Theoretical Hyperbolic Model of a Partial Agonism: Explicit Formulas for Affinity, Efficacy and Amplification

Milanov, Peter; Pencheva, Nevena

Serdica Journal of Computing (2011)

  • Volume: 5, Issue: 4, page 333-358
  • ISSN: 1312-6555

Abstract

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The quantitative analysis of receptor-mediated effect is based on experimental concentration-response data in which the independent variable, the concentration of a receptor ligand, is linked with a dependent variable, the biological response. The steps between the drug–receptor interaction and the subsequent biological effect are to some extent unknown. The shape of the fitting curve of the experimental data may give some in-sights into the nature of the concentration–receptor–response (C-R-R) mechanism. It can be evaluated by non-linear regression analysis of the experimental data points of the independent and dependent variables, which could be considered as a history of the interaction between the drug and receptors. However, this information is not enough to evaluate such important parameters of the mechanism as the dissociation constant (affinity) and efficacy. There are two ways to provide more detailed information about the C-R-R mechanism: (i) an experimental way for obtaining data with new orThe study was partially supported by Bulgarian NSF Projects: DOO2-162/ 2008 and DOO2-135/2009.

How to cite

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Milanov, Peter, and Pencheva, Nevena. "Theoretical Hyperbolic Model of a Partial Agonism: Explicit Formulas for Affinity, Efficacy and Amplification." Serdica Journal of Computing 5.4 (2011): 333-358. <http://eudml.org/doc/219549>.

@article{Milanov2011,
abstract = {The quantitative analysis of receptor-mediated effect is based on experimental concentration-response data in which the independent variable, the concentration of a receptor ligand, is linked with a dependent variable, the biological response. The steps between the drug–receptor interaction and the subsequent biological effect are to some extent unknown. The shape of the fitting curve of the experimental data may give some in-sights into the nature of the concentration–receptor–response (C-R-R) mechanism. It can be evaluated by non-linear regression analysis of the experimental data points of the independent and dependent variables, which could be considered as a history of the interaction between the drug and receptors. However, this information is not enough to evaluate such important parameters of the mechanism as the dissociation constant (affinity) and efficacy. There are two ways to provide more detailed information about the C-R-R mechanism: (i) an experimental way for obtaining data with new orThe study was partially supported by Bulgarian NSF Projects: DOO2-162/ 2008 and DOO2-135/2009.},
author = {Milanov, Peter, Pencheva, Nevena},
journal = {Serdica Journal of Computing},
keywords = {Model; Agonist; Affinity; Efficacy; Amplification; Receptor},
language = {eng},
number = {4},
pages = {333-358},
publisher = {Institute of Mathematics and Informatics Bulgarian Academy of Sciences},
title = {Theoretical Hyperbolic Model of a Partial Agonism: Explicit Formulas for Affinity, Efficacy and Amplification},
url = {http://eudml.org/doc/219549},
volume = {5},
year = {2011},
}

TY - JOUR
AU - Milanov, Peter
AU - Pencheva, Nevena
TI - Theoretical Hyperbolic Model of a Partial Agonism: Explicit Formulas for Affinity, Efficacy and Amplification
JO - Serdica Journal of Computing
PY - 2011
PB - Institute of Mathematics and Informatics Bulgarian Academy of Sciences
VL - 5
IS - 4
SP - 333
EP - 358
AB - The quantitative analysis of receptor-mediated effect is based on experimental concentration-response data in which the independent variable, the concentration of a receptor ligand, is linked with a dependent variable, the biological response. The steps between the drug–receptor interaction and the subsequent biological effect are to some extent unknown. The shape of the fitting curve of the experimental data may give some in-sights into the nature of the concentration–receptor–response (C-R-R) mechanism. It can be evaluated by non-linear regression analysis of the experimental data points of the independent and dependent variables, which could be considered as a history of the interaction between the drug and receptors. However, this information is not enough to evaluate such important parameters of the mechanism as the dissociation constant (affinity) and efficacy. There are two ways to provide more detailed information about the C-R-R mechanism: (i) an experimental way for obtaining data with new orThe study was partially supported by Bulgarian NSF Projects: DOO2-162/ 2008 and DOO2-135/2009.
LA - eng
KW - Model; Agonist; Affinity; Efficacy; Amplification; Receptor
UR - http://eudml.org/doc/219549
ER -

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