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; CRF2a and CRF2b.

Targets
Literature
Receptor Data

CRF Receptor Target Files

The tables below summarizes the properties of these receptors and include examples of selective ligands available from Tocris.

Literature for CRF Receptors

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:

  • Anterior Pituitary Regulation
  • Blood Pressure Regulation
  • Feeding and Appetite Regulation
  • Glucose Regulation
  • Peptide Hormone Processing
Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

CRF Receptor Data

Receptor Subtype CRF1 CRF2a CRF2b
Transduction Mechanism Activates Gs Activates Gs Activates Gs

Key Compounds Ki (nM)
Agonists CRF (human, rat) (1151)
Urocortin (rat) (1605)
Sauvagine (1609)
Stressin I (1608)
11
13
9.4
1.5
44
1.5
9.9
224
38
0.97
3.8
224
Antagonists Astressin (1606)
α-helical CRF 9-41 (1184)
NBI 27914 (1591)
CP 154526 (2779)
CP 376395 (3212)
K 41498 (2070)
2
17
2
2.7
12
425
1.5
5
> 10000
> 10000
> 10000
0.66
1
0.97
-
> 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.