Receptor design

There are known to be three opioid receptors, designated p, k, and 8, and these receptors share a high degree of amino acid sequence homology. The p-opioid receptor (MOR) is the primary receptor, which is activated by the nonselective... 

Brauner-Osborne, H., Egebjerg, J., Nielsen, E. 0., Madsen, U., and Krogsgaard-Larsen, P. (2000) Ligands for glutamate receptors design and therapeutic prospects. J. Med. Chem. 43, 2609-2645. 

Receptor affinity chromatography, 3 847 Receptor blockers, 5 158 Receptor design, principles of, 76 769-775 Receptor purity, in microarray fabrication, 76 383... 

In contrast to the -conjugated probe architecture utilizing an ICT process, the number of anion probes that rely on the fluorophore-spacer-receptor design and an active PET process is abundant [72], Again, anthracene and naphthalene... 

Ferrocene crown receptors designed to show conformationally induced electrochemical perturbations... 

Bipyridinium crown receptors designed to exhibit conformationally induced electrochemical perturbations on cation complexation... 

The recognition of a receptor function is the practical manifestation of successful receptor design. It follows that synthetic molecular receptors, in common with their natural counterparts, must be capable of recognizing other chemical species by achieving complementarity of steric and electronic shape, as well as, of course, size. 

There are three principal classes of opiate receptors, designated x, K, and 5, and there exist a number of drugs that are specific for each of these receptor types. However, most of the clinically used opiates are quite selective for the preceptor the endogenous opiates enkephalin, endorphin and dynorphin are selective for the p and 5, 5 and k receptors respectively. When activated by opioids these receptors produce biochemical signals that block neurotransmitter release from nerve terminals, a process that underlies their blockade of pain signaling pathways as well as other effects, such as constipation, diuresis, euphoria, and feeding. 

Possible measures that are expected to improve the potentiometric selectivity are (1) use of hosts that form stronger complexes, (2) modification of the host to avoid ionophore self-association, and (3) an improved choice of the membrane solvent to avoid strong solvation of the hosts in the membrane. Evidence for the importance of (2) and (3) has been obtained from C NMR spectra of 12. While the properties of 1 1 host-guest complexes are very often of primary interest in supramolecular chemistry, the above results show that use of receptors for sensing purposes must be based on a receptor design that goes beyond this viewpoint. 

Excitatory Amino Acid Receptors. Design of Agonists and Antagonists, Krogsgaard-Larsen, P, Hansen, J. J., Eds. Ellis Horwood Chichester, UK, 1992. 

The actions of substance P and neurokinins A and are mediated by three G protein-coupled tachykinin receptors designated NK i, NK 2, and NK 3. Substance P is the preferred ligand for the NK receptor, the predominant tachykinin receptor in the human brain. However, neurokinins A and also possess considerable affinity for this receptor. In humans, most of the central and peripheral effects of substance P are mediated by NKi receptors. All three receptor subtypes are coupled to inositol trisphosphate synthesis and calcium mobilization. 

Three subtypes of NT receptors, designated NT 1, NT 2, and NT 3, have been cloned. NT and NT2 receptors belong to the G protein-coupled superfamily with seven transmembrane domains the NT3 receptor is a single transmembrane domain protein that belongs to a family of sorting proteins. 

These diverse effects are mediated by multiple receptors designated Y through Y 6. All receptors except Y3 have been cloned and shown to be G protein-coupled receptors linked to mobilization of Ca2+ and inhibition of adenylyl cyclase. Yj and Y2 receptors are of major importance in the cardiovascular and other peripheral effects of the peptide. Y4 receptors have a high affinity for pancreatic polypeptide and may be a receptor for the pancreatic peptide rather than for NPY. Y5 receptors are found mainly in the central nervous system and... 

The central release of ATP from dorsal horn synaptosomes was proven by White et al. (1985). Further studies (Sawynok et al., 1993) suggest that ATP can be released from central terminals of primary afferent neurons as well as from terminals of non-primary afferents within the dorsal horn and that ATP and GABA are cotransmitters at many synapses in the dorsal horn (Jo and Schlichter, 1999). After being released ATP acts on specific receptors, designated as P2 purinoreceptors, on the cell surface. 

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