TABLE 2.
Inhibitory binding constants, Ki (nM), of representative CRF family ligands determined by competitive binding of PD-Svg or PS-Svg radioligands bound to either CRF1 or CRF2(b) receptor
Ranges given in parentheses correspond to 95% confidence limits; n = 3–6 per cell. Data reproduced from previous publications are indicated
| PD-Svg | PS-Svg | r/hCRF | rUcn 1 | mUcn 2 | mUcn 3 | Astressin | |
|---|---|---|---|---|---|---|---|
| PD-Svg radioligand bound to either CRF1 or CRF2(b) receptors | |||||||
| CRF1 | 4.4 (2.9–6.5) | 62 (29–140) | 19 (7–49) | 3.0 (2.0–4.5) | >300 | >300 | 0.47 (0.42–0.52) |
| CRF2(b) | 1.9 (1.3–2.7) | 28 (21–40) | 13 (2–16) | 4.3 (3.7–4.9) | 4.8 (3.3–7.0) | 120 (100–140) | 0.7 (0.2–3) |
| PS-Svg radioligand bound to either CRF1 or CRF2(b) receptors | |||||||
| CRF1 | 0.22 (0.18–0.27) | 0.75 (0.59–0.94) | 1 (0.2–5)a | 0.32 (0.14–0.77)b | >100b | >100b | 0.7 (0.3–2)a |
| CRF2(b) | 0.40 (0.38–0.42) | 3.6 (2.5–5.1) | 6 (2–20)a | 0.6 (0.1–3)b | 0.7 (0.1–3)b | 2 (0.8–4)b | 0.62 (0.49–0.78)a |