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大鼠中前列环素的代谢

Metabolism of prostacyclin in rat.

作者信息

Sun F F, Taylor B M

出版信息

Biochemistry. 1978 Sep 19;17(19):4096-101. doi: 10.1021/bi00612a035.

Abstract

Following a single intravenous administration of [11-3H]prostacyclin in rat, 77% of the administered dose was excreted within 3 days with 33% in urine and 44% in feces. Urinary metabolites were accumulated by chronic intravenous infusions of [11-3H]prostacyclin for 14 days. The drug was extensively metabolized and the structures of seven metabolites were elucidated by combined gas chromatography and mass spectrometry. The urinary products include the dinor and 19-hydroxy dinor derivatives of 6-keto-PGF1alpha and 13,14-dihydro-6,15-diketo-PGF1alpha, omega-hydroxy and omega-carboxyl dinor derivates of dihydro-6,15-diketo-PGF1alpha, and a dihydrodiketotetranordicarboxylic acid. The metabolic pathways of PGI2 in rat are similar to that of PGF2alpha.

摘要

给大鼠单次静脉注射[11-³H]前列环素后,77%的给药剂量在3天内排出,其中33%经尿液排出,44%经粪便排出。通过慢性静脉输注[11-³H]前列环素14天来积累尿液代谢产物。该药物被广泛代谢,通过气相色谱和质谱联用阐明了七种代谢产物的结构。尿液产物包括6-酮-PGF1α的双降和19-羟基双降衍生物、13,14-二氢-6,15-二酮-PGF1α、二氢-6,15-二酮-PGF1α的ω-羟基和ω-羧基双降衍生物,以及一种二氢二酮四降二羧酸。大鼠体内PGI2的代谢途径与PGF2α相似。

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