A novel bombesin receptor antagonist selectively blocks the satiety action of peripherally administered bombesin

Pharmacol Biochem Behav. 1994 Jul;48(3):809-11. doi: 10.1016/0091-3057(94)90351-4.

Abstract

To investigate the effect of a new, specific antagonist for bombesin receptors on the satiating action of exogenous bombesin, adult male rats were adapted to a nondeprivation test regimen with daily access to a palatable liquid food. In a prefeeding paradigm, rats received intraperitoneal injections of the bombesin receptor antagonist, BW2258U89 (6.25, 25, 50, or 100 micrograms kg-1) or vehicle 20 min before, and then a second injection of either bombesin (4 micrograms kg-1), gastrin-releasing peptide (GRP; 16 micrograms kg-1), the C-terminal octapeptide of cholecystokinin (CCK-8; 4 micrograms kg-1), or vehicle 5 min before a 2-h feeding test. BW2258U89 pretreatment antagonized the satiating actions of bombesin and GRP18-27 in a very potent, dose-related manner, but did not antagonize the satiating action of CCK-8. These differential results with BW2258U89 are consistent with prior results showing the potency of this antagonist for bombesin receptor-mediated effects in visceral systems; in addition, they demonstrate the selectivity of the compound for the satiating actions of peripherally administered bombesin and bombesin-like peptides.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Bombesin / administration & dosage
  • Bombesin / antagonists & inhibitors*
  • Bombesin / pharmacology
  • Dose-Response Relationship, Drug
  • Eating / drug effects
  • Male
  • Oligopeptides / pharmacology
  • Peptide Fragments / antagonists & inhibitors
  • Peptide Fragments / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Bombesin / antagonists & inhibitors*
  • Satiety Response / drug effects*
  • Sincalide / antagonists & inhibitors
  • Sincalide / pharmacology

Substances

  • Oligopeptides
  • Peptide Fragments
  • Receptors, Bombesin
  • BW 10
  • neuromedin C
  • Sincalide
  • Bombesin