Abstract
The value of the γ-aminobutyric acid (GABA) receptor of nematodes as a target for ivermectin's mode of action remains unclear. Using binding assays, we examined extracts from Trichinella spiralis muscle larvae for the presence of [3H]-ivermectin and [3H]-GABA binding sites. Tissue preparations displayed affinity binding sites for [3H]-ivermectin with a dissociation constant (K d) of 83 nM and a receptor density (Bmax) of 145 fmol/mg protein. We also identified a specific [3H]-GABA binding activity with a K d of 1.2 μM and a Bmax of 4.78 pmol/mg protein. In competition studies, ivermectin was found to be a competitive inhibitor of specific [3H]-GABA binding activity with an inhibition constant (K i) of 3.39 nM, suggesting that GABA receptors could be implicated in the mechanism of action of ivermectin in nematodes.
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Received: 7 August 1998 / Accepted: 22 September 1998
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Ros-Moreno, R., Moreno-Guzmán, M., Jiménez-González, A. et al. Interaction of ivermectin with γ-aminobutyric acid receptors in Trichinella spiralis muscle larvae. Parasitol Res 85, 320–323 (1999). https://doi.org/10.1007/s004360050555
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DOI: https://doi.org/10.1007/s004360050555