Table 3.
Relative intrinsic activities and relative potencies of various CRF-like antagonists
| Antagonist | Rel. intrinsic activity,*
%
|
Rel. potency of
antagonist,† %
|
||
|---|---|---|---|---|
| rCRFR1 | mCRFR2β | rCRFR1 | mCRFR2β | |
| Ast | 9.8 (9.3–10.3) | 1.1 (0.9–1.2) | 86 (85–87) | 99 (99–98) |
| [Glu11]Ast | 8.4 (7.9–8.8) | 0.84 (0.67–1.0) | 86 (85–86) | 98 (99–98) |
| [Glu11,16]Ast | 9.1 (8.4–9.4) | 1.0 (0.76–1.3) | 83 (82–85) | 97 (96–97) |
| aSvg-30 | 6.5 (6.1–6.8) | 1.0 (0.9–1.1) | 2.0 (0–6.9) | 99 (98–99) |
| α-hel-CRF9–41 | 19 (18–20) | 1.4 (1.2–1.5) | 14 (13–15) | 97 (96–97) |
*
The intrinsic activity was determined by the stimulation of rCRFR1-HEK-293 cells and mCRFR2β-HEK-293 cells with 10 pM h/rCRF and Svg, respectively. Rel. intrinsic activity (%) = [cAMP (1 μM antagonist)/cAMP (10 nM agonist)] × 100.
†
Rel. potency (%) = 100 − [cAMP (1 nM agonist + 1 μM antagonist)/cAMP (1 nM agonist)] × 100. Numbers in parentheses are 95% confidence intervals.