾上腺素能受体。拮抗剂的效能顺序为哌唑嗪 = 2-(β-(4-羟基苯基)-乙胺甲基)-四氢萘酮(BE2254)>酚妥拉明>育亨宾>萝芙木碱,表明是α1型受体。在门静脉中,拮抗剂的效能顺序为哌唑嗪>BE2254>酚妥拉明>育亨宾>萝芙木碱,同样表明是α1型受体。育亨宾的平均pA2值在两种组织中无显著差异。然而,哌唑嗪、BE-2254和酚妥拉明的平均pA2值在门静脉中比在主动脉条中约低一个数量级,提示两种组织中的受体可能不相同。