In vitro modulation of CNS beta-receptor number by antidepressants and beta-agonists.
In vitro incubation of rat cerebral cortex slices with antidepressant drugs reduced beta-adrenergic receptor binding of 3H-dihydroalprenolol by 30%. The decrease was maximum after 60 min, and was reversible after 120 min. (-)-Isoproterenol incubation caused a rapid and reversible loss (60%) of beta-receptor binding. Both effects were due to a decrease in beta-receptor sites. In vitro beta-receptor subsensitivity due to desipramine and isoproterenol was non-additive. The observed reversible loss of beta-receptor sites may be an initial phase of the beta-receptor down-regulation by antidepressants seen in vivo.
D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects*; D004082:Dihydroalprenolol / Q000378:metabolism; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D051381:Rats; D011941:Receptors, Adrenergic / Q000187:drug effects*; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D013997:Time Factors
D000318:Adrenergic beta-Agonists; D000928:Antidepressive Agents; D011941:Receptors, Adrenergic; D011943:Receptors, Adrenergic, beta; D004082:Dihydroalprenolol; D007545:Isoproterenol