Comparative profile of novel potent bradykinin antagonists at human B-1 and B-2 receptors

We have undertaken a comparative pharmacological profile of novel bradykinin antagonists on human B-1 and B-2 receptor binding and functional assays. We found that there was an excellent correlation between binding and functional data for the compounds at the B-1 receptor. In general, although there was a good correlation between the binding and functional data at the B-2 receptor there was a greater degree of scatter in the correlation, particularly with compounds that possessed both B-1 and B-2 binding and antagonist activity. Of the compounds that were highly selective for the B-2 receptor, CP-0597 had high binding activity but showed an unexpectedly low functional potency in the human ileum. The reason for this discrepancy is unclear. In general we found that binding activity with both the B-1 and B-2 antagonist compounds correlated well with their functional activity.