Upregulating G Protein-Coupled Receptors with Receptor Antagonists

2011 ◽  
pp. 403-419 ◽  
Author(s):  
Ellen M. Unterwald
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Receptor Antagonists ◽  
G Protein Coupled

Receptor antagonists for gastrointestinal peptides

1993 ◽  
Vol 264 (3) ◽  
pp. G399-G406
Author(s):  
M. E. Presti ◽  
J. D. Gardner
Keyword(s):  
Receptor Antagonist ◽  
G Protein ◽  
Therapeutic Potential ◽  
G Protein Coupled Receptors ◽  
Gastrointestinal Function ◽  
Receptor Antagonists ◽  
Cholecystokinin Receptor ◽  
Gastrointestinal Peptides ◽  
Complex Regulation ◽  
G Protein Coupled

Receptors for gastrointestinal peptides are all G protein-coupled receptors. Since the discovery that dibutyryl guanosine 3',5'-cyclic monophosphate was a cholecystokinin-receptor antagonist, a variety of receptor antagonists have been developed for a number of different gastrointestinal peptides. These antagonists have been useful in classifying receptors for gastrointestinal peptides and in elucidating complex regulation of gastrointestinal function. Some antagonists also have therapeutic potential. Based on the receptors with which they interact, gastrointestinal peptides can be grouped into families, and, in general, a given receptor antagonist is specific for a given family. This review covers the different families of gastrointestinal peptides and the major antagonists that exist for each family.

Bradykinin B2 receptor antagonists: development and applications

1995 ◽  
Vol 73 (7) ◽  
pp. 787-790 ◽  
Author(s):  
John M. Stewart
Keyword(s):  
G Protein ◽  
Biomedical Research ◽  
Clinical Applications ◽  
G Protein Coupled Receptors ◽  
Bradykinin Receptors ◽  
Receptor Antagonists ◽  
Bradykinin B2 Receptor ◽  
Kinin Receptors ◽  
Bradykinin Antagonists ◽  
G Protein Coupled

Most physiological and pathophysiological responses to bradykinin are mediated by G-protein-coupled receptors designated B2 receptors. Discovery of antagonists for these receptors has brought about a revolution in research in the kinin field. The chemistry and development of antagonists for B2 kinin receptors are discussed. Uses of the antagonists in biomedical research and potential clinical applications are presented.Key words: bradykinin antagonists, bradykinin inflammation, bradykinin receptors.

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