CRF1 | CRF2 | ||||||
---|---|---|---|---|---|---|---|
Ki (Binding) | EC50 (cAMP) | Ki (Binding) | EC50 (cAMP) | ||||
nM | |||||||
mUcn 3 | >1000a | >1000a | 5.0b | 0.073b | |||
oCRF | 2.2c | 0.42c | 16d | 130d | |||
Stressin1-A | 1.7e | N.D.f | 222e | N.D.f |
↵ a Data are from murine CRF1 receptors expressed in COS-7 cells (Venihaki et al., 2004).
↵ b Data are from rat CRF2(a) receptors expressed in Chinese hamster ovary cells (Lewis et al., 2001).
↵ c Data are from rat CRF1 receptors expressed in human embryonic kidney cells (Rühmann et al., 1999).
↵ d Ki from rat olfactory bulb [CRF2(a) receptors]; EC50 from rat CRF2(b) receptors expressed in A7r5 cells (Hoare et al., 2005).
↵ e Data are from human CRF1 receptors and mouse CRF2(b) receptors expressed in Chinese hamster ovary cells (Rivier et al., 2007).
↵ f Although cAMP assays have not yet been performed (N.D.) for stressin1-A, it is similarly potent to oCRF in releasing adrenocorticotropin from dispersed anterior pituitary cells (a CRF1-mediated endpoint), and it does not reduce gastric emptying (10 μg/kg i.p.) or arterial blood pressure (10 μg/kg i.v.) in vivo (CRF2-mediated endpoints) at a dose that stimulates fecal output and diarrhea (CRF1-mediated endpoints) (Rivier et al., 2007).