Inhibitory binding constants for CRF and related compounds
| Compound | hCRF-R1 | rCRF-R2α | mCRF-R2β | |||
|---|---|---|---|---|---|---|
| Ast* | Ucn* | Ast* | Ucn* | Ast* | Ucn* | |
| Astressin | 2.0 nM1-a | 1.6 nM | 1.5 nM | 2.8 nM | 1.0 nM | 0.87 nM |
| (1.8–2.3) | (0.95–2.7) | (0.81–2.8) | (1.7–4.7) | (0.39–2.8) | (0.56–1.4) | |
| α-helical CRF(9–41) | 17 nM1-a | 49 nM | 5.0 nM | 4.1 nM | 0.97 nM | 0.81 nM |
| (13–21) | (29–82) | (2.6–10) | (2.5–6.7) | (0.43–2.2) | (0.52–1.3) | |
| [DPhe12,Nle21,38] | 56 nM1-a | 75 nM | 5.2 nM | 31 nM | 8.4 nM | 6.9 nM |
| r/hCRF(12–41) | (41–75) | (64–88) | (2.6–10) | (19–51) | (4.4–16) | (5.0–9.5) |
| r/hCRF | 11 nM | 5.2 nM | 44 nM | 13 nM1-c | 38 nM | 17 nM1-b |
| (8.4–15) | (2.9–9.3) | (26–75) | (7.2–22) | (21–67) | (10–29) | |
| rUcn | 1.3 nM | 0.79 nM | 1.5 nM | 0.58 nM1-c | 0.97 nM | 0.41 nM1-b |
| (0.71–2.6) | (0.43–1.4) | (0.74–3.2) | (0.42–0.82) | (0.46–2.0) | (0.26–0.66) | |
| sfUrotensin I | 3.1 nM | 2.8 nM | 9.8 nM | 3.4 nM1-c | 6.4 nM | 3.0 nM1-b |
| (2.4–4.0) | (2.4–3.3) | (5.5–17) | (2.6–4.4) | (3.8–11) | (1.8–4.8) | |
| Sauvagine | 9.4 nM | 11 nM | 9.9 nM | 1.4 nM1-c | 3.8 nM | 2.0 nM1-b |
| (7–13) | (8.8–13) | (4.4–22) | (1.1–1.8) | (2.3–6.2) | (1.1–3.6) | |