Table 2.

Relative potency of CRFR antagonists

Compound	Peptides	HEK-mCRFR2β cells		HEK-rCRFR1 cells
		cAMP (1 μM antag.)/ cAMP (1 nM Svg)*	cAMP (Svg + antag.)/ cAMP (Svg)†	cAMP (1 μM antag.)/ cAMP (1 nM oCRF)*	cAMP (oCRF + antag.)/ cAMP (oCRF)†
1	[dPhe11,His12]Svg(11-40)	0.004  ±  0.001	0.42  ±  0.02a	0.04  ±  0.01	0.73  ±  0.07b
2	[dPhe11]Svg(11-40)	0.005  ±  0.001	0.71  ±  0.04	0.07  ±  0.01	0.75  ±  0.13
3	Astressin	0.004  ±  0.001	0.57  ±  0.04	0.10  ±  0.02	0.11  ±  0.03
5	[dPhe11]rUcn(11-40)	0.011  ±  0.003	0.57  ±  0.06	0.07  ±  0.01	0.18  ±  0.03
6	α-Helical CRF(9-41)	0.007  ±  0.004	0.67  ±  0.02	0.16  ±  0.02c	0.58  ±  0.05
7	[dPhe11,Glu12]rUcn(11-40)	0.004  ±  0.001	0.61  ±  0.02	0.22  ±  0.05c	0.42  ±  0.11
8	Svg(11-40)	0.005  ±  0.001	0.76  ±  0.02	0.14  ±  0.02c	0.76  ±  0.16
9	[dPhe12,Nle21,38]h/rCRF(12-41)	0.007  ±  0.002	0.87  ±  0.08	0.06  ±  0.01	0.33  ±  0.08
10	[dLeu11]Svg(11-40)	0.008  ±  0.002	0.75  ±  0.06	0.22  ±  0.04c	0.92  ±  0.16
11	Cyclo(29–32)[dPhe11,Glu29,Lys32]rUcn(11-40)	0.005  ±  0.001	0.89  ±  0.01	0.10  ±  0.06	0.78  ±  0.10
12	[dLeu11,Glu12]rUcn(11-40)	0.009  ±  0.002	0.81  ±  0.06	0.23  ±  0.04c	0.56  ±  0.05
13	[dPhe12]oCRF(12-41)	0.008  ±  0.003	0.92  ±  0.07	0.05  ±  0.01	0.89  ±  0.07
14	oCRF	—	—	1.00	1.00
4	Svg	1.00	1.00	—	—
	Control without peptide	0.004  ±  0.001		0.01  ±  0.003

Statistically significant differences between the relative potencies of the peptides: a, P < 0.001 vs. 6, 9, 10, 11, 12, and 13; b, P ≤ 0.001 vs. 3 and 5. Statistically significant differences between the relative agonist activities of the peptides: c, P > 0.001 vs. control without peptide. 

^*The ratio of cAMP production of transfected HEK cells stimulated by antagonist or Svg or oCRF served as measure of the intrinsic activity. 

^†The relative potency determined by the effect of 10 nM (mCRFR2β) or 1 μM (rCRFR1) CRFR antagonist on the cAMP production stimulated by 1 nM Svg (mCRFR2β) or 1 nM oCRF (rCRFR1).