Characterization of bombesin receptors in peripheral contractile organs

Br J Pharmacol. 1991 May;103(1):1141-7. doi: 10.1111/j.1476-5381.1991.tb12314.x.

Abstract

1 Guinea-pig and rat urinary bladders, rat stomach and the guinea-pig gall bladder, four isolated organs that show high sensitivity to bombesin, were used to characterize bombesin receptors in peripheral organs. 2 The order of potency of agonists was determined with several naturally occurring peptides of the bombesin series, namely bombesin (BBS), litorin (Lit), neuromedin B (NMB), the gastrin-releasing peptide (GRP 18-27), neuromedin C (NMC) and with some bombesin fragments. It was found that bombesin, neuromedin C, litorin and two bombesin fragments, BBS (6-14) and AcBBS (6-14) had similar activities in the four preparations, while neuromedin B and [Phe6]-neuromedin C were more active on the rat urinary bladder than on the other tissues. 3 The order of potency of agonists determined in the rat urinary bladder was as follows: BBS = NMB greater than Lit greater than NMC greater than [Phe6]NMC = GRP and it was found to be different from that observed in the other preparations: BBS greater than GRP = Lit greater than or equal to NMC much greater than NMB greater than [Phe6]NMC, suggesting the existence of two different bombesin receptors, BBS1 and BBS2. 4 This interpretation was convalidated by the finding that bombesin antagonists, namely Ac.GRP(20-26)OCH3 and Ac.GRP(20-26)OC2H5 reduced or blocked the effects of bombesin-related peptides on BBS2 receptor systems while being completely inactive on the rat urinary bladder (BBS1 system).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bombesin / pharmacology
  • Gallbladder / drug effects
  • Guinea Pigs
  • In Vitro Techniques
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / metabolism*
  • Peptides / pharmacology
  • Protease Inhibitors / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, Bombesin
  • Receptors, Neurotransmitter / drug effects
  • Receptors, Neurotransmitter / metabolism*
  • Stomach / drug effects
  • Urinary Bladder / drug effects

Substances

  • Peptides
  • Protease Inhibitors
  • Receptors, Bombesin
  • Receptors, Neurotransmitter
  • Bombesin