Menon M K, Kodama C K
Life Sci. 1985 Dec 2;37(22):2091-8. doi: 10.1016/0024-3205(85)90581-8.
A lipid soluble alpha 1-adrenoceptor agonist 2-(2-chloro-5-trifluoromethyl phenylimino) imidazolidine (St 587) dose-dependently antagonized the hypnotic, hypothermic and respiratory depressant effects of ethanol in C57B1/6 mice. This effect was present whether St 587 was given before or after ethanol. St 587 did not block the pentobarbitone-induced hypnosis. It also did not influence the elimination of ethanol. Combined treatment with a subhypnotic dose of ethanol and St 587 resulted in marked hyperactivity in mice. This effect was completely abolished by pimozide pretreatment. It was inferred that the dopamine released from brain areas by this dose of ethanol together with the norepinephrine receptor activation offered by St 587 resulted in this hyperactivity. Cirazoline, a more potent alpha 1-adrenoceptor agonist than St 587 was relatively more effective than the latter in blocking the ethanol-induced hypnosis in mice. It seems that alpha 1-adrenoceptor stimulation is a major contributing factor to the ethanol antagonism exerted by St 587. This drug might prove to be useful in the treatment of acute ethanol intoxication and in understanding the mode of action of ethanol.
一种脂溶性α1 - 肾上腺素能受体激动剂2 - (2 - 氯 - 5 - 三氟甲基苯基亚氨基)咪唑烷(St 587)能剂量依赖性地拮抗乙醇对C57B1/6小鼠的催眠、体温降低及呼吸抑制作用。无论St 587在乙醇之前还是之后给药，这种作用均存在。St 587不阻断戊巴比妥钠诱导的催眠作用。它也不影响乙醇的消除。用亚催眠剂量的乙醇和St 587联合处理可导致小鼠明显的多动。匹莫齐特预处理可完全消除这种作用。据推测，该剂量的乙醇从脑区释放的多巴胺与St 587提供的去甲肾上腺素受体激活共同导致了这种多动。西拉唑啉是一种比St 587更强效的α1 - 肾上腺素能受体激动剂，在阻断小鼠乙醇诱导的催眠作用方面比后者相对更有效。似乎α1 - 肾上腺素能受体刺激是St 587发挥乙醇拮抗作用的主要因素。这种药物可能在治疗急性乙醇中毒及理解乙醇的作用方式方面被证明是有用的。
