摘要
探讨半乳糖基人生长激素（ｈＧＨＧａｌ）作为受体介导肝靶向促生长介素（ＳＯＭ）分泌，以治疗侏儒症的可能性。利用双功能试剂亚氨基甲氧基乙基硫代半乳吡喃糖甙和人生长激素（ｈＧＨ）偶联合成ｈＧＨＧａｌ。以１３１Ｉ标记ｈＧｈＧａｌ和ｈＧＨ后，进行小鼠体内分布实验、家兔显像实验的对比研究及１３１ＩｈＧＨＧａｌ鸡显像和家兔体内竞争结合实验。结果：ｈＧＨＧａｌ具有明显的趋肝性，肝最大摄取率为７５２７％～７７４０％，是ｈＧＨ的２倍以上，与肝脏的结合具有受体介导特性。表明ｈＧＨＧａｌ是一种很有希望的受体介导肝靶向促ＳＯＭ分泌及治疗侏儒症的新药。
PURPOSE To assess livertaxis mechanism of anti dwarfism drug galactosyl human growth hormone (hGH Gal) using radioactive tracer technique METHODS hGH Gal was prepared by the covalent coupling of human growth hormone (hGH) and a bifunctional reagent 2 imino 2 methoxycthyl 1 thiogalactose After hGH Gal and hGH were labelled with 131 I, the data of biodistribution in mice, imaging in rabbits and chicken were obtained RESULTS hGH Gal had remarkable livertaxis and its uptake in liver was 75 27%～77 40% that was about two fold high than hGH Its hepatic binding was receptor mediated and triple its pharmaceutical effect than hGH CONCLUSIONS hGH Gal is a potential receptor mediated hepatic targeting secreting somatomedian drug for treating dwarfism
出处
《中华核医学杂志》
CAS
CSCD
北大核心
1997年第2期106-108,共3页
Chinese Journal of Nuclear Medicine
基金
国家自然科学基金
