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• W2160758064 abstract "Abstract: The β1 and β2-adrenoceptor populations in rat cortex were individually quantified by labelling all of the receptors with [3H]dihydroalprenolol and displacing with iso-prenaline (200 μM) or CGP 20712A (l-{2-[(3-carbamoyl-4-hydroxy)phenoxy]ethylamino}-3-[4-(l-methyl-4-trifluoro-methyl-2-imidazolyl)phenoxy]-2-propanol methanesul-phonate; 100 nM) to define total β-adrenoceptors and β1-adrenoceptors, respectively. Binding parameters for β2-adrenoceptors were calculated by the difference. Oral administration of the monoamine reuptake inhibitors sibutramine HC1 (3 mg/kg), amitriptyline (10 mg/kg), desipramine (10 mg/kg), or zimeldine (10 mg/kg) for 10 days decreased the total number of β-adrenoceptors present in rat cortex. This effect was entirely due to a reduction in the number of β1-adrenoceptors. Similarly, 10 days of treatment with the monoamine oxidase inhibitor tranylcypromine (10 mg/kg p.o.) or five electroconvulsive shocks (ECSs; 200 V, 2 s) spread over this period also down-regulated β-adrenoceptors by reducing the content of the βsubtype. By contrast, treatment with clenbuterol (5 mg/kg p.o.) for 10 days reduced the number of cortical β-adrenoceptors by an effect on the β2-adre-noceptor population. The effects of short-term treatment with these drugs were also investigated, and, using the doses shown above, the results of 3 days of administration or a single ECS were determined. Sibutramine HC1 and desipramine were alone in producing a reduction in number of β-adrenoceptors after 3 days. Once again, this was exclusively due to a loss of β1-adrenoceptors. Together, the results show that antidepressants with disparate pharmacological actions all down-regulated β-adrenoceptors through the neuronal β1-adrenoceptor subtype. In addition, sibutramine HC1 and desipramine produced this attenuation very rapidly. However, clenbuterol treatment reduced the number of β2-adrenoceptors, and its reported antidepressant activity is, therefore, unlikely to be mediated via this mechanism." @default.
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• W2160758064 date "1989-10-01" @default.
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• W2160758064 title "Antidepressant Treatments, Including Sibutramine Hydrochloride and Electroconvulsive Shock, Decrease ?1but Not ?2-Adrenoceptors in Rat Cortex" @default.
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• W2160758064 doi "https://doi.org/10.1111/j.1471-4159.1989.tb07389.x" @default.
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