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Effects of SR 48968 on the neuropeptide gamma‐induced contraction of the human isolated bronchus
Author(s) -
Qian Y.,
Advenier C.,
Naline E.,
Bellamy JF,
EmondsAlt X.
Publication year - 1994
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/j.1472-8206.1994.tb00781.x
Subject(s) - phosphoramidon , neurokinin a , endocrinology , medicine , substance p , neuropeptide , contraction (grammar) , neprilysin , receptor , antagonist , agonist , bronchus , tachykinin receptor , neurokinin b , biology , chemistry , endothelin receptor , biochemistry , respiratory disease , lung , enzyme
Summary— Neuropeptide gamma (NPγ) 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. NPγ was 3.31‐fold more potent than NKA. Contractile response curves to NPγ were shifted to the right and maximal responses reduced by the non‐peptide NK 2 ‐receptor antagonist, SR 48968. The pK B of SR 48968 (8.94 ± 0.18, n = 15), calculated according to Kenakin (1987) was very close to that reported for [Nle 10 ]‐NKA (4–10), a specific agonist of neurokinin NK 2 ‐receptors (8.86 ± 0.13, n = 13), suggesting that the contractile effects of NPγ on the human isolated bronchus were mediated through NK 2A ‐receptors.