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Appetite-Modifying Effects of Bombesin Receptor Subtype-3 Agonists

  • Ishita Deb Majumdar
  • H. Christian Weber
Chapter
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 209)

Abstract

Studies on bombesin-like peptides (BLP) and their respective mammalian receptors (Bn-r) have demonstrated a significant biological impact on a broad array of physiological and pathophysiological conditions. Pharmacological experiments in vitro and in vivo as well as utilization of genetic rodent models of the gastrin-releasing peptide receptor (GRP-R/BB2-receptor), neuromedin B receptor (NMB-R/BB1-receptor), and the bombesin receptor subtype-3 (BRS-3/BB3-receptor) further delineated their role in health and disease. All three mammalian bombesin receptors have been shown to possess some role in the regulation of energy balance and appetite and satiety. Compelling experimental evidence has accumulated indicating that the orphan BRS-3 is an important regulator of body weight, energy expenditure, and glucose homeostasis. BRS-3 possesses no high affinity to the endogenous bombesin-like peptides (BLP) bombesin, GRP, and NMB, and its endogenous ligand remains unknown. Recently, the synthesis of novel, selective high-affinity BRS-3 agonists and antagonists has been accomplished and has demonstrated that BRS-3 regulates energy balance independent of other established pathways. Accordingly, the availability of new BRS-3 selective agonists and antagonists will facilitate further elucidation of its role in energy homeostasis and provides a potential approach for the pharmacological treatment of obesity.

Keywords

Bombesin receptor subtype-3 Bombesin-like peptides Energy homeostasis Gastrin-releasing peptide Mammalian bombesin receptors Neuromedin B Obesity Synthetic BRS-3 agonist 

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Copyright information

© Springer-Verlag Berlin Heidelberg 2012

Authors and Affiliations

  1. 1.Section of GastroenterologyBoston University School of MedicineBostonUSA
  2. 2.Department of Medicine and Department of Pathology and Laboratory MedicineBoston University School of MedicineBostonUSA

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