Medicinal Chemistry
X-RAY CRYSTALLOGRAPHY ANDNMR M. R. Jefson (1998). Applications of NMR spectroscopy to structure determination. Ann. Rev. Med. Ch ...
2 Basic Principles of Drug Design II Receptors: structure and properties 67 2.1 THE RECEPTOR CONCEPT AND ITS HISTORY Along with ...
2.2 THE NATURE OF RECEPTORS AND CRITERIA FOR RECEPTOR IDENTITY From the medicinal chemistry perspective, a receptor is a biologi ...
The receptor should be present in the tissues in quantities commensurate with established receptor concentrations (10–100 pmol/ ...
2.3.1 Covalent Bond Interactions Although very important in traditional organic chemistry, covalent bonds are less important in ...
While most drugs do not covalently attach themselves to their receptors, a few do. Penicillin (2.3), one of the most important a ...
dipole moments, dipole–dipole interactions are frequent. A carbonyl (C=O) functional group, for example, constitutes a dipole si ...
with free, nonbonding electron pairs. Acceptor molecules are p-electron-deficient systems such as purines and pyrimidines or aro ...
once the hydrocarbon chains are in sufficient proximity, van der Waals forces become operative between them. 2.3.8 Selection of ...
The first strategy concerns the optimal number of contact points between the drug and the receptor. If the drug molecule has onl ...
There are also partial agonists that act on the same receptor as other agonists in a group of ligands (binding molecules) or dru ...
Potencyrefers to the dose of a drug required to produce a specific effect of given magnitude as compared to a standard reference ...
2.5 CLASSICAL THEORIES OF DRUG–RECEPTOR BINDING INTERACTIONS The classical theories of drug action were developed by Gaddum and ...
Combining equations (2.9) and (2.10) yields Equation (2.11) indicates a hyperbolic relationship between the effect and the conce ...
Dividing (2.15) by (2.16): The Schild equation is thus obtained, where [D]/[d] is the “dose ratio.” From equation (2.17), [A] 2 ...
to this view, the duration of receptor occupation determines whether a molecule is an agonist, partial agonist, or antagonist. A ...
and where the fraction of occupied sites υis 2.6.1 Direct Plot In the direct plot, equation (2.22) is solved for [DR] and its va ...
2.6.3 Double Reciprocal Plot The hyperbolic direct plot can easily be straightened out, as analogies from classical enzymology t ...
in the same population. The classical example is oxygen binding by hemoglobin, which is treated in every biochemistry text. In a ...
precise molecular pictures of receptor structure. The reshaping of our ideas on drug receptors is an ongoing process. 2.7.1 Func ...
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