Receptor partial agonism and method to express receptor partial activation with respect to novel Full Logistic Model of mixture toxicology

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F18%3A10373081" target="_blank" >RIV/00216208:11310/18:10373081 - isvavai.cz</a>

Alternative codes found

RIV/61388971:_____/18:00490187

Result on the web

<a href="http://dx.doi.org/10.1016/j.tox.2017.10.012" target="_blank" >http://dx.doi.org/10.1016/j.tox.2017.10.012</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.tox.2017.10.012" target="_blank" >10.1016/j.tox.2017.10.012</a>

Result language

angličtina

Original language name

Receptor partial agonism and method to express receptor partial activation with respect to novel Full Logistic Model of mixture toxicology

Original language description

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&apos;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.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10511 - Environmental sciences (social aspects to be 5.7)

Project

<a href="/en/project/GA15-02328S" target="_blank" >GA15-02328S: Organisms and mechanisms determining the fate of endocrine disruptors in the environment</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2018

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Toxicology

ISSN

0300-483X

e-ISSN

—

Volume of the periodical

393

Issue of the periodical within the volume

January 2018

Country of publishing house

NL - THE KINGDOM OF THE NETHERLANDS

Number of pages

8

Pages from-to

26-33

UT code for WoS article

000423636200004

EID of the result in the Scopus database

2-s2.0-85033408223