Drug affinity

From the time of A. J. Clark until the late 1970s, receptor models have been refined to describe drug affinity and efficacy. These ideas are collectively referred to as classical receptor theory. 

Drug affinity is best quantified in terms of the equilibrium dissociation constant for these varied forms of the target enzyme. 

Moore, V. A., et al. A rapid screening system to determine drug affinities for the intestinal dipeptide transporter 2 affinities of ACE inhibitors. Int. J. Pharm. 2000, 210, 29-44. 

A241G Tardive dyskinesia Altered drug affinity or (88,94 5) t... 

Beusniak, M.-Y., Pearlman, R.S., Neve, K.A., and Wilcox, R.E. Comparative molecular field analysis-based prediction of drug affinity at... 

We thus have a series of unbound drug affinity measures relating to the action of the drug. The values are those typically obtained by the pharmacologist and form the basis of the structure-activity relationships which the medicinal chemist will work on. It is possible to extend this model to provide a pharmacokinetic phase as shown in Figure 2.9. 

Another simplification can be made if all binding sites are independent (noncooperative binding) and they can be attributed to classes of identical sites. In protein-drug affinity studies the fraction of drug molecules bound (D4) per protein molecule (P) is given by... 

Three-dimensional representation of VHD-associated and non-VHD-associated drug affinity for a battery of GPCRs, ligand-gated ion channels, and biogenic amine transporters. 

Such calculations should eventually be able to provide a better understanding of the thermodynamic fundamentals of biochemical separation methods, particularly for such processes as membrane and chromatographic techniques a clearer understanding of the causes of molecular clustering will be important in this area. In the next five to ten years, these methods should be much more sophisticated and will play a major role in the design of drugs, affinity agents, and proteins that fold into desired patterns. 

Structural differences of ARBs influence the variation in pharmacological (pharmacokinetic /pharmacodynamic) properties of these drugs. Affinity for the ATj receptor is highest with candesartan, followed by irbesartan, losartan, valsartan, and telmisartan. Differences and affinities at the ATj receptor are also involved in... 

Pharmacological drug properties regrouping the drug affinity for transporters and enzymes of metabolism... 

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