Jiménez-González A, Ros-Moreno R M, Moreno-Guzmán M J, Rodríguez-Caabeiro F
Parasitology and Microbiology Department, Faculty of Pharmacy, University of Alcalá, Alcalá de Henares, Madrid, Spain.
Parasitol Res. 1998 Sep;84(9):757-9. doi: 10.1007/s004360050482.
Characterization of the levamisole receptor was performed with total extracts of Trichinella spiralis muscle larvae using binding assays with tritiated levamisole ([3H]LEV, 291 GBq/mmol). We detected a specific [3H]LEV binding activity with a dissociation constant (Kd) of 4.76 microM and a receptor density (Bmax) of 2.14 pmol/mg of protein. In inhibition studies, only dimethylphenylpiperazinium iodide (DMPP) and hexamethonium were found to be competitive inhibitors of the [3H]LEV binding with an inhibition constant (Ki) of 31.04 and 4.43 microM, respectively, whereas d-tubocurarine and alpha-bungarotoxine had no effect on [3H]LEV binding activity, and procaine and atropine potentiated the [3H]LEV-receptor binding. All these data support the idea that levamisole acts as a cholinergic agonist in T. spiralis.
利用氚标记的左旋咪唑（[3H]LEV，291 GBq/mmol）结合试验，对旋毛虫肌幼虫的总提取物进行了左旋咪唑受体的鉴定。我们检测到一种特异性的[3H]LEV结合活性，其解离常数（Kd）为4.76 microM，受体密度（Bmax）为2.14 pmol/mg蛋白质。在抑制研究中，仅发现碘化二甲基苯基哌嗪（DMPP）和六甲铵是[3H]LEV结合的竞争性抑制剂，其抑制常数（Ki）分别为31.04和4.43 microM，而d-筒箭毒碱和α-银环蛇毒素对[3H]LEV结合活性无影响，普鲁卡因和阿托品增强了[3H]LEV与受体的结合。所有这些数据支持左旋咪唑在旋毛虫中作为胆碱能激动剂起作用的观点。
