alpha 1/alpha 2 Selectivity ratio in a series of agonists and their relation to pre/postsynaptic activity ratios.
beta-Blocked pithed rats were used to obtained dose-response curves (blood-pressure increase) for 13 various alpha-adrenoceptor agonists of clinical and theoretical interest, in the absence and in the presence of the selective antagonists rauwolscine (alpha 2) and prazosin (alpha 1). Antagonist doses which shifted the dose-response curves for an agonist 10-fold to the right along the abscissa were then calculated (D10rauwolscine = D10R; D10prazosin = D10P). The ratio D10R/D10P is considered to be a quantitative estimation of an agonist's alpha 1/alpha 2 selectivity ratio. A correlation with post/presynaptic activity ratios is presented.
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D008297:Male; D011224:Prazosin / Q000494:pharmacology; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000145:classification / Q000187:drug effects*; D013569:Synapses; D015016:Yohimbine / Q000494:pharmacology
D000316:Adrenergic alpha-Agonists; D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine; D011224:Prazosin