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用~(125)Ⅰ标记从尖吻蝮蛇(Agkistrodon acutus)毒中分离出的出血毒素(Ⅰ Aa-HI),得到Ⅰ~(125)Ⅰ—AaHI。静脉注射~(125)Ⅰ—AaHI到家兔体内,对~(125)Ⅰ—AaHI在动物体内的分布和药物代谢动力学进行研究。注射~(125)Ⅰ—AaHI 5小时后将家兔杀死,测定各组织的放射性强度。结果表明有血脑屏障存在。~(125)Ⅰ—AaHI代谢的大量产物由肾通过尿排出。对于药物代谢动力学,计算机模似结果为一室模型,其中生物半衰期T_(1/2)为55.9分钟,K值为0.0124分钟。我们认为在动物体内可能有AaHI相关的结合位点或受体存在。
The hemorrhagic toxin (Ⅰ Aa-HI) isolated from the Agkistrodon acutus virus was labeled with ~ (125) Ⅰ to obtain Ⅰ ~ (125) Ⅰ-AaHI. Intravenous injection of ~ (125) Ⅰ-AaHI into rabbits was used to study the distribution and pharmacokinetics of ~ (125) I-AaHI in rabbits. Rabbits were sacrificed 5 hours after injection of ~ (125) I-AaHI, and the radioactivity of each tissue was measured. The results show that there is a blood-brain barrier. A large quantity of ~ (125) I-AaHI metabolites are excreted by the kidneys through the urine. For pharmacokinetics, the computer simulation results for the one-compartment model, biological half-life T_ (1/2) of 55.9 minutes, K value of 0.0124 minutes. We think there may be AaHI related binding sites or receptors in animals.