Drug action receptor theory

It is amazing to note that complex processes such as drug binding to protein, activation of cells, and observation of syncytial cellular response should apparently so closely follow a model based on these simple concepts. This was not lost on A. J. Clark in his treatise on drug receptor theory The Mode of Action of Drugs on Cells [4] ... 

MacKay, D. (1977). A critical survey of receptor theories of drag action. In Kinetics of drug action, edited by J. M. Van Rossum, pp. 255—322. Springer-Verlag, Berlin. 

Limbird, L. E., Cell Surface Receptors A Short Course on Theory and Methods, 2nd ed., Nijhoff, Boston, 1996. Pratt, W. B. and Taylor, P., Principles of Drug Action, Churchill Livingstone, New York, 1990 (see, in particular, Chapters 1 and 2). 

DIFFUSION OF LIGAND TO RECEPTOR DRUG RECEPTOR OCCUPANCY THEORY OF DRUG ACTION... 

Paton, W. D. M. A Theory of Drug Action Based on the Rate of Drug-Receptor Combination. Proc. R. Soc. London, Ser. B. 1961,154, 21-69. 

The receptor occupation theory of drug action equates drug effect to receptor occupancy. The intensity of drug effect is proportional to the number of receptors that are occupied by drug and the maximum effect occurs when all receptors are occupied by drug. 

This mechanism was defined later by Bush [6] as the blocking mechanism. Bush s classification is based on Raton s rate theory of drug action [181]. Raton suggested that a pharmacological effect depends not upon the number of individual drug-receptor combinations but upon the rate, of drug-receptor occupation. He assumes that receptor... 

Ariens, E.J 1966 Receptor Theory and Structure-Action Relationships. Adv Drug Res. 3 235-285 ... 

Paton, W. D. M. (1961). A theory of drug action based on the rate of drug-receptor combinations. Proceeding of the Royal Society of London, Series B, 154, 21—69. 

In the recent past, receptors and drug-reeeptor interaetions theories have highlighted the importance of physical and chemical characteristics with regard to drug action. Such salient features may include partition coefficients, solubility, degree of ionization, isosterism and bio-isosterism, surface activity, thermodynamic activity, intramolecular and intermolecular forces, redox potentials, stereochemisty and interatomic distances between various funetional groups. 

The Receptor Theory of Drug Action Langley and Ehrlich first proposed that drug actions were mediated by chemical receptors. In 1933, Clark developed the dose-response theory which stated that increased response to a drug depended on increased binding of drug to receptors. Clark s theory was incorrect on several points. In 1956, Stephenson presented a modified dose-response theory which is more widely accepted today. 

Eariy descriptions of drug action were confined to their reference as tonic or toxic effects. This approach was foiiowed by the concept of receptor theory, which for decades remained primariiy an operationai concept that was usefui for discussing the new actions of drugs on a moiecuiar ievei (1). Research in receptor theories, however, has provided evidence that the drug receptors do exist as distinct entities, and a iimited success has been attained in the characterization of receptors (2,3). 

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