Hollingsworth P J, Smith C B
Department of Pharmacology, University of Michigan Medical School, Ann Arbor 48109.
Eur J Pharmacol. 1989 Sep 13;168(2):159-67. doi: 10.1016/0014-2999(89)90561-x.
The specific binding of [3H]clonidine to alpha 2-adrenoceptors on neural membranes isolated from six brain areas was determined with rats treated for various periods of time with the muscarinic agonists, oxotremorine or pilocarpine, or with the muscarinic antagonists atropine, atropine methyl nitrate, scopolamine and scopolamine methyl bromide. Administration of pilocarpine, 10 mg/kg, twice daily i.p. for 1 and 14 days increased markedly the number of alpha 2-adrenoceptors on neural membranes from all six brain areas. In contrast, oxotremorine, 0.3 mg/kg, twice daily i.p., for 7 days decreased the number of alpha 2-adrenoceptors on membranes from all brain areas except the brainstem and caudate nucleus. Both atropine and scopolamine increased the density of alpha 2-adrenoceptors in specific brain areas. Neither atropine methyl nitrate nor scopolamine methyl bromide had an appreciable effect upon the specific binding of [3H]clonidine to neural membranes from most brain areas.
用毒蕈碱激动剂氧化震颤素或毛果芸香碱,或用毒蕈碱拮抗剂阿托品、硝酸甲基阿托品、东莨菪碱和溴甲东莨菪碱对大鼠进行不同时间段的处理,然后测定[3H]可乐定与从六个脑区分离出的神经膜上α2 -肾上腺素能受体的特异性结合。每天腹腔注射10 mg/kg毛果芸香碱,连续1天和14天,显著增加了所有六个脑区神经膜上α2 -肾上腺素能受体的数量。相比之下,每天腹腔注射0.3 mg/kg氧化震颤素,连续7天,除脑干和尾状核外,所有脑区膜上α2 -肾上腺素能受体的数量均减少。阿托品和东莨菪碱均增加了特定脑区α2 -肾上腺素能受体的密度。硝酸甲基阿托品和溴甲东莨菪碱对大多数脑区神经膜上[3H]可乐定的特异性结合均无明显影响。