摘要
用125I标记尖吻蝮蛇毒出血毒素I(AaHI),用125I-AaHI为材料研究它在家兔体内的分布和药物代谢动力学,研究结果表明,有血脑屏障存在,肝脏和肾脏含量较高,125I-AaHI代谢的产物主要通过肾排出,经计机模拟,125 I-AaHI的药物代谢动力学为一室模型,其中生物半衰期T1/2 为53.1min,K值为0.0154min-1.结合动力学研究结果表明,离子强度、温度和离子种类对125I-AaHI与肾匀浆组织结合无影响,pH低于5.8或高于8.0时结合能力下降,结合有时间饱和性,并有明显的竞争抑制现象.上述结果说明125I-AaHI在动物体内均匀分布,可能有AaHI相关的结合位点或受体存在.
Hemorrhagin I(AaH I)isolated from Agkistrodon acutus venom was labeled with 125I and 125I-AaH I was given to rabbits by intravenous injectiom.The distribution of the toxin in the rabbits,the pharmacokinetic and the binding kinetics were studied.The results indicate that the blood brain barrier exists and most of 125I-AaH I metabolites is eliminated by kidney.For pharmacokinetics,the compartment-simulated curve demonstrates that the result corresponds to one compartment model.The biological half-life T is 53.1min,and K is 0.0154 min-1.The results in binding kinetics show that temperature,ionic strengh and different ions had no influences to the combination of 125I-AaH I with homogenized kidney,which is rich in blood capillary.pH had some influence under the condition of above 8.0 or below 5.8. There were time-dependent and concentration-dependent saturation properties.The unlabeled AaH I can inhibited the binding of 125I-AaH I with homogenized kidney.We concluded that the distribution of the toxin in rabbits is even except brain,and there may been some corresponding receptors or binding sites to AaH I in animal body.
出处
《科技通报》
北大核心
2003年第2期154-157,161,共5页
Bulletin of Science and Technology