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PubMed · 38911

Studies on the structure-activity relationships of adrenergic beta-mimetic benzylamine derivatives. V. 9-Aryl-1H-2,3,7,8,9,10-hexahydrobenzo[d,e]quinolines.

S Yamamura·K Oda·T Mizoguchi·S Saito·Y Iwasawa·A Kiyomoto
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Adrenergic beta-AgonistsAminesAnimalsBenzylaminesChemical PhenomenaChemistryIn Vitro TechniquesMiceQuinolinesStructure-Activity RelationshipJournal Article

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S Yamamura, K Oda, T Mizoguchi, S Saito, Y Iwasawa, A Kiyomoto. 1979. Studies on the structure-activity relationships of adrenergic beta-mimetic benzylamine derivatives. V. 9-Aryl-1H-2,3,7,8,9,10-hexahydrobenzo[d,e]quinolines.. https://doi.org/10.1248/cpb.27.858

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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.

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