Durcan M J, Lister R G, Linnoila M
Laboratory of Clinical Studies, National Institute on Alcohol Abuse and Alcoholism, Bethesda, Maryland 20892.
Neuropharmacology. 1989 Mar;28(3):275-81. doi: 10.1016/0028-3908(89)90104-4.
The effects of two selective alpha 2-adrenoceptor agonists (clonidine and medetomidine) and antagonists (atipamezole and idazoxan) were examined in the holeboard test. The interactions of the two antagonists with ethanol were also investigated. Atipamezole (0.1-3.0 mg/kg) and idazoxan (0.01-0.3 mg/kg) were without effect on either directed exploration or locomotor activity in the holeboard test, whereas clonidine (0.003-0.1 mg/kg) and medetomedine (0.003-0.1 mg/kg) were sedative. Atipamezole (1-3 mg/kg) and idazoxan (0.3-1.0 mg/kg) reversed the behavioral effects of 0.1 mg/kg of medetomidine. When administered with ethanol (2 g/kg), atipamezole (1-3 mg/kg) showed a significant antagonism of the ethanol-induced reduction in exploratory head-dipping: no change in the locomotor stimulant properties of ethanol was seen. A similar trend was seen for exploration after a combination of idazoxan (1-3 mg/kg) with 2 g/kg ethanol; however, the 3 mg/kg dose attenuated the locomotor stimulant effect. Both antagonists caused a dose-related reduction in the increase in head-dipping seen after administration of 1 g/kg of ethanol, without any effect on the locomotor stimulant effect of this dose. These results suggest mediation of alpha 2-adrenoceptors in some of the behavioral effects of ethanol.
在空板试验中研究了两种选择性α2 -肾上腺素能受体激动剂（可乐定和美托咪定）及拮抗剂（阿替美唑和咪唑克生）的作用。还研究了这两种拮抗剂与乙醇之间的相互作用。在空板试验中，阿替美唑（0.1 - 3.0毫克/千克）和咪唑克生（0.01 - 0.3毫克/千克）对定向探索或运动活动均无影响，而可乐定（0.003 - 0.1毫克/千克）和美托咪定（0.003 - 0.1毫克/千克）具有镇静作用。阿替美唑（1 - 3毫克/千克）和咪唑克生（0.3 - 1.0毫克/千克）可逆转0.1毫克/千克美托咪定的行为效应。当与乙醇（2克/千克）合用时，阿替美唑（1 - 3毫克/千克）对乙醇诱导的探索性头部浸入减少具有显著拮抗作用：未观察到乙醇的运动兴奋特性发生变化。咪唑克生（1 - 3毫克/千克）与2克/千克乙醇合用后探索方面也出现类似趋势；然而，3毫克/千克剂量减弱了运动兴奋效应。两种拮抗剂均使1克/千克乙醇给药后头部浸入增加量呈剂量依赖性减少，而对该剂量的运动兴奋效应无任何影响。这些结果表明α2 -肾上腺素能受体参与了乙醇某些行为效应的介导过程。
