Novel alpha 2-adrenoceptor antagonists show selectivity for alpha 2A- and alpha 2B-adrenoceptor subtypes.
Pharmacological characterization of mammalian alpha 2-adrenoceptors in various tissues and species has provided evidence for the existence of two alpha 2-adrenoceptor subtypes. These subtypes can be defined in rat and human tissues by prazosin which is alpha 2B selective and oxymetazoline which is alpha 2A selective. In addition to these agents, two types of alpha 2-adrenoceptor antagonists are described which show high affinity and selectivity for the alpha 2A-adrenoceptor and the alpha 2B-adrenoceptor respectively.
Young
P
P
Beecham Pharmaceuticals Research Division, Epsom, Surrey, U.K.
Berge
J
J
Chapman
H
H
Cawthorne
M A
MA
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000818:Animals; D000831:Animals, Newborn; D001667:Binding, Competitive / Q000187:drug effects; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008168:Lung / Q000187:drug effects / Q000378:metabolism; D008297:Male; D010109:Oxymetazoline / Q000494:pharmacology; D011224:Prazosin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D015016:Yohimbine
D000317:Adrenergic alpha-Antagonists; D011942:Receptors, Adrenergic, alpha; D015016:Yohimbine; D010109:Oxymetazoline; D011224:Prazosin