ISSN:
1522-9602
Source:
Springer Online Journal Archives 1860-2000
Topics:
Biology
,
Mathematics
Notes:
Abstract According to the occupation theory of drug receptor interaction, the response is a functionf of the number of receptors occupied by drug molecules. Considerable controversy exists regarding assumptions about this function. Without knowledge of the nature of the function, it is not possible to determine directly the rate constants, and hence the affinity constant, in the reaction between the receptor and an agonist drug. Instead, indirect determinations involving the use of antagonists have been employed, limiting the determination of affinity to those agents for which specific antagonists exist. The present paper discusses a method for the direct determination of affinity of an agonist drug. It is a “relaxation method,” i.e., the equilibrium is perturbed and the kinetics of the restoration process are studied. Assuming only thatf is non-decreasing and approximately linear over a limited domain of concentrations, it is shown that the change in response obeys first order kinetics, permitting a determination of the rate constants from the time course of the restoration process.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02476793
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