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The receptor occupancy model, which describes agonist and competitive antagonists, was built on the work of Langley, Hill, and Clark.The occupancy model was the first model put forward by Clark to explain the activity of drugs at receptors and quantified the relationship between drug concentration and observed effect.
IUPAC defines a pharmacophore to be "an ensemble of steric and electronic features that is necessary to ensure the optimal supramolecular interactions with a specific biological target and to trigger (or block) its biological response". [1] A pharmacophore model explains how structurally diverse ligands can bind to a common receptor site.
When two drugs affect each other, it is a drug–drug interaction (DDI). The risk of a DDI increases with the number of drugs used. [1] A large share of elderly people regularly use five or more medications or supplements, with a significant risk of side-effects from drug–drug interactions. [2] Drug interactions can be of three kinds ...
Easson and Stedman [30] (1933) advanced a drug-receptor interaction model to account for the differential pharmacodynamic activity between enantiomeric pairs. In this model the more active enantiomer (the eutomer) take part in a minimum of three simultaneous intermolecular interactions with the receptor surface (good fit), Figure.
Toggle Theories of drug-receptor interaction subsection. 3.1 Occupation. 3.2 Rate. 3.3 Induced-fit. 3.4 Spare Receptors. 4 Receptor regulation. 5 Examples and ligands.
By knowing the interaction between a certain site of a drug and a receptor, other drugs can be formulated in a way that replicates this interaction, thus producing the same therapeutic effects. Indeed, this method is used to create new drugs. It can help identify which patients are most likely to respond to treatment.
where L, R, and LR represent ligand (drug), receptor, and ligand-receptor complex concentrations, respectively. This equation represents a simplified model of reaction dynamics that can be studied mathematically through tools such as free energy maps.
In a ligand-receptor interaction, the ligand binds with the receptors to form a drug-receptor complex, producing a biological response. [3] [4] The biological nature of receptors can be enzymes, nucleic acids or cellular proteins. Common types of receptors include G-protein coupled receptors, nuclear receptors and ion channels. [4]