Lister R G, Durcan M J, Nutt D J, Linnoila M
Laboratory of Clinical Studies, National Institute on Alcohol Abuse and Alcoholism, Bethesda, Maryland 20892.
Life Sci. 1989;44(2):111-9. doi: 10.1016/0024-3205(89)90528-6.
The interaction of a highly potent and selective alpha-2 adrenoceptor antagonist, atipamezole with ethanol was investigated in tests assessing a number of ethanol's behavioral effects. Atipamezole antagonized ethanol's effects on directed exploration in a holeboard test, reduced observer-rated intoxication and also reduced the duration of loss of righting reflex caused by ethanol. Similar effects were produced by another alpha-2 adrenoceptor antagonist idazoxan. The magnitude of the effects was comparable to that produced in the same animal models by the imidazodiazepine Ro 15-4513, which antagonizes ethanol by an action at central benzodiazepine receptors. Whereas Ro 15-4513 possesses marked behavioral effects on its own, atipamezole is comparatively inactive in all paradigms so far tested. The data suggest that alpha-2 adrenoceptors can play an important role in modulating the intoxicating effects of ethanol.
在评估乙醇多种行为效应的试验中，研究了强效选择性α-2肾上腺素能受体拮抗剂阿替美唑与乙醇的相互作用。阿替美唑在洞板试验中拮抗乙醇对定向探索的作用，降低观察者评定的醉酒程度，并缩短乙醇引起的翻正反射丧失持续时间。另一种α-2肾上腺素能受体拮抗剂伊达唑胺也产生了类似效应。这些效应的程度与咪唑二氮杂䓬Ro 15-4513在相同动物模型中产生的效应相当，Ro 15-4513通过作用于中枢苯二氮䓬受体拮抗乙醇。虽然Ro 15-4513自身具有显著的行为效应，但阿替美唑在迄今为止测试的所有范式中相对无活性。数据表明，α-2肾上腺素能受体在调节乙醇的中毒效应中可发挥重要作用。
