Download e-book for kindle: Receptor - Based Drug Design (Drugs and the Pharmaceutical by Paul Leff
By Paul Leff
Applying a variety of examples from G-protein-coupled receptors and ligand-gated ion channels, this designated, single-source reference illustrates the rules of pharmacological research and receptor category which are the root of rational drug layout. Explains the experimental and theoretical equipment used to signify interactions among ligands and receptors-providing the pharmacological info had to clear up remedy difficulties and facilitate the drug layout technique! Demonstrating the achievements of the receptor-based strategy in therapeutics and indicating destiny instructions, Receptor-Based Drug layout ·introduces novel computer-assisted recommendations for the layout of recent agonists, antagonists, and inverse agonists for G-protein-coupled receptors ·shows the way to examine agonist concentration-effect curve facts ·discusses radioligand binding assays ·presents new in vitro multiarray assays for G-protein-coupled receptors ·explains using person moment messenger signaling responses in reading drug-receptor interactions ·examines the position of electrophysiology find new medications and drug ambitions ·describes selectively performing b-adrenoceptor agonists and glucocorticoid steroids for bronchial asthma therapy ·outlines the explanation for utilizing angiotensin receptor antagonists ·and extra! Written via over 25 foreign experts and containing approximately 1200 bibliographic citations, Receptor-Based Drug layout is a realistic source for pharmacologists, pharmacists, and pharmaceutical scientists; natural and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate scholars in those disciplines.
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Additional info for Receptor - Based Drug Design (Drugs and the Pharmaceutical Sciences: a Series of Textbooks and Monographs)
Html (2 of 2) [2/29/2004 2:43:53 AM] ). Document Page 43 types Q and R, respectively, and a = [A]50R/[A]50Q, the ratio of the midpoint locations of the two “individual” E/[A] curves that contribute to the experimentally measured E/[A] curve. Equation (12) can be fitted directly to experimentally determined values of log10(r - 1) as a function of log10[B], allowing estimates of KBQ, KBR, and a to be made. The position of the inflexion of the plot depends on the values of [A]50R and [A]50Q. For an antagonist that has higher affinity for receptor type Q than for receptor type R, the inflexion will be below the abscissa of the Schild plot when a < 1, above it when a > 1, and will lie on the abscissa when a = 1.
49. (From Ref. ) which allows an explicit equation to be written down for the E/[A] relation (see above). In theory, this assumption about postreceptor events may restrict the use of the operational model (21,22). Such assumptions are deliberately avoided in the conventional null approach to agonist analysis (4,6,19). These null methods are based on the idea of pharmacological stimulus (S), which was originally defined by Stephenson (4) to be the product of efficacy (e) and fractional occupancy (y).
48; ). 07. The estimated slope parameter was not significantly different from unity, indicating that the interaction is consistent with simple competition. (From Ref. ) where [AR]/[R0] represents fractional receptor occupancy, [A] and [A'] are equieffective concentrations of agonist before and following receptor inactivation, KA is the agonist dissociation constant, and q is the fraction of receptors remaining after receptor inactivation. html (1 of 2) [2/29/2004 2:43:08 AM] Document (8) Thus a plot of 1/[A] versus 1/[A'] yields estimates of the slope (1/q) and the intercept [(1 - q)/qKA] from which KA can be estimated as slope-1/intercept.
Receptor - Based Drug Design (Drugs and the Pharmaceutical Sciences: a Series of Textbooks and Monographs) by Paul Leff