Table V.
PAR1 and PAR4 antagonists.
| PAR1 antagonists | Characteristic | Selectivity | Refs. |
|---|---|---|---|
| AFLARAA | Peptide with multiple alanine substitutions in both critical and non-critical residues of SFLLRN | Not available | 134 |
| Anti-PAR1 pepducin (P1pal-12) | Palmitoylated peptide based on the human PAR1 i3 loop | PAR1 selective | 135,136 |
| FR-171113 | Non-peptide PAR1 antagonist | PAR1 selective | 137 |
| RWJ-56110 | Peptide-mimetic PAR1 antagonists | PAR1 selective | 138–140 |
| RWJ-58259 | Indole-based SFLLR peptide mimetic | PAR1 selective | 140–142 |
| SCH-328725 | Non-peptide PAR1 antagonist based on the natural product himbacine | PAR1 selective | 137 |
| SCH-205831 | Non-peptide PAR1 antagonist based on the natural product himbacine | PAR1 selective | 143 |
| SCH-79797 | Non-peptide PAR1 antagonist based on the natural product himbacine | PAR1 selective | 144 |
| BMS-200261 | Peptide-mimetic PAR1 antagonists | PAR1 selective | 145,146 |
| BMS-200661 | Peptide-mimetic PAR1 antagonists | PAR1 selective | 146 |
| BMS-200260 | Peptide-mimetic PAR1 antagonists | PAR1 selective | 146 |
| tc-Y-NH2 | Trans-cinnamoyl (tc-) PAR4 peptide analogue | PAR4 selective | 147–149 |
| Anti-PAR4 pepducin (P4pal-10) | Palmitoylated peptide based on the human PAR4 i3 loop | Higher selectivity for PAR4 over PAR1 | 135,136, 147,150 |
| YD-3 | Non-peptide PAR4 antagonist | PAR4 selective | 138,151 |
| P20.1 | Monoclonal antibody directed against the N-terminal 20 amino acid portion of human PAR4 | PAR4 selective | 152 |