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5-羟色胺和β-苯乙胺在灌注大鼠肺及体外的代谢

The metabolism of 5-hydroxytryptamine and beta-phenylethylamine in perfused rat lung and in vitro.

作者信息

Bakhle Y S, Youdim M B

出版信息

Br J Pharmacol. 1979 Jan;65(1):147-54. doi: 10.1111/j.1476-5381.1979.tb17343.x.

Abstract

1 Metabolism of 5-hydroxytryptamine (5-HT) and beta-phenylethylamine (PHE) by monoamine oxidase (MAO) was investigated in rat isolated lungs and in mitochondrial preparations from rat lung. 2. In perfused lungs 5-HT metabolism had an apparent Km of 2 microgram and PHE metaoblism a Km of 54 microgram, whereas in vitro the Km values were 330 microgram and 28 microgram respectively. 3 In vitro, MAO activity had substrate and inhibitor specificities compatible with the presence of A and B types of MAO. 4 In perfused lung, metabolism of 5-HT but not that of PHE was inhibited by desmethylimipramine. 5 These results show that PHE metabolism in perfused lung, unlike that of other metabolized amines, is not limited by transport and the transport process for PHE is unlike that of 5-HT or noradrenaline. 6 These results also show that the kinetic parameters obtained for MAO activity in vitro do not generally apply to the isolated lung where transport of substrate can be the deciding factor. This discrepancy emphasizes that the enzymic properties of the whole organ cannot relaibly be deduced from its enzymic content.

摘要
  1. 在大鼠离体肺脏和大鼠肺脏的线粒体制剂中研究了单胺氧化酶(MAO)对5-羟色胺(5-HT)和β-苯乙胺(PHE)的代谢作用。2. 在灌注肺中,5-HT代谢的表观Km为2微克,PHE代谢的Km为54微克,而在体外,Km值分别为330微克和28微克。3. 在体外,MAO活性具有与A和B型MAO存在相符的底物和抑制剂特异性。4. 在灌注肺中,5-HT的代谢受到去甲丙咪嗪的抑制,但PHE的代谢未受抑制。5. 这些结果表明,灌注肺中PHE的代谢与其他代谢胺类不同,不受转运限制,且PHE的转运过程与5-HT或去甲肾上腺素的不同。6. 这些结果还表明,体外获得的MAO活性动力学参数通常不适用于离体肺,在离体肺中底物转运可能是决定性因素。这种差异强调了不能从整个器官的酶含量可靠地推断其酶学性质。

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