Postjunctional alpha-adrenoceptors in human superficial epigastric arteries and veins.
A pharmacological characterization of the postjunctional alpha-adrenoceptors in human superficial epigastric artery and vein was performed, using several alpha-adrenoceptor subtype selective agonists, and the antagonists prazosin (alpha 1) and rauwolscine (alpha 2). In the arteries prazosin fulfilled the criteria for a competitive antagonism in concentrations 10(-9)-10(-7) M, giving a pA2-value of 9.17 in the Schild plot. Rauwolscine in concentrations 10(-8)-10(-6) M caused less pronounced but significant dextral shifts of the noradrenaline (NA) concentration-response curves. In the veins rauwolscine behaved like a competitive antagonist (10(-8)-10(-7) M). The pA2-value was 9.16. Prazosin 10(-9) M displaced the NA concentration-response curve, but higher concentrations (10(-8) and 10(-7) M) caused no further displacement. Prazosin reduced the Emax-values in the veins. In the arteries the rank order of potency for the agonists was: cirazoline (alpha 1) greater than NA greater than naphazoline (alpha 2) greater than guanfacine (alpha 2) greater than phenylephrine (alpha 1). The intrinsic activities of clonidine (alpha 2), ST 587 (alpha 1), B-HT 920 (alpha 2) and B-HT 933 (alpha 2) were too low to allow meaningful comparisons to be made. The rank order of potency in the veins was: NA greater than clonidine (alpha 2) greater than naphazoline (alpha 2) greater than guanfacine (alpha 2) greater than phenylephrine (alpha 1) greater than B-HT 920 (alpha 2) greater than cirazoline (alpha 1) greater than B-HT 933 (alpha 2). The intrinsic activity of ST 587 was low.(ABSTRACT TRUNCATED AT 250 WORDS)
D000293:Adolescent; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D000328:Adult; D000368:Aged; D001158:Arteries / Q000187:drug effects / Q000378:metabolism; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008875:Middle Aged; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000378:metabolism*; D009638:Norepinephrine / Q000494:pharmacology; D011188:Potassium / Q000494:pharmacology; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism*; D014680:Veins / Q000187:drug effects / Q000378:metabolism
D000316:Adrenergic alpha-Agonists; D011942:Receptors, Adrenergic, alpha; D011188:Potassium; D009638:Norepinephrine