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Characterization of levamisole binding sites in Trichinella spiralis
被引:0
|作者:
A. Jiménez-González
R. M. Ros-Moreno
M. J. Moreno-Guzmán
F. Rodríguez-Caabeiro
机构:
[1] Parasitology Laboratory,
[2] Parasitology and Microbiology Department,undefined
[3] Faculty of Pharmacy,undefined
[4] University of Alcalá,undefined
[5] Ctra. Madrid-Barcelona Km. 33,undefined
[6] 600,undefined
[7] 28871 Alcalá de Henares,undefined
[8] Madrid,undefined
[9] Spain e-mail: mpmjmg@microb.alcala.es,undefined
[10] Tel.: +34 1 885 46 36 Fax: +34 1 885 46 63,undefined
来源:
关键词:
Binding Site;
Iodide;
Atropine;
Dissociation Constant;
Binding Activity;
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摘要:
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 μM 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 μM, respectively, whereas d-tubocurarine and α-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.
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页码:757 / 759
页数:2
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