In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form

Evgeniy A Gorbunov, Irina A Ertuzun, Evgeniya V Kachaeva, Sergey A Tarasov, Oleg I EpsteinOOO “NPF “MATERIA MEDICA HOLDING”, Moscow, Russian FederationAbstract: Experimentally and clinically, it was shown that released-active form of antibodies to S100 protein (RAF of A...

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Autores principales:	Gorbunov EA, Ertuzun IA, Kachaeva EV, Tarasov SA, Epstein OI
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Neurosciences. Biological psychiatry. Neuropsychiatry RC321-571 Neurology. Diseases of the nervous system RC346-429
Acceso en línea:	https://doaj.org/article/6471bba13d9341a68856c071ab3664de
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spelling	oai:doaj.org-article:6471bba13d9341a68856c071ab3664de2021-12-02T00:58:02ZIn vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form1178-2021https://doaj.org/article/6471bba13d9341a68856c071ab3664de2015-11-01T00:00:00Zhttps://www.dovepress.com/in-vitro-screening-of-major-neurotransmitter-systems-possibly-involved-peer-reviewed-article-NDThttps://doaj.org/toc/1178-2021Evgeniy A Gorbunov, Irina A Ertuzun, Evgeniya V Kachaeva, Sergey A Tarasov, Oleg I EpsteinOOO “NPF “MATERIA MEDICA HOLDING”, Moscow, Russian FederationAbstract: Experimentally and clinically, it was shown that released-active form of antibodies to S100 protein (RAF of Abs to S100) exerts a wide range of pharmacological activities: anxiolytic, antiasthenic, antiaggressive, stress-protective, antihypoxic, antiischemic, neuroprotective, and nootropic. The purpose of this study was to determine the influence of RAF of Abs to S100 on major neurotransmitter systems (serotoninergic, GABAergic, dopaminergic, and on sigma receptors as well) which are possibly involved in its mechanism of pharmacological activity. Radioligand binding assays were used for assessment of the drug influence on ligand–receptor interaction. [35S]GTPγS binding assay, cyclic adenosine monophosphate HTRF™, cellular dielectric spectroscopy assays, and assays based on measurement of intracellular concentration of Ca2+ ions were used for assessment of agonist or antagonist properties of the drug toward receptors. RAF of Abs to S100 increased radioligand binding to 5-HT1F, 5-HT2B, 5-HT2Cedited, 5-HT3, and to D3 receptors by 142.0%, 131.9%, 149.3%, 120.7%, and 126.3%, respectively. Also, the drug significantly inhibited specific binding of radioligands to GABAB1A/B2 receptors by 25.8%, and to both native and recombinant human sigma1 receptors by 75.3% and 40.32%, respectively. In the functional assays, it was shown that the drug exerted antagonism at 5-HT1B, D3, and GABAB1A/B2 receptors inhibiting agonist-induced responses by 23.24%, 32.76%, and 30.2%, respectively. On the contrary, the drug exerted an agonist effect at 5-HT1A receptors enhancing receptor functional activity by 28.0%. The pharmacological profiling of RAF of Abs to S100 among 27 receptor provides evidence for drug-related modification of major neurotransmitter systems.Keywords: dopamine agent, released-activity, serotonin agent, sigma1 receptorGorbunov EAErtuzun IAKachaeva EVTarasov SAEpstein OIDove Medical PressarticleNeurosciences. Biological psychiatry. NeuropsychiatryRC321-571Neurology. Diseases of the nervous systemRC346-429ENNeuropsychiatric Disease and Treatment, Vol 2015, Iss default, Pp 2837-2846 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Neurosciences. Biological psychiatry. Neuropsychiatry RC321-571 Neurology. Diseases of the nervous system RC346-429
spellingShingle	Neurosciences. Biological psychiatry. Neuropsychiatry RC321-571 Neurology. Diseases of the nervous system RC346-429 Gorbunov EA Ertuzun IA Kachaeva EV Tarasov SA Epstein OI In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form
description	Evgeniy A Gorbunov, Irina A Ertuzun, Evgeniya V Kachaeva, Sergey A Tarasov, Oleg I EpsteinOOO “NPF “MATERIA MEDICA HOLDING”, Moscow, Russian FederationAbstract: Experimentally and clinically, it was shown that released-active form of antibodies to S100 protein (RAF of Abs to S100) exerts a wide range of pharmacological activities: anxiolytic, antiasthenic, antiaggressive, stress-protective, antihypoxic, antiischemic, neuroprotective, and nootropic. The purpose of this study was to determine the influence of RAF of Abs to S100 on major neurotransmitter systems (serotoninergic, GABAergic, dopaminergic, and on sigma receptors as well) which are possibly involved in its mechanism of pharmacological activity. Radioligand binding assays were used for assessment of the drug influence on ligand–receptor interaction. [35S]GTPγS binding assay, cyclic adenosine monophosphate HTRF™, cellular dielectric spectroscopy assays, and assays based on measurement of intracellular concentration of Ca2+ ions were used for assessment of agonist or antagonist properties of the drug toward receptors. RAF of Abs to S100 increased radioligand binding to 5-HT1F, 5-HT2B, 5-HT2Cedited, 5-HT3, and to D3 receptors by 142.0%, 131.9%, 149.3%, 120.7%, and 126.3%, respectively. Also, the drug significantly inhibited specific binding of radioligands to GABAB1A/B2 receptors by 25.8%, and to both native and recombinant human sigma1 receptors by 75.3% and 40.32%, respectively. In the functional assays, it was shown that the drug exerted antagonism at 5-HT1B, D3, and GABAB1A/B2 receptors inhibiting agonist-induced responses by 23.24%, 32.76%, and 30.2%, respectively. On the contrary, the drug exerted an agonist effect at 5-HT1A receptors enhancing receptor functional activity by 28.0%. The pharmacological profiling of RAF of Abs to S100 among 27 receptor provides evidence for drug-related modification of major neurotransmitter systems.Keywords: dopamine agent, released-activity, serotonin agent, sigma1 receptor
format	article
author	Gorbunov EA Ertuzun IA Kachaeva EV Tarasov SA Epstein OI
author_facet	Gorbunov EA Ertuzun IA Kachaeva EV Tarasov SA Epstein OI
author_sort	Gorbunov EA
title	In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form
title_short	In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form
title_full	In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form
title_fullStr	In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form
title_full_unstemmed	In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form
title_sort	in vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to s100 protein in released-active form
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/6471bba13d9341a68856c071ab3664de
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In vitro screening of major neurotransmitter systems possibly involved in the mechanism of action of antibodies to S100 protein in released-active form

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