Table 2.
Binding affinities and in vitro relative potencies
| hCRF R1 EC50 nM |
mCRF R2β EC50 nM |
Relative Potenciesa,b RAP assay |
|
|---|---|---|---|
| oCRFa | 1.2 (0.9 – 1.6) (Rivier et al., 2007) | 52 (21 – 128) (Rivier et al., 2007) | 1.0 |
| r/hCRFa | 1.0 (0.2 – 4.6) (Rivier et al., 2007) | 6.2 (2.0 – 19) (Rivier et al., 2007) | 1.0 (Gulyas et al., 1995) |
| hUcn 1a | 01. (0.1 – 0.2)* | 0.5 (0.3 – 0.7)* | ND |
| hUcn 2a | >100 (Lewis et al., 2001) | 0.5 (0.2 – 1.2) (Lewis et al., 2001) | ND |
| hUcn 3a | >100 (Lewis et al., 2001) | 13.5 (9.2 – 19.7) (Lewis et al., 2001) | ND |
| Sauvaginea | 0.9 (0.5 – 1.7) (Rivier et al., 2002) | 1.6 (0.7 – 3.8) (Rivier et al., 2002) | ND |
| Stressin1a | 1.7 (0.5 – 6.2) (Rivier et al., 2007) | 222 (137 – 361) (Rivier et al., 2007) | 1.1(0.53 – 2.2) (Rivier et al., 2007) |
| α-helical CRF(1–41)a | 2.5 (1.1 – 5.5)* | 0.4 (0.3 – 0.6) | 2.0 – 3.0 (Rivier et al., 1984) |
| α-helical CRF(9–41)b | 19 (5.5 – 66) (Rivier et al., 2002) | 1.1 (1.0 – 1.3) (Rivier et al., 2002) | 0.03(0.02–0.05) (Gulyas et al., 1995) |
| [DPhe12,Nle21,38]-hCRF(12–41)b | 19.2 (13.4 – 27.5) (Rivier et al., 2002) | 4.4 (2.0 – 9.6) (Rivier et al., 2002) | 1.0 (Gulyas et al., 1995) |
| [DPhe12,Nle21,38,CαMe Leu37]-hCRF(12–41)b | 2.7 (1.2–5.9)* 7.7 (6.0–9.8) |
2.8 (2.0–3.9)* 4.9 (3.7–6.5) |
1.0 (0.5 – 2.0) (Hernandez et al., 1993) |
| Astressinb | 0.7 (0.3 – 1.8) (Rivier et al., 2002) | 0.6 (0.5 – 0.8) (Rivier et al., 2002) | 32.5(12–82) (Gulyas et al., 1995) |
| Astressin Bb | 0.3 (0.1 – 0.8)* | 1.2 (0.9 – 1.6)* | 1.1 (0.50 – 2.5) (Rivier et al., 1999) |
| Astressin2-Bb | >500 (Rivier et al., 2002) | 1.3 (1.0 – 1.7) (Rivier et al., 2002) | ND |
| Anti-sauvagine 30b | 400 (Rivier et al., 2002) | 1.1 (0.6 – 2.2) (Rivier et al., 2002) | ND |
a
CRF agonists were tested in an in vitro assay measuring stimulation of ACTH release by rat anterior pituitary cells in culture (RAP assay) when using hCRF or oCRF as the standard compound (Gulyas et al., 1995; Rivier et al., 2007).
b
CRF antagonists were tested measuring alteration of CRF-induced release of ACTH by rat anterior pituitary cells in culture relative to that of [DPhe12,Nle21,38]-h/rCRF(12–41) as the standard compound (Hernandez et al., 1993).
*
Unpublished data; assay carried out by C. Miller under the supervision of Dr. M. Perrin.