Počet záznamů: 1
Receptor partial agonism and method to express receptor partial activation with respect to novel Full Logistic Model of mixture toxicology
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SYSNO ASEP 0490187 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Receptor partial agonism and method to express receptor partial activation with respect to novel Full Logistic Model of mixture toxicology Tvůrce(i) Ezechiáš, Martin (MBU-M) RID
Cajthaml, Tomáš (MBU-M) RID, ORCIDZdroj.dok. Toxicology. - : Elsevier - ISSN 0300-483X
Roč. 393, JAN 15 (2018), s. 26-33Poč.str. 8 s. Jazyk dok. eng - angličtina Země vyd. IE - Irsko Klíč. slova Receptor theory ; Partial agonist ; Mixture toxicology Vědní obor RIV EE - Mikrobiologie, virologie Obor OECD Microbiology CEP GA15-02328S GA ČR - Grantová agentura ČR Institucionální podpora MBU-M - RVO:61388971 UT WOS 000423636200004 EID SCOPUS 85033408223 DOI 10.1016/j.tox.2017.10.012 Anotace Living organisms interact with various chemical compounds via receptors, which is described by the receptor theory. The affinity of the biologically active compounds toward receptors and their ability to trigger a biological or toxic signal vary substantially. In this work, we describe a new insight into understanding of the mode of action of receptor partial agonists and the receptor theory using a Full Logistic Model (FLM) of mixture toxicology. We describe the hypothesis that the effect of a partial agonist can be mathematically described via separation of agonistic and antagonistic behavior of the partial agonist where the antagonistic effect is described as an action of the compound producing zero effect. In this way, a competitive antagonist can be considered as an agonist with zero effect. This idea is also placed into a context with classical concepts, e.g., Gaddum's equation. Using the assumption that competitive antagonists are agonists with no effect, equations describing the microscopic and macroscopic equilibrium connts have been derived. Accordingly, we show that the constants could be calculated from the measured partial agonistic dose-response curve. As a consequence, we provide a simple mathematical tool for comparison of dose-response curves of drugs according to their affinities and efficacies.
Pracoviště Mikrobiologický ústav Kontakt Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Rok sběru 2019
Počet záznamů: 1