Agrawal D K, Triggle C R, Daniel E E
J Pharmacol Exp Ther. 1984 Jun;229(3):831-8.
Postsynaptic alpha adrenoceptors have been characterized in rat superior mesenteric artery and branches of canine mesenteric artery. l-Phenylephrine, naphazoline and clonidine were used as agonists and prazosin and yohimbine were used as antagonists. The pA2 values for prazosin and yohimbine were determined against these agonists in canine and rat mesenteric arteries. The pA2 values for either prazosin or yohimbine were similar when l-phenylephrine and naphazoline were used as the agonists. The slope of the Schild plot was less than unity for prazosin and yohimbine acting as antagonists to l-phenylephrine in canine mesenteric artery whereas in the rat mesenteric artery, the slopes obtained for either phenylephrine or naphazoline against the antagonists were not significantly different from unity. In rat mesenteric artery, the pA2 value for yohimbine against clonidine was not statistically different from values obtained with the other agonists; however, in the presence of prazosin the dose-response curve to clonidine was biphasic, suggesting that the action of clonidine is mediated through two distinct sites to which prazosin has different affinities. However, these results do not provide definitive support for the concept of functionally independent subtypes of postsynaptic alpha adrenoceptors in rat and canine mesenteric artery.
突触后α肾上腺素能受体已在大鼠肠系膜上动脉和犬肠系膜动脉分支中得到表征。使用去氧肾上腺素、萘甲唑啉和可乐定作为激动剂,哌唑嗪和育亨宾作为拮抗剂。在犬和大鼠肠系膜动脉中,针对这些激动剂测定了哌唑嗪和育亨宾的pA2值。当使用去氧肾上腺素和萘甲唑啉作为激动剂时,哌唑嗪或育亨宾的pA2值相似。在犬肠系膜动脉中,当哌唑嗪和育亨宾作为去氧肾上腺素的拮抗剂时,Schild图的斜率小于1,而在大鼠肠系膜动脉中,去氧肾上腺素或萘甲唑啉针对拮抗剂获得的斜率与1无显著差异。在大鼠肠系膜动脉中,育亨宾针对可乐定的pA2值与用其他激动剂获得的值无统计学差异;然而,在存在哌唑嗪的情况下,对可乐定的剂量反应曲线是双相的,这表明可乐定的作用是通过两个不同的位点介导的,哌唑嗪对这两个位点具有不同的亲和力。然而,这些结果并未为大鼠和犬肠系膜动脉中突触后α肾上腺素能受体功能独立亚型的概念提供确凿支持。