By John C. Foreman, Torben Johansen, Alasdair J. Gibb
"Providing an creation to the research 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 constructions of drug receptors; and the weather that delivery the sign from the activated receptor to the intracellular compartment. This 3rd edition gains effects from fresh study on how the constitution of receptors determines the interplay among the receptor and the sign transducer. This version additionally bargains new info on ligand binding receptor experiences that use newly constructed techniques"--Provided via publisher. Read more...
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Additional info for Textbook of receptor pharmacology
With these reservations in mind, no more than a brief mention is needed of three approaches that were used in past years to assess the efficacy of a partial agonist acting on an intact tissue. 4. 2) and with receptor occupancy given by the Hill–Langmuir equation in its simplest form (which we have already seen to be inadequate for agonists). The second analysis defines receptor occupancy as all the receptors that are occupied, active plus inactive. The first two of the three methods presuppose that the measurements are made with a tissue that has a large receptor reserve.
34 Donald H. 11, which is reproduced as the front face of the cube. Each of its four elements (R, R*, LR, and LR*) can combine with a G-protein to form RG, R*G, LRG, and LR*G, respectively. Of these, only R*G and LR*G lead to a tissue response. The top face of the cube shows ligand-bound states of the receptor. 5). 14). 5 at the end of the chapter). Finding the proportion in the active form is more difficult if the supply of G-protein is limited, but can be done using numerical methods. , single channel recording; changes in receptor fluorescence following the binding of a ligand) are becoming increasingly practicable, it still often happens that the only available measure of receptor activation is the response of an intact tissue.
The first is to apply the law of mass action to each of the equilibria that exist. The second is to write an equation that expresses the fact that the fractions of receptors in each condition that can be distinguished must add up to 1 (the conservation rule). 3) there are three such conditions: R (vacant and inactive), AR (inactive though A is bound), and AR* (bound and active). The corresponding fractions of receptors in these conditions* are pR, pAR, and pAR*. * The term state rather than condition is often used in this context.