Characterization of alpha-adrenergic receptors in guinea pig cerebral cortex: effect of chronic antidepressant treatments.
Alpha-adrenergic receptor sites in cerebral cortex membranes of the guinea pig have been characterized by the specific binding of 3H-WB4101, an alpha-adrenergic antagonist. The binding was rapid, reversible, saturable, and stereoselective. The maximal binding site (Bmax) and dissociation constant (kd) for 3H-WB4101 were calculated to be 251 fmol/mg protein and 1.23 nM, respectively. Ligand displacement experiments suggest that 3H-WB4101 binds to alpha 1-adrenergic receptors. Chronic treatment of guinea pigs with desipramine, amitriptyline, phenelzine, or electroconvulsive shock failed to show any statistically significant change in alpha-adrenergic receptor sensitivity as measured by the binding of 3H-WB4101.
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000187:drug effects*; D004146:Dioxanes; D006168:Guinea Pigs; D008297:Male; D011941:Receptors, Adrenergic / Q000187:drug effects*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*
D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D000928:Antidepressive Agents; D004146:Dioxanes; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane