Effects of SR 48968 on the neuropeptide gamma-induced contraction of the human isolated bronchus.
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.
Qian
Y
Y
Faculté de Médecine Paris-Ouest, Paris, France.
Advenier
C
C
Naline
E
E
Bellamy
J F
JF
Emonds-Alt
X
X
D001549:Benzamides / Q000494:pharmacology*; D001980:Bronchi / Q000187:drug effects* / Q000502:physiology; D016084:Bronchoconstriction / Q000187:drug effects*; D046508:Culture Techniques; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006020:Glycopeptides / Q000494:pharmacology; D006801:Humans; D010446:Peptide Fragments / Q000494:pharmacology*; D010880:Piperidines / Q000494:pharmacology*; D018039:Receptors, Tachykinin / Q000037:antagonists & inhibitors*; D015320:Tachykinins / Q000494:pharmacology*; D013820:Thermolysin / Q000037:antagonists & inhibitors
D001549:Benzamides; D006020:Glycopeptides; D010446:Peptide Fragments; D010880:Piperidines; D018039:Receptors, Tachykinin; D015320:Tachykinins; C059905:tachykinin neuropeptide gamma; C073839:SR 48968; D013820:Thermolysin; C008890:phosphoramidon