~(125)I-标记尖吻蝮蛇出血毒素在兔体内的药代动力学研究

STUDIES ON THE DISTRIBUTION OF ~(125)I-LABELLED HEMORRHAGIC TOXIN FROM AGKISTRODON ACUTUS (~(125)I-AaT) IN RABBITS AND ITS PHARMACOKINETIC CHARACTERS

  • 摘要: <正> 一、引言 尖吻蝮蛇(五步蛇)以血液毒为主,其毒性之大是蛇咬伤死亡率最高的。致死的主要原因是全身性出血及局部组织坏死,目前尚无有效的临床治疗方法。因此,对出血毒素的研究,不论对探讨出血致死机理还是寻找有效的治疗方法均是十分重要的。我们用~(125)I标记研究出血毒素在家兔体内的分布及代谢动力学特点。

     

    Abstract: ~(125)I-AaT, prepared by oxidant-chloroamine T from the related venom of Agkistrodon Acutus, is given to a rabbit by intravenous injection, and then, the distribution of the toxin in the rabbit and its Pharmacokinetic characters have been studied. The rabbit is killed five hours after the injection, and tthe radioactivity in each tissue calculated. The result indicates that the blood-brain barrier exist in the body, and large quantity of by-Products of ~(125)I-AaT metabolism is eliminated from urine by the kidney. For Pharmacokinetics, the computer simulated curve demonstrates that the result conforms to the Two Compartment Model. The fast component half-life T_(1/2α) is 3.15mins., slow component T_(1/2β) 165 mins., and the biological half-life T_(1/2) is 75.2 mins. V_(?), V_t and V_c have been analyzed, and we think Preliminarily that there must have been a corresponding receptor to the toxin in the body.

     

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