Effects of SR 48968 on the neuropeptide gamma-induced contraction of the human isolated bronchus

Fundam Clin Pharmacol. 1994;8(1):71-5. doi: 10.1111/j.1472-8206.1994.tb00781.x.

Abstract

Neuropeptide gamma (NP gamma) induced a contractile response of the human isolated bronchus which was potentiated by the neutral endopeptidase inhibitor, phosphoramidon, but was not modified by atropine and indomethacin. NP gamma was 3.31-fold more potent than NKA. Contractile response curves to NP gamma were shifted to the right and maximal responses reduced by the non-peptide NK2-receptor antagonist, SR 48968. The pKB of SR 48968 (8.94 +/- 0.18, n = 15), calculated according to Kenakin (1987) was very close to that reported for [Nle10]-NKA (4-10), a specific agonist of neurokinin NK2-receptors (8.86 +/- 0.13, n = 13), suggesting that the contractile effects of NP gamma on the human isolated bronchus were mediated through NK2A-receptors.

MeSH terms

  • Benzamides / pharmacology*
  • Bronchi / drug effects*
  • Bronchi / physiology
  • Bronchoconstriction / drug effects*
  • Culture Techniques
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Glycopeptides / pharmacology
  • Humans
  • Peptide Fragments / pharmacology*
  • Piperidines / pharmacology*
  • Receptors, Tachykinin / antagonists & inhibitors*
  • Tachykinins / pharmacology*
  • Thermolysin / antagonists & inhibitors

Substances

  • Benzamides
  • Glycopeptides
  • Peptide Fragments
  • Piperidines
  • Receptors, Tachykinin
  • Tachykinins
  • tachykinin neuropeptide gamma
  • SR 48968
  • Thermolysin
  • phosphoramidon