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犬静脉注射T-2毒素及其代谢产物HT-2毒素后的药代动力学

Pharmacokinetics of T-2 toxin and its metabolite HT-2 toxin, after intravenous administration in dogs.

作者信息

Sintov A, Bialer M, Yagen B

出版信息

Drug Metab Dispos. 1986 Mar-Apr;14(2):250-4.

PMID:2870902
Abstract

The pharmacokinetics of T-2 toxin and HT-2 toxin were investigated comparatively in five dogs, after iv administration of the toxins (0.4 mg/kg). T-2 toxin was very rapidly and almost completely biotransformed to HT-2 toxin (fm = 83.6 +/- 3.9%). The following mean pharmacokinetic parameters were determined in this study for T-2 toxin and HT-2 toxin, respectively: half-life 5.3 +/- 2.1 and 19.6 +/- 4.7 min, clearance 0.107 +/- 0.056 and 0.167 +/- 0.074 liters/min/kg, and volume of distribution 0.86 +/- 0.63 and 4.47 +/- 1.38 liters/kg. The high clearance values suggest that the metabolism of T-2 toxin and HT-2 toxin is carried out in blood and/or through diffusion by nonspecific carboxyesterases. The results of this study suggest the possibility of a sustenance of T-2 toxin metabolism by its binding to blood cells.

摘要

在五只犬静脉注射毒素(0.4mg/kg)后,对T-2毒素和HT-2毒素的药代动力学进行了比较研究。T-2毒素非常迅速且几乎完全生物转化为HT-2毒素(转化率fm = 83.6 +/- 3.9%)。在本研究中,分别测定了T-2毒素和HT-2毒素的以下平均药代动力学参数:半衰期分别为5.3 +/- 2.1和19.6 +/- 4.7分钟,清除率分别为0.107 +/- 0.056和0.167 +/- 0.074升/分钟/千克,分布容积分别为0.86 +/- 0.63和4.47 +/- 1.38升/千克。高清除率值表明T-2毒素和HT-2毒素的代谢是在血液中进行的,和/或通过非特异性羧酸酯酶的扩散进行。本研究结果表明T-2毒素通过与血细胞结合维持其代谢的可能性。

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