Transmembrane G-coupled Receptor Proteins

W. H. Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substi-tuted)glycine peptoid library. J. Med. Chem. 1994, 37, 2678-2685. 

Also, a number of other neuropeptides have also been shown to interfere with the expression of thirst subsequent to water deprivation and/or sodium appetite subsequent to sodium depletion. In some instances, ANG 11, presumably in the neural system subserving thirst, stimulates the release of a neuropeptide that inhibits the expression of sodium appetite. ANG II stimulates the release of oxytocin (Lang et al., 1981) and oxytocin appears to be one of the main inhibitory factors that limit the expression of sodium appetite (Stricker Verbalis, 1987 Verbalis, Blackburn, Hoffman, Stricker, 1995). Oxytocin is a 9-amino acid peptide synthesized in PVN or SON neurons that project either to the neurohypophysis or to sites within the central nervous system. Oxytocin receptors are part of the 7 transmembrane, G-protein-coupled receptor family (Barberis, Mouillac, Durroux, 1998) and are found in the BNST, nucleus ofthe solitary... 

Figure 13.7 7-Transmembrane G-protein coupled receptor protein...

G. M. Figliozzi, D. A. Goff, M. A. Siani, R. J. Simson, S. C. Banville, E. G. Brown, L. Wang, L. S. Richter, and W. H. Moos, J. Med. Chem., 37, 2678 (1994). Discovery of Nanomolar Ligands for 7-Transmembrane G-Protein-Coupled Receptors from a Diverse N-(Substi-tuted)Glycine Peptoid Library. 

The physiological and pharmacological effects of histamine are mediated through four different receptors Hi, Hj, Hj, and Ht, all members of the 7-transmembrane g protein-coupled receptor (GPCR) family with amino terminal glycosylation sites and phosphorylation sites for protein kinases A and C. The receptors are widely expressed on different tissues that are responsive to histamine. For the Hi receptor these tissues include smooth muscle cells of the airways and vasculature, the gastrointestinal tract, cardiovascular system, neutrophils, endothelial cells, T and B cells, hepatocy tes, nerve... 

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