By Bertram Katzung, Anthony Trevor
Prepared to mirror the syllabi in lots of pharmacology classes and in built-in curricula, simple & medical Pharmacology, 12e covers the real options scholars want to know in regards to the technological know-how of pharmacology and its software to scientific perform. number of the subject material and order of its presentation are in line with the authors’ a long time event in instructing this fabric to millions of clinical, pharmacy, dental, podiatry, nursing, and different well-being technology scholars.
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This is not the case with an irreversible (or noncompetitive) antagonist, which reduces the maximal effect the agonist can achieve, although it may not change its EC50. CHAPTER 2 Drug Receptors & Pharmacodynamics for a given degree of response, and so the agonist concentrationeffect curve is shifted to the right. The concentration (C′) of an agonist required to produce a given effect in the presence of a fixed concentration ([I]) of competitive antagonist is greater than the agonist concentration (C) required to produce the same effect in the absence of the antagonist.
In this case, the ability to prevent responses to varying and high concentrations of agonist is a therapeutic advantage. If overdose occurs, however, a real problem may arise. If the α-adrenoceptor blockade cannot be overcome, excess effects of the drug must be antagonized “physiologically,” ie, by using a pressor agent that does not act via α receptors. Antagonists can function noncompetitively in a different way; that is, by binding to a site on the receptor protein separate from the agonist binding site, and thereby modifying receptor activity without blocking agonist binding (see Figure 1–3C and D).
Now receptors are being discovered by predicted structure or sequence homology to other (known) receptors, and drugs that bind to them are developed later using chemical screening methods. This effort has revealed, for many known drugs, a larger diversity of receptors than previously anticipated. It has also identified a number of “orphan” receptors, so-called because their ligands are presently unknown, which may prove to be useful targets for the development of new drugs. The best-characterized drug receptors are regulatory proteins, which mediate the actions of endogenous chemical signals such as neurotransmitters, autacoids, and hormones.