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1 Polish Journal of Chemistry

1 2003

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New Bradykinin Analogues Modified in Position 6 and 7 with Naphthylalanine

Prahl A., Derdowska I., Dawidowska O., Neubert K., Hartrodt B., Wierzba T., Juzwa W., Lammek B.

Polish Journal of Chemistry

2003

Vol. 77 / nr 7

881-887

We describe the synthesis and some pharmacological properties of eight new analogues of a previously synthesized bradykinin antagonist, D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser- D-Phe-Thi-Arg. Two peptides were designed by substitution of Ser6 with L-1- and L-2-naphthylalanine. In two further analogues this modification was combined with placement in position 7 of D-naphthylalanine residue. We also obtained four analogues by acylation of N-terminus of the peptides mentioned above with 1-adamantaneacetic acid. The activity of analogues was assessed by their ability to inhibit vasodepressor response to exogenous bradykinin (rat blood pressure test). Our results indicate that the modifications proposed decreased significantly the B2 antagonistic activity. Moreover, our earlier observation, suggesting that acylation of the N-terminus of many BK antagonists with bulky groups consistently improved the antagonistic potency, appears to be valid only for one pair of analogues.