Drug-receptor analysis

T. Kenakin, Pharmacological Analysis of Drug Receptor Interaction, 2nd ed.. Raven, New York, 1993 D. Oksenberg and co-workers. Nature, 360, 161 (1992). 

Kenakin, T. P. (1997). The pharmacologic analysis of drug receptor interaction, Third edition. Lippincott-Raven, New York. 

For a detailed description of spectral map analysis (SMA), the reader is referred to Section 31.3.5. The method has been designed specifically for the study of drug-receptor interactions [37,44]. The interpretation of the resulting spectral map is different from that of the usual principal components biplot. The former is symmetric with respect to rows and columns, while the latter is not. In particular, the spectral map displays interactions between compounds and receptors. It shows which compounds are most specific for which receptors (or tests) and vice versa. This property will be illustrated by means of an analysis of data reporting on the binding affinities of various opioid analgesics to various opioid receptors [45,46]. In contrast with the previous approach, this application is not based on extra-thermodynamic properties, but is derived entirely from biological activity spectra. 

Kenakin, T. (1997), Pharmacologic Analysis of Drug-Receptor Interactions, 3rd ed., Lippincott-Raven, Philadelphia. 

Kenakin, T. P., Pharmacologic Analysis of Drug-Receptor Interaction, 3rd ed., Raven Press, New York, 1997. Kenakin, T. and Angus, J. A., The pharmacology of functional, biochemical and recombinant receptor systems, in Handbook of Experimental Pharmacology, Vol. 148, 2000. 

Wieland GA, Molinoff PB. 1981. Quantitative analysis of drug-receptor interactions I. Determination of kinetic and equilibrium properties. Life Sci 29 313. 

Computer-Assisted Drug Receptor Mapping Analysis... 

Lapinsh, M., Prusis, P., Gutcaits, A., Lundstedt, T., and Wikberg, J.E.S. Development of proteo-chemometrics a novel technology for the analysis of drug-receptor interactions. Biochim. Biophys. Acta 2001, 1525, 180-190. 

Kenakin TP. Pharmacological Analysis of Drug-receptor Interaction. New York Lippincott-Raven, 1993. Kenakin TP, Bond RA, and Bonner TI. Definition of pharmacological receptors. Pharmacol Rev 1992 44 351-362. 

Introduced by Corwin Hansch in the early 1960s, Hansch analysis considers both the physicochemical aspects of drug distribution from the point of application to the point of effect and the drug-receptor interaction. In a given group of drugs that have analogous structures and act by the same mechanism, three parameters seem to play a major role ... 

Thermodynamic analysis offers an insight into the molecular events underlying drug-receptor interactions (Testa etal., 1987 Raffa and Porreca, 1989). The thermodynamic quantification of binding may be obtained through application of the familiar equations (6) and (7)... 

Thermodynamic Analysis in Drug-Receptor Binding The A3 Adenosine Receptor... 

Raffa RB, Porreca F (1989) Thermodynamic analysis of the drug-receptor interaction. Life Sci 44(4) 245-258... 

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