Melzacka M, Janczar L, Nocon H
Department of Pharmacokinetics and Drug Metabolism, Polish Academy of Sciences, Krakow.
Biochem Pharmacol. 1993 Aug 3;46(3):449-53. doi: 10.1016/0006-2952(93)90521-w.
This study investigates the effect of imipramine (IMI) on the methylation of phosphatidylethanolamine (PE) in crude cortical membranes of rat brain in vitro and ex vivo. It was found that IMI enhanced the formation of phosphatidyl-N-monomethylethanolamine (PME) and phosphatidyl-N,N-dimethylethanolamine (PDE) and inhibited the formation of phosphatidylcholine (PC) in the cortical membranes of rats in vitro. The same effect i.e. increased incorporation of methyl groups in PE and PME and decreased formation of PC was found in the cortical membrane of rats killed 1 hr after intraperitoneal administration of IMI at a single dose of 10 mg/kg. Chronic treatment of rats with IMI for 14 days with a daily dose of 10 mg/kg i.p. led to further inhibition of PC formation but did not affect the formation of PME and PDE and abolished the stimulating effect of IMI on the formation of PME and PDE in vitro.
本研究调查了丙咪嗪（IMI）在体外和体内对大鼠脑粗皮质膜中磷脂酰乙醇胺（PE）甲基化的影响。研究发现，在体外，IMI增强了磷脂酰 - N - 单甲基乙醇胺（PME）和磷脂酰 - N，N - 二甲基乙醇胺（PDE）的形成，并抑制了大鼠皮质膜中磷脂酰胆碱（PC）的形成。在腹腔注射单剂量10mg/kg IMI 1小时后处死的大鼠皮质膜中，发现了相同的效果，即PE和PME中甲基掺入增加，PC形成减少。以每日10mg/kg腹腔注射的剂量对大鼠进行14天的IMI慢性治疗，导致PC形成进一步受到抑制，但不影响PME和PDE的形成，并且消除了IMI在体外对PME和PDE形成的刺激作用。
