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Characterization of levamisole binding sites in Trichinella spiralis
A Jiménez-González1, R M Ros-Moreno, M J Moreno-Guzmán
1Parasitology and Microbiology Department, Faculty of Pharmacy, University of Alcalá, Alcalá de Henares, Madrid, Spain. mpmjmg@microb.alcala.es
Abstract:
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.