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New insight into isobolographic analysis for combinations of a full and partial agonist: Curved isoboles
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SYSNO ASEP 0496199 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název New insight into isobolographic analysis for combinations of a full and partial agonist: Curved isoboles Tvůrce(i) Ezechiáš, Martin (MBU-M) RID
Cajthaml, Tomáš (MBU-M) RID, ORCIDZdroj.dok. Toxicology. - : Elsevier - ISSN 0300-483X
402-403, JUN 1 (2018), s. 9-16Poč.str. 8 s. Jazyk dok. eng - angličtina Země vyd. IE - Irsko Klíč. slova Receptor theory ; Partial agonist ; Mixture toxicology Obor OECD Toxicology CEP GA15-02328S GA ČR - Grantová agentura ČR TE01020218 GA TA ČR - Technologická agentura ČR Institucionální podpora MBU-M - RVO:61388971 UT WOS 000435064100002 EID SCOPUS 85045535851 DOI 10.1016/j.tox.2018.04.004 Anotace Receptor ligands in mixtures may produce effects that are greater than the effect predicted from their individual dose-response curves. The historical basis for predicting the mixture effect is based on Loewe's concept and its mathematical formulation. This concept considers compounds with constant relative potencies (parallel dose response curves) and leads to linear additive isoboles. These lines serve as references for distinguishing additive from nonadditive interactions according to the positions of the experimental data on or outside of the lines. In this paper, we applied a highly relevant two-state model for a description of the receptor-ligand interaction in the construction of the isobologram. In our model we consider partial agonists that have dose-response curve slopes differing from one. With this theoretical basis, we demonstrated that a combination of compounds with different efficacies leads to curved isoboles. This model should overwrite Tallarida's flawed assumption about isobolographic analysis of partial agonists and enhance our understanding of how the partial agonists contribute to the overall mixture effect. Pracoviště Mikrobiologický ústav Kontakt Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231 Rok sběru 2019
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