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氯吉兰和帕吉林在人体内作为单胺氧化酶A和B抑制剂的体内选择性。

Selectivity of clorgyline and pargyline as inhibitors of monoamine oxidases A and B in vivo in man.

作者信息

Murphy D L, Lipper S, Slater S, Shiling D

出版信息

Psychopharmacology (Berl). 1979 Apr 11;62(2):129-32. doi: 10.1007/BF00427125.

Abstract

During 4 weeks of treatment with clorgyline, a selective MAO-A inhibitor, platelet monoamine oxidase (MAO) activity was unchanged. During a similar 4-week crossover treatment period with pargyline, a selective MAO-B inhibitor, platelet MAO activity was essentially completely inhibited in the same individuals. The differential effects of the two drugs on platelet MAO, which consists exclusively of the MAO-B form, suggests that the in vitro selectivity of clorgyline, and possibly of pargyline, on MAO-A and MAO-B may be maintained in vivo during long-term administration in man. Reductions in blood pressure, heart rate, and plasma amine oxidase activity were generally similar in magnitude during treatment with both drugs, however, suggesting that either these effects are nonspecific consequences of both MAO-A and MAO-B inhibition, or that pargyline also inhibited MAO-A activity.

摘要

在使用选择性单胺氧化酶-A(MAO-A)抑制剂氯吉兰治疗的4周期间,血小板单胺氧化酶(MAO)活性未发生变化。在使用选择性单胺氧化酶-B(MAO-B)抑制剂帕吉林进行的为期4周的类似交叉治疗期间,相同个体的血小板MAO活性基本被完全抑制。这两种药物对仅由MAO-B形式组成的血小板MAO的不同作用表明,氯吉兰以及可能还有帕吉林对MAO-A和MAO-B的体外选择性在人体长期给药期间可能在体内得以维持。然而,在两种药物治疗期间,血压、心率和血浆胺氧化酶活性的降低幅度通常相似,这表明要么这些作用是MAO-A和MAO-B抑制的非特异性后果,要么帕吉林也抑制了MAO-A活性。

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