A potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor. |
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Authors: | X Emonds-Alt P Vilain P Goulaouic V Proietto D Van Broeck C Advenier E Naline G Neliat G Le Fur J C Brelière |
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Affiliation: | Sanofi Recherche, Montpellier, France. |
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Abstract: | SR 48968 is a potent and selective non-peptide antagonist of the neurokinin A (NK2) receptor. SR 48968 selectively inhibited neurokinin A binding to its receptor and was a competitive antagonist of neurokinin A-mediated contraction of different isolated smooth muscle preparations from various species including human. In vivo, the compound inhibited the bronchoconstriction induced by neurokinin A in guinea pigs. SR 48968 can be used to study the physiological or pathological role of neurokinin A and may be useful in the treatment of neurokinin A-dependent pathology. |
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