Photoactivatable peptides based on BMS-197525: A potent antagonist of the human thrombin receptor (PAR-1)

Article abstract of DOI:10.1016/S0960-894X(98)00730-6

Photoactivatable analogs of the human thrombin receptor (PAR-1) antagonist, N-trans-cinnamoyl-p-fluoroPhe-p-guandinoPhe-Leu-Arg-NH₂ (BMS- 197525), were prepared with benzophenone substitutions in the N-terminal, Leu, or Arg position. The analogs retained antagonist activity (with reduced potency); the tritium-labeled isotopomers are potential photoaffinity labels for the receptor. C-Terminal extension of the analogs with ornithine(biotin) did not significantly alter antagonist potency.