大鼠硬膜外和静脉注射虎纹毒素-Ⅰ后的组织分布  

Distribution profiles of huwentoxin-Ⅰafter epidural and intravenous administration in rats

作　　者：廖智[1] 戴舒佳[2] 刘秀文[2] 梁宋平[1] 汤仲明[2] 

机构地区：[1]湖南师范大学生命科学学院,湖南长沙410081 [2]北京放射医学研究所,北京100850

出　　处：《中国药理学与毒理学杂志》2003年第2期146-150,共5页Chinese Journal of Pharmacology and Toxicology

基　　金：国家自然科学基金资助项目 ( 39930 180 )~~

摘　　要：目的　比较大鼠硬膜外 (ed)和iv [12 5I]标记虎纹毒素 Ⅰ ([12 5I]HWTX Ⅰ )后分布的差异。方法Iodogen法制备 [12 5I]HWTX Ⅰ ,膈神经 膈肌法测定生物活性。反相高效液相色谱法鉴定放射化学纯度 ,三氯醋酸沉淀法测定放射性药物浓度。结果[12 5I]HWTX Ⅰ生物活性标记前后相近 ,放射化学纯度为 98.5 %。给药后 2h ,ed组椎管局部放射性明显高于iv组 (P <0 .0 5 ) ,ed和iv后组织放射性分别在 2h和 10min达峰值。泌尿系统放射性含量最高 ,脂肪、肌肉和脑放射性最低。放射性主要经尿排泄。结论　ed后椎管局部放射性高 ,维持时间较长 ,血清峰浓度较iv组低 ,有利于发挥局部镇痛作用 ,减少全身副作用。AIM To compare the bio distribution of 25 I labeled huwentoxin Ⅰ([ 125 I]huwentoxin Ⅰ, a novel analgestic peptide purified from the venom of spider Selenocosmia huwenna) after epidural(ed) and intravenous injection(iv) 13.2 kBq·g -1 in rats. METHODS [ 125 I]huwentoxin Ⅰ was prepared with iodogen methods and purified by gel filtration. The purity of [ 125 I]huwentoxin Ⅰ identified by reverse phase high performance liquid chromatography was 98.5% and exhibited biological activity assayed by mouse phrenic nerve diaphragm preparation in vitro . RESULTS Radioactivity in dural vertebral samples was significantly higher after ed than after iv, indicating a successful injection of [ 125 I]huwentoxin Ⅰ into epidural space. Radioactivity in epidural space declined post injection and sustained for a long time after ed injection. Radioactivity showed a gradient in body tissues following ed injection. The distribution profiles after iv were similar to ed but higher in most tissues. The highest concentrations in most tissues were found at 2 h following ed injection and at 10 min after iv. CONCLUSION The bio distribution profiles following epidural injection confirmed the higher concentration in dural vertebral samples and lower peak concentration in serum.

关 键 词：虎纹毒素-I 镇痛药 硬膜外给药 静脉注射给药 药物代谢动力学 

分 类 号：R285[医药卫生—中药学]