The aim of the study was to assess the state of receptor binding parameters under the action of sodium fluoride on the organism under model conditions for the intoxication formation.
Material and methods. The experimental part of the work was performed on 16 white rats of the Wistar population. Internal organs and tissues were subjected to the study of the state of receptor binding parameters of labeled C1, C2 serotonin, α1, α2, β-adreno, D2-dopamine and glucocorticoid type II receptor agonists and antagonists in various regions of the brain and liver. The functional activity of the receptors was assessed by affinity and the number of binding sites and ligands.
Results. The study of the effect of sodium fluoride on the kinetic characteristics of the adrenoreceptors of the membrane fractions of liver cells and the cerebral cortex showed similar dynamic changes in the parameters of receptor binding of both α1-adreno- and β1-adrenoreceptors. The effect of sodium fluoride was manifested in a decrease in the affinity of the radioligand for α2-adrenoreceptors and an increase in the number of binding sites for this type of receptors. Similar dynamics of the kinetic characteristics of α2-adrenoreceptors was found in the cerebellum. The number of binding sites for β1-adrenoreceptors increased, while their affinity for ligands decreased. In the brainstem, there was a decrease in the affinity of the D2-receptors for ligands and the number of binding sites. Under conditions of subtoxic effect of sodium fluoride on white rats, a decrease in the affinity of radioligands for C2-receptors and the number of their binding sites in the cerebral cortex was observed.
Conclusions. The results of the study show that under the conditions of the formation of fluoride intoxication, structural and functional disorders of the receptor apparatus occur, which confirms the leading role in the development of this pathology of the state of biological membranes. Changes in the kinetic characteristics of adrenaline (α1, α2, β1), serotonin (C1, C2), dopamine (D2) and glucocorticoid receptors confirm the polytropic nature of the action of sodium fluoride on organs, systems and functions of the body.
Keywords: sodium fluoride, receptors, number of binding sites, equilibrium constant dissociation.
Cd = equilibrium constant dissociation
Bmax = number of binding sites
CNS = central nervous system
cAMP = cyclic adenosine monophosphate
Department of Clinical Pathophysiology, Topographic Anatomy and Operative Surgery, Kharkiv Medical Academy of Postgraduate Education, Ukraine
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