Pharmacological characterization of the postsynaptic alpha-adrenoceptors in human uterine artery.
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.
D001158:Arteries / Q000378:metabolism*; D003000:Clonidine / Q000494:pharmacology; D004347:Drug Interactions; D005260:Female; D006801:Humans; D007700:Kinetics; D009278:Naphazoline / Q000494:pharmacology; D009638:Norepinephrine / Q000494:pharmacology; D010656:Phenylephrine / Q000494:pharmacology; D011224:Prazosin / Q000494:pharmacology; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism*; D014599:Uterus / Q000098:blood supply*; D014661:Vasoconstriction / Q000187:drug effects; D015016:Yohimbine / Q000494:pharmacology
D011942:Receptors, Adrenergic, alpha; D010656:Phenylephrine; D015016:Yohimbine; D009278:Naphazoline; D003000:Clonidine; D009638:Norepinephrine; D011224:Prazosin