Abstract
The newly discovered bradykinin antagonists [Thi 5,8, D-Phe 7]Bradykinin, supplied by J.-M. Stewart and three other compounds, [D-Phe 7]BK, [Thi 5,8,D-Phe 7]Bradykinin and [Thi 6,9,D-Phe 8]Kallidin synthesized in our laboratory, were tested for their ability to antagonize bradykinin in four B 2 receptor systems, the guinea-pig ileum, the rabbit jugular vein, the dog carotid artery and the dog urinary bladder as well as against desArg 9-bradykinin in the rabbit aorta (a B 1 receptor system). [D-Phe 7]Bradykinin is a partial agonist, while [Thi 5,8, D-Phe 7]Bradykinin and [Thi 6,9,D-Phe 8]Kallidin are pure antagonists, the second one showing little BK-like activity on three of the four preparations. The kallidin analogue is more potent in all preparations than the bradykinin one. The two [Thi 5,8,D-Phe 7]BK (that supplied by J.-M. Stewart and that prepared in our laboratory) show very similar affinities in all preparations. The bradykinin analogue as well as the kallidin one are also active against desArg 9-bradykinin in the rabbit aorta, at concentrations similar to those active on B 2 receptor systems. The kinin antagonists are however specific for the kinins, since they do not interfere with the myotropic effects of angiotensin or substance P (SP) in the various preparations.
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