CRF Receptors

Corticotropin-releasing factor (CRF), also known as corticotropin-releasing hormone, is a major regulator of homeostasis, mediating the autonomic, behavioral and neuroendocrine responses to stress. CRF has also been suggested to play a role in cell growth and survival. To date, two types of CRF receptors have been cloned from several mammals: CRF₁ and CRF₂ receptors. Two splice variants of the CRF₂ receptor have been identified in rodents; CRF_2a and CRF_2b.

Targets | Receptor Data

Targets

CRF Receptor Target Files

CRF₁ Receptors (CRHR1)

CRF₂ Receptors (CRHR2)

CRF₂ Receptor Antagonists

Related Targets

Non-selective CRF Receptors
- Non-selective CRF Receptor Agonists

Receptor Data

CRF Receptor Data

Receptor Subtype	CRF₁	CRF_2a	CRF_2b
Transduction Mechanism	Activates G_s	Activates G_s	Activates G_s

Featured Compounds		K_i (nM)
Agonists	CRF (human, rat) (1151) Stressin I (1608)	11 1.5	44 224	38 224
Antagonists	NBI 27914 (1591) CP 154526 (2779) CP 376395 (3212) K 41498 (2070)	2 2.7 12 425	> 10000 > 10000 > 10000 0.66	- > 10000 > 10000 0.62

References

Perrin and Vale (1999) Corticotropin releasing factor receptors and their ligand family. Ann.N.Y.Acad.Sci. 885 312. Maciejewski-Lenoir et al (200) Selective impairment of corticotropin-releasing factor₁ (CRF₁) receptor-mediated function using CRF coupled to saporin. Endocrinology 141 498.