Hara S, Satoh T, Kitagawa H
Res Commun Chem Pathol Pharmacol. 1981 Feb;31(2):251-7.
Pretreatment with hydralazine caused prolongation of hypnosis induced by hexobarbital (80 mg/kg, i.p.) or intracerebroventricular injection of phenobarbital (1 mg/rat). Under the same condition, brain concentration of hexobarbital was lower than that of no hydralazine treatment. In addition, no appreciable change in liver microsomal drug metabolizing enzyme activities of rats after hydralazine treatment was observed. These findings strongly suggested that hydralazine increases the sensitivity of brain to barbiturates, which leads to prolongation of sleeping time without inhibition of drug metabolizing enzymes.
用肼苯哒嗪预处理可使由己巴比妥(80毫克/千克,腹腔注射)或脑室内注射苯巴比妥(1毫克/大鼠)诱导的催眠时间延长。在相同条件下,己巴比妥的脑内浓度低于未用肼苯哒嗪处理的情况。此外,未观察到肼苯哒嗪处理后大鼠肝脏微粒体药物代谢酶活性有明显变化。这些发现有力地表明,肼苯哒嗪增加了脑对巴比妥类药物的敏感性,从而导致睡眠时间延长,而不抑制药物代谢酶。