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Independent regulation of β 1 ‐ and β 2 ‐adrenoceptors
Author(s) -
Beer Margaret,
Hacker Stephen,
Poat Judith,
Stahl Stephen M.
Publication year - 1987
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1987.tb11387.x
Subject(s) - desipramine , agonist , clenbuterol , mianserin , medicine , endocrinology , pindolol , antagonist , chemistry , alpha 2 adrenergic receptor , antidepressant , pharmacology , receptor , serotonin , hippocampus
1 The down‐regulation of β‐adrenoceptors has been postulated as a biochemical marker of antidepressant efficacy. Here we demonstrate that chronic treatment with desipramine down‐regulates β 1 ‐adrenoceptors in rat cerebral cortex and that β‐adrenoceptor subtypes can be independently regulated by treatment with different β‐adrenoceptor agonists. 2 Desipramine, (±)‐clenbuterol, prenalterol, corwin (20 mg kg −1 daily) and corwin (10 mg kg −1 daily) were administered to male, Sprague‐Dawley rats, over eight days, by means of osmotic Alzet pumps placed subcutaneously and removed 24 h before analysis. Control rats received vehicle only. The β 1 ‐ and β 2 ‐adrenoceptor populations were measured in cerebral cortex by a modified (–)‐[ 125 I]‐pindolol receptor binding assay. 3 The conventional antidepressant, desipramine, preferentially down‐regulated β 1 ‐adrenoceptors whereas the non‐selective β‐adrenoceptor agonist (±)‐clenbuterol preferentially down‐regulated β 2 ‐adrenoceptors. The β 1 ‐selective partial agonist, prenalterol, up‐regulated β 1 ‐adrenoceptors perhaps acting more as an antagonist than as an agonist. Finally, neither dose of corwin had any significant effect on β‐adrenoceptor number.