Alpha-adrenoceptor antagonism by apoyohimbine and some observations on the pharmacology of alpha-adrenoceptors in the rat anococcygeus and vas deferens.
alpha-Adrenoceptor antagonism of several test drugs was assessed against adrenergic contractile responses to field stimulation in rat vas deferens and anococcygeus, the prejunctional inhibitory effect of xylazine in vas deferens and the contractile effects of alpha-adrenoceptor agonists in anococcygeus. Against the adrenergic nerve-induced contraction in vas deferens, the potency series was WB 4101 greater than prazosin greater than apoyohimbine greater than corynanthine greater than yohimbine greater than rauwolscine. Against the inhibitory effect of xylazine in vas deferens the potency series was apoyohimbine greater than rauwolscine = yohimbine greater than WB 4101 much greater than prazosin and corynanthine. In anococcygeus, against the contractile responses to adrenergic nerve stimulation or to the agonists amidephrine, noradrenaline and xylazine, the potency series was apoyohimbine greater than corynanthine greater than rauwolscine. These results show that apoyohimbine is more potent than the yohimbine sterioisomers as an antagonist at alpha 1- and alpha 2-adrenoceptors but is not more selective. The assay methods employed confirm the current classification of 'alpha'-receptors and drugs.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D003000:Clonidine / Q000031:analogs & derivatives / Q000494:pharmacology; D003042:Cocaine / Q000494:pharmacology; D004558:Electric Stimulation; D004983:Ethanolamines / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects*; D009638:Norepinephrine / Q000502:physiology; D051381:Rats; D011919:Rats, Inbred Strains; D014649:Vas Deferens / Q000187:drug effects / Q000294:innervation; D014991:Xylazine / Q000494:pharmacology; D015016:Yohimbine / Q000031:analogs & derivatives* / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D004983:Ethanolamines; C042187:apoyohimbine; D014991:Xylazine; D015016:Yohimbine; C016980:amidephrine; D003042:Cocaine; D003000:Clonidine; C034204:indanidine; D009638:Norepinephrine