Comparison of central and peripheral alpha 1-adrenoceptors.
A series of alpha-adrenergic agonists and antagonists having diverse chemical structure was examined for both central and peripheral alpha 1-adrenoceptor activity. The agonists tested included several novel aminotetralin derivatives which were potent and selective alpha 1-agonists. Peripheral alpha 1-activity was determined in the isolated rabbit ear artery; central alpha 1-receptor affinity was measured as the ability to inhibit 3H-WB 4101 binding to rat brain homogenates. In the agonist series, an excellent correlation between peripheral alpha 1-activity and central alpha 1-affinity was obtained, providing that partial agonists were excluded. Likewise, the receptor dissociation constant for blockade of the peripheral alpha 1-adrenoceptor correlated well with affinity for the central receptor for all of the alpha-antagonists. These data support the conclusion that central and peripheral alpha 1-adrenoceptors are similar or identical.
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D000818:Animals; D001158:Arteries / Q000187:drug effects; D002540:Cerebral Cortex / Q000187:drug effects; D003000:Clonidine / Q000494:pharmacology; D004146:Dioxanes / Q000378:metabolism; D004423:Ear / Q000098:blood supply; D066298:In Vitro Techniques; D008297:Male; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011941:Receptors, Adrenergic / Q000187:drug effects*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D011954:Receptors, Dopamine / Q000187:drug effects; D013329:Structure-Activity Relationship
D000316:Adrenergic alpha-Agonists; D004146:Dioxanes; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D011954:Receptors, Dopamine; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane; D003000:Clonidine