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Transcript
Logarithmic transformation of the dose axis and experimental demonstration of spare receptors, using different concentrations of an irreversible antagonist. Curve A shows agonist response in the absence of antagonist. After treatment with a low concentration of antagonist (curve B), the curve is shifted to the right. Maximal responsiveness is preserved, however, because the remaining available receptors are still in excess of the number required. In curve C, produced after treatment with a larger concentration of antagonist, the available receptors are no longer “spare”; instead, they are just sufficient to mediate an undiminished maximal response. Still higher concentrations of antagonist (curves D and E) reduce the number of available receptors to the point that maximal response is diminished. The apparent EC50 of the agonist in curves D and E may approximate the Kd that characterizes the binding Source: Drug Receptors & Pharmacodynamics, Basic & Clinical Pharmacology, 13e affinity of the agonist for the receptor. Citation: Katzung BG, Trevor AJ. Basic & Clinical Pharmacology, 13e; 2015 Available at: http://mhmedical.com/ Accessed: June 11, 2017 Copyright © 2017 McGraw-Hill Education. All rights reserved