Table 1 Sequences of novel BK analogs with N-terminal extensions compared to that of parent peptides in each category (italicized names)
Peptide | Position | Binding competition IC50 nM (95 % C.L.) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
−1 | 0 | 1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | 9 | ||
B2 receptor agonists | ||||||||||||
First parent peptide: BK | Arg | Pro | Pro | Gly | Phe | Ser | Pro | Phe | Arg-COOH | 8.2 (6.0–11.2) | ||
Second parent peptide: B-9972 | D-Arg | Arg | Pro | Hyp | Gly | Igl | Ser | Oic | Igl | Arg-COOH | 17.3 (13.3–22.4) | |
B-10666 = Cy7-B-9972 | Cy7 | D-Arg | Arg | Pro | Hyp | Gly | Igl | Ser | Oic | Igl | Arg-COOH | 598 (481–742) |
B2 receptor antagonists | ||||||||||||
Parent peptide: B-9430 | D-Arg | Arg | Pro | Hyp | Gly | Igl | Ser | D-Igl | Oic | Arg-COOH | 42.6 (20.0–90.8) | |
B-10665 = Cy7-B-9430 | Cy7 | D-Arg | Arg | Pro | Hyp | Gly | Igl | Ser | D-Igl | Oic | Arg-COOH | 25.7 (11.5–57.1) |