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Cardiovascular and Metabolic Science

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Antes Revista Mexicana de Cardiología

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2020, Number 3

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Cardiovasc Metab Sci 2020; 31 (3)

Defining pharmacological terms based on receptor ligand interactions

Portilla-Martínez A, Ortiz-Flores M, Hidalgo I, González-Ruiz C, Ceballos G, Nájera N
Full text How to cite this article 10.35366/95585

DOI

DOI: 10.35366/95585
URL: https://dx.doi.org/10.35366/95585

Language: English
References: 12
Page: 66-70
PDF size: 195.31 Kb.


Key words:

Ligands, agonist, antagonism, receptor theory, biased agonist, GPCR.

ABSTRACT

There are several theories of how a drug interacts with a receptor. This review discuss the theories considered the most relevant to elucidate the mechanisms that govern drug-receptor interactions such as the occupational theory proposed by A. J. Clark, who stablished that drug-receptor interactions can be interpreted as processes that obey the laws of physics and chemistry, proposing for the first time a mathematical approach describing the behavior of a ligand-receptor interaction. This theory has been modified with the development of new technics, such as recombinant technology, protein crystallization and in silico methodologies, which all contribute with important experimental data for a better understanding of ligand-receptor interaction. Over time the drug-receptor interactions theories became more complex and accurate, and gain a few fundamental parameters such as potency, efficacy, dose, types of agonism (partial, total, inverse), antagonism (competitive and non-competitive) or modulation. The deep understanding of these new concepts in drug-receptor pharmacology, can make the difference between success or failure in pharmacological treatment in the clinical area.


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Cardiovasc Metab Sci . 2020;31