d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin, a potent antagonist of smooth muscle BK2 receptors and BK3 receptors

d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d‐Phe7‐BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding an...

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Veröffentlicht in:British journal of pharmacology 1991-04, Vol.102 (4), p.785-787
Hauptverfasser: Farmer, S.G., Burch, R.M., Kyle, D.J., Martin, J.A., Meeker, S.N., Togo, J.
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Sprache:eng
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Zusammenfassung:d‐Arg[Hyp3‐Thi5‐d‐Tic7‐Tic8]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d‐Phe7‐BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding and BK‐induced contraction, and 45Ca2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK3 receptor.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1991.tb12251.x