Frontiers in CNS Drug Discovery

Volume: 1

The Gastrin-Releasing Peptide Receptor as a Therapeutic Target in CNS Disorders

Author(s): Rafael Roesler, Flavio Kapczinski, Joao Quevedo, Felipe Dal Pizzol, Gilberto Schwartsmann

Pp: 390-399 (10)

DOI: 10.2174/978160805159511001010390

* (Excluding Mailing and Handling)


Gastrin-releasing peptide (GRP) is a mammalian counterpart of the amphibian peptide bombesin (BB) that stimulates cell proliferation, acts as a growth factor in the pathogenesis of many types of cancer, and regulates several aspects of neuroendocrine function. BB and GRP act by binding to the GRPpreferring type of BB receptor (GRPR, also known as BB2 receptor), a member of the superfamily of G-protein coupled membrane receptors. This review summarizes recent evidence from animal and human studies indicating that abnormalities in GRPR function in the brain might play a role in the pathogenesis of neurological and psychiatric disorders, and suggesting that BB, GRP, and GRPR antagonists might display therapeutic actions in central nervous system diseases.

Keywords: Bombesin-like peptides, gastrin-releasing peptide, gastrin-releasing peptide receptor, neuropeptides, neurological disorders

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