Ribeiro C A, Macedo T A
J Pharm Pharmacol. 1986 Aug;38(8):600-5. doi: 10.1111/j.2042-7158.1986.tb03088.x.
Prazosin and yohimbine were used to differentiate postjunctional alpha-adrenoceptors in the human uterine artery in-vitro. Two postjunctional alpha-adrenoceptor subtypes were distinguished by the affinities of the receptor for yohimbine and prazosin. The pA2 for prazosin was 8.91 against phenylephrine with a slope not significantly different from unity (0.91), and the pA2 for yohimbine was 7.25 against naphazoline and 8.70 against clonidine, with slopes not significantly different from unity (1.11 and 1.18, respectively). Yohimbine was not very active against phenylephrine, while prazosin was very active against the mixed and selective alpha 2-adrenoceptor agonist noradrenaline and clonidine; the intercepts of the Schild plot were 8.80 and 8.82 but with slopes significantly less than unity (0.77 and 0.67, respectively). Prazosin competitively antagonized phenylephrine at the alpha 1-adrenoceptor, whereas yohimbine competitively antagonized naphazoline and clonidine at the alpha 2-adrenoceptor. It is concluded that both alpha 1- and alpha 2-adrenoceptors are present in the human uterine artery.
哌唑嗪和育亨宾被用于在体外区分人子宫动脉中的节后α-肾上腺素能受体。通过受体对育亨宾和哌唑嗪的亲和力区分出两种节后α-肾上腺素能受体亚型。哌唑嗪对去氧肾上腺素的pA2为8.91,斜率与1无显著差异(0.91),育亨宾对萘甲唑啉的pA2为7.25,对可乐定的pA2为8.70,斜率与1无显著差异(分别为1.11和1.18)。育亨宾对去氧肾上腺素的活性不强,而哌唑嗪对混合性和选择性α2-肾上腺素能激动剂去甲肾上腺素和可乐定的活性很强;Schild图的截距分别为8.80和8.82,但斜率显著小于1(分别为0.77和0.67)。哌唑嗪在α1-肾上腺素能受体处竞争性拮抗去氧肾上腺素,而育亨宾在α2-肾上腺素能受体处竞争性拮抗萘甲唑啉和可乐定。结论是人子宫动脉中同时存在α1和α2肾上腺素能受体。