Specific Receptors

The absorption of sulfonylureas from the upper gastrointestinal tract is faidy rapid and complete. The agents are transported in the blood as protein-bound complexes. As they are released from protein-binding sites, the free (unbound) form becomes available for diffusion into tissues and to sites of action. Specific receptors are present on pancreatic islet P-ceU surfaces which bind sulfonylureas with high affinity. Binding of sulfonylureas to these receptors appears to be coupled to an ATP-sensitive channel to stimulate insulin secretion. These agents may also potentiate insulin-stimulated glucose transport in adipose tissue and skeletal muscle. 

Dmg receptors represent another type of receptor family. The central nervous system (CNS) effects of the anxiolytic, diazepam, and the psychotropic actions of the caimabiaoids and phencycUdine have resulted ia the identification of specific receptors for these molecules. This has resulted ia the search for an endogenous ligand for these receptors. Thus, ia these situations, the pharmacological action has preceded the discovery of the receptor which, ia turn, has provided clues ia several iastances to the endogenous ligand. 

Olfactory receptors have been a subject of great interest (9). Much that has been postulated was done by analogy to the sense of sight in which there are a limited number of receptor types and, as a consequence, only three primary colors. Thus attempts have been made to recognize primary odors that can combine to produce all of the odors that can be perceived. Evidence for this includes rough correlations of odors with chemical stmctural types and the existence in some individuals having specific anosmias. Cross-adaptation studies, in which exposure to one odorant temporarily reduces the perception of a chemically related one, also fit into this hypothetical framework. Implicit in this theory is the idea that there is a small number of well-defined odor receptors, so that eventually the shape and charge distribution of a specific receptor can be learned and the kinds of molecular stmctures for a specified odor can be deduced. 

Adenosine, 6-amino-9-P-ribofuranosyl-9-ff-purine (see Table 1), is an endogenous nucleoside found in all ceUs of the body. Its ubiquitousness suggests that adenosine functions as an autocoid and that its actions are mediated by specific receptors on the plasma membranes of all ceUs. 

Calcium Channel Blockers. Because accumulation of calcium is one of the facets of the mote involved process leading to atherosclerosis, it would foUow that the antihypertensive calcium channel blockers might be effective in preventing atheroma. Both verapamil (Table 1) and nifedipine (Table 3) have been shown to stimulate the low density Upoprotein (LDL) receptor (159). This specific receptor-mediated pathway could theoretically improve Upid metaboUsm in the arterial wall, and thereby prove antiatherogenic. These effects have been proven in animals. 

Oestrogen action is mediated through specific receptors localised within the nucleus of target cells (see Carson-Jurnica et and Tsai and O Malley " for... 

In its simplest form, a model requires two types of data inputs information on the source or sources including pollutant emission rate, and meteorological data such as wind velocity and turbulence. The model then simulates mathematically the pollutant s transport and dispersion, and perhaps its chemical and physical transformations and removal processes. The model output is air pollutant concentration for a particular time period, usually at specific receptor locations. 

When most lipids circulate in the body, they do so in the form of lipoprotein complexes. Simple, unesterified fatty acids are merely bound to serum albumin and other proteins in blood plasma, but phospholipids, triacylglycerols, cholesterol, and cholesterol esters are all transported in the form of lipoproteins. At various sites in the body, lipoproteins interact with specific receptors and enzymes that transfer or modify their lipid cargoes. It is now customary to classify lipoproteins according to their densities (Table 25.1). The densities are... 

We have seen here that these simple methods which only rely upon the optimal use of molecular graphics tools can address highly specific receptor-ligand interactions. 

Watson, C., Chen, G., Irving, P. E., Way, J., Chen, W.-J., and Kenakin, T. P. (2000). The use of stimulus-biased assay systems to detect agonist-specific receptor active states Implications for the trafficking of receptor stimulus by agonists. Mol. Pharmacol. 58 1230-1238. 

Conjugation of DOX with copolymers or peptides Recognition of DOX by tumor-specific receptors or proteases Investigational... 

An antigen is a molecule recognised by specific receptors on cells of the immune system such as B lymphocytes. 

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