Antagonism of receptor-activated biological effects mediated by second messenger pathways |
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Authors: | R B Raffa C P Bianchi |
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Institution: | Department of Pharmacology, Jefferson Medical College Thomas Jefferson University, Philadelphia, PA 19107, USA;Molecular Endocrinology Laboratory, Department of Biotechnology, Yuvaraja’s College, A Constituent Autonomous College of University of Mysore, Mysore 570005, India |
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Abstract: | It is generally held that many biologically active compounds produce their effects through a sequence of events that are initiated when the substances combine with selective receptors located on the cell surface membrane. Activation of these receptors produces a stimulus that is somehow transmitted intracellularly. The transduction between the stimulus and the response is now known to be mediated, in many systems, by an intracellular intermediary or second messenger. A model describing the relation of agonist concentration, receptor occupation, and biological response in such a system is herein extended to include antagonist binding at two target sites the cell-surface receptor and the receptor for the second messenger. It is demonstrated that the shift of an agonist's dose-response curve is characteristic of the site of antagonism and that analysis of this shift can reveal the existence of a second messenger pathway or, if this is known, the site of action of the antagonist. |
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