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d ‐Arg[Hyp 3 ‐Thi 5 ‐ d ‐Tic 7 ‐Tic 8 ]‐bradykinin, a potent antagonist of smooth muscle BK 2 receptors and BK 3 receptors
Author(s) -
Farmer S.G.,
Burch R.M.,
Kyle D.J.,
Martin J.A.,
Meeker S.N.,
Togo J.
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb12251.x
Subject(s) - bradykinin , antagonist , chemistry , radiochemistry , receptor , biochemistry
d ‐Arg[Hyp 3 ‐Thi 5 ‐ d ‐Tic 7 ‐Tic 8 ]‐bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK‐induced contraction in guinea‐pig ileum, being markedly more potent than d ‐Phe 7 ‐BK analogues as a BK 2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK 2 antagonists, inhibited BK binding and BK‐induced contraction, and 45 Ca 2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK 3 receptor.