TABLE 1

Amino Acid Sequences and B1R Binding Affinities of BK and Related Peptides

PeptideRadiolabel complex–linkerSequenceKi (nM)Reference
BKArgProProGlyPheSerProPheArg5.7*29
KallidinLys 1Arg 2Pro 3Pro 4Gly 5Phe 6Ser 7Pro 8Phe 9Arg 107.4*29
[des-Arg10]kallidinLysArgProProGlyPheSerProPhe9.7*29
[Leu9,des-Arg10]kallidinLysArgProProGlyPheSerProLeu8.929
P03083Ga-DOTA-AhxLysArgProProGlyPheSerProLeu2.6 ± 0.723
P03034Ga-DOTA-dPEG2LysArgProHypGlyChaSerProLeu16.0 ± 1.923
B9858LysLysArgProHypGlyIgISerD-IgIOic10.124
B9958LysLysArgProHypGlyCpgSerD-TicCpg0.08925
P04158Ga-DOTA-dPEG2LysLysArgProHypGlyIgISerD-IgIOic1.5 ± 1.9
Z02090Ga-DOTA-dPEG2LysLysArgProHypGlyCpgSerD-TicCpg1.1 ± 0.8
  • * pEC50 (EC50 is the concentration of a drug needed to induce its half-maximal response).

  • pIC50 (IC50 is the concentration of an inhibitor needed to reduce response by half).