A study on the effect of deoxynivalenol on serotonin receptor binding in fig brain membranes
Titel:
A study on the effect of deoxynivalenol on serotonin receptor binding in fig brain membranes
Auteur:
Prelusky, D. B.
Verschenen in:
Journal of environmental science and health. Part B, Pesticides, food contaminants, and agricultural wastes
Paginering:
Jaargang 31 (1996) nr. 5 pagina's 1103-1117
Jaar:
1996-09
Inhoud:
Central serotoninergic (5-hydroxytryptamine, 5HT) pathways are believed to be involved in the mechanisms of anorexia and/or emesis evoked by the trichothecene mycotoxin deoxynivalenol (DON). Using an in vitro membrane receptor binding assay, the competitive potency of DON was investigated against several radioactive ligands that have a high affinity for selective 5HT-receptor subgroups. Receptor site densities and displacement profiles in twelve selected regions of pig brain were investigated. Overall, DON possessed only minimal efficacy to competently block any of the 5HT-ligands tested. IC50 values (50% inhibitory concentration) of at least 5 mM DON were required to inhibit binding, and in certain regions concentrations of 100 mM were ineffective. In comparison, several standard 5HT-antagonists showed 103-105 times greater capability than DON to displace binding of these ligands. Because these results indicated DON possesses only weak affinity for the 5HT-receptor subtypes investigated here, this suggested that in vivo, unless relatively high concentrations of the toxin are present, its pharmacological effects may be mediated by mechanisms other than a functional interaction with serotoninergic receptors at the central level.
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