Abstract

PORTILLA-MARTINEZ, Andrés et al. Defining pharmacological terms based on receptor ligand interactions. Cardiovasc. metab. sci [online]. 2020, vol.31, n.3, pp.66-70.  Epub June 07, 2024. ISSN 2954-3835.  https://doi.org/10.35366/95585.

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.

Keywords : Ligands; agonist; antagonism; receptor theory; biased agonist; GPCR.