Effects of SR 48968 on the neuropeptide gamma-induced contraction of the human isolated bronchus |
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Authors: | Y. Qian C. Advenier E. Naline JF Bellamy and X. Emonds-Alt |
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Affiliation: | Fucultéde Médecine Paris-Ouest, 15, rue de l'Ecole de Médecine, F-75270 Paris Cedex 06;Centre Médicochirurgical du Val d'Or, Saint Cloud;SANOFI Recherche, 184, rue du Professeur Blayac, 34184 Montpellier Cedex 04, France |
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Abstract: | 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 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 NPγ on the human isolated bronchus were mediated through NK2A-receptors. |
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Keywords: | SR 48968 neuropeptide gamma (NPγ) neurokinin NK2-receptor human isolated bronchi |
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