By John C. Foreman, Torben Johansen, Alasdair J. Gibb
"Providing an creation to the learn of drug receptors, the Textbook of receptor pharmacology discusses quantitative descriptions of sensible reviews with agonists and antagonists; quantitative descriptions of ligands binding to receptors; the molecular buildings of drug receptors; and the weather that shipping the sign from the activated receptor to the intracellular compartment. This 3rd edition Read more...
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Example text
The panel on the left shows the log concentration response curves for the conventional agonist (open squares) and the inverse agonist (open circles). The closed symbols show how the curves change when the antagonist (WAY 100,635 at 10 nM) is included in the incubation fluid. Note the parallel, and similar, shift in the lines. The right hand panel illustrates the effects of a wide range of concentrations of the same antagonist applied on its own (open symbols) or in the presence of a high concentration of either the conventional agonist (closed squares) or the inverse agonist (closed circles).
Receptors are not involved. For example, the chelating agent EDTA (ethylenediaminetetraacetic acid) can be used to treat poisoning by lead (a less toxic chelate is formed and excreted). Functional antagonism—This involves cellular sites other than that for the agonist and can take several forms. In physiological antagonism, the action of an agonist is countered by a second agonist, which exerts an opposing biological effect. Each acts through its own receptors. For example, adrenaline relaxes bronchial smooth muscle, thus reducing the bronchoconstriction caused by histamine and the cysteinyl-leukotrienes.
37) 29 Classical Approaches to the Study of Drug-Receptor Interactions From this we can see that the term E/(1 + E) is equivalent, if only in a formal sense, to Stephenson’s efficacy. If an agonist is applied at a very high concentration, so that all the receptors are occupied, the proportion in the active state is E/(1 + E). If this agonist is also very effective, that is, if E is >>1, the proportion of active receptors becomes close to unity, the upper limit. 5). 37), we can see that E must be unity for this agonist.