Timár J, Knoll B
Arch Int Pharmacodyn Ther. 1986 Jan;279(1):50-60.
Phenylethylamine (PEA) in a dose of 40 mg/kg induces a moderate and short-lasting stereotype behaviour. The intensity and duration of PEA-induced stereotypy was strongly potentiated in rats with single selective doses of (-) deprenyl and J-508 (0.25 and 0.1 mg/kg s.c., respectively), which inhibit selectively the B form of MAO. Neither the increase of the single dose nor the daily administration of the selective doses of (-) deprenyl and J-508 for eight weeks caused a more intense or longer lasting potentiation of the PEA effect than single small dose of these drugs. Stopping administration of MAO-B inhibitors, normal sensitivity towards PEA returned after 3-4 weeks, in a parallel way with the recovery of MAO-B activity in the brain. Clorgyline, the selective inhibitor of MAO-A failed to influence the effect of PEA (0.25-2 mg/kg s.c.). The data support the view that the strong potentiation of the stimulatory effects of endogenous PEA via inhibition of its metabolism by (-) deprenyl may play a role in the antidepressant effect of this drug in man.
40毫克/千克剂量的苯乙胺(PEA)会诱发中度且持续时间较短的刻板行为。在单次给予选择性剂量的(-)司来吉兰和J - 508(分别为0.25毫克/千克和0.1毫克/千克皮下注射)的大鼠中,PEA诱发的刻板行为的强度和持续时间被显著增强,这两种药物分别选择性抑制单胺氧化酶(MAO)的B型。无论是单次剂量的增加,还是(-)司来吉兰和J - 508的选择性剂量连续八周每日给药,都不会比单次小剂量给药导致更强烈或更持久的PEA效应增强。停止给予MAO - B抑制剂后,对PEA的正常敏感性在3 - 4周后恢复,这与大脑中MAO - B活性的恢复呈平行关系。MAO - A的选择性抑制剂氯吉兰未能影响PEA的效应(0.25 - 2毫克/千克皮下注射)。这些数据支持这样一种观点,即通过(-)司来吉兰抑制内源性PEA的代谢,从而强烈增强其刺激作用,可能在该药物对人类的抗抑郁作用中发挥作用。