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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Oral versus transdermal selegiline: antidepressant-like activity in rats.
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Oral versus transdermal selegiline: antidepressant-like activity in rats.

机译：口服与经皮司来吉兰对比：大鼠抗抑郁样活性。

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These studies compared the dose-response effects of oral vs. transdermal selegiline on antidepressant-like activity and brain monoamine oxidase (MAO) activities in rats. Rats received selegiline by gavage (0-100 mg/kg) or via transdermal patches (0-4.8 cm2, 0-8.7 mg/kg) daily for 7 days; antidepressant-like activity was determined using the forced-swim test. Following behavioral testing, cerebral cortices were assayed for MAO-A and MAO-B activities. Doses of selegiline that selectively inhibited MAO-B (3 and 10 mg/kg/day by gavage and 0.4 mg/kg/day via patch) did not alter either immobility or latency time. However, the oral administration of 30 or 100 mg/kg/day or the transdermal administration of 8.7 mg/kg/day, doses that led to greater than 70% inhibition of MAO-A, decreased immobility time significantly. The IC50s for inhibition of MAO-A following oral and transdermal administration for 7 days were 19.8 and 1.1 mg/kg, respectively. Results indicate that both oral and transdermal selegiline have antidepressant-like activity as assessed by the forced-swim test, and that transdermal administration, which bypasses first-pass metabolism, allows for using lower doses than oral administration.
机译：这些研究比较了口服与经皮司来吉兰对大鼠抗抑郁样活性和脑单胺氧化酶（MAO）活性的剂量反应作用。大鼠每天通过管饲法（0-100 mg / kg）或经皮贴剂（0-4.8 cm2，0-8.7 mg / kg）接受司来吉兰治疗7天;使用强迫游泳试验确定抗抑郁样活性。进行行为测试后，测定大脑皮层的MAO-A和MAO-B活性。选择性抑制MAO-B的司来吉兰剂量（管饲法分别为3和10 mg / kg /天，经贴剂为0.4 mg / kg /天）不会改变固定性或潜伏时间。但是，口服剂量为30或100 mg / kg /天或经皮给药的8.7 mg / kg /天，导致对MAO-A的抑制作用大于70％，因此显着减少了固定时间。口服和经皮给药7天后抑制MAO-A的IC50分别为19.8和1.1 mg / kg。结果表明，口服和经皮司来吉兰均具有通过强迫游泳试验评估的抗抑郁样活性，并且绕过首过代谢的经皮给药允许使用比口服给药更低的剂量。

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