Corticotropin-Releasing Factor GPCR Family Subtypes and Products

What Are Corticotropin-Releasing Factor Receptors?

Corticotropin-releasing factor receptors (CRFRs) are a family of G protein-coupled receptors (GPCRs) comprised of two receptor types: CRF1 and CRF2. CRFRs play an important role in the activation of the autonomic stress response. CRFRs bind corticotropes, secreting adrenocorticotropic hormones, and as a result, activating the hypothalamic-pituitary-adrenal axis, which is part of the fight-or-flight response. Constant activation of CRFRs have also been shown to have an impact on the development of anxiety and learning impairments from early life to adulthood.

Corticotropin-Releasing Factor Receptor Information

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Hypothalamic corticotropin releasing hormone (CRH) exerts its diverse physiological actions via cell surface G protein-coupled CRH receptors (CRHRs), of which two subtypes (CRHR1 and CRHR2) have been identified. CRH regulates pituitary ACTH secretion and mediates behavioral and autonomic responses to stress. Overproduction of CRH and stress system abnormalities are associated with psychiatric diseases such as depression, anxiety, eating disorders, and addiction. CRHR1 is expressed in pituitary corticotrophs and the brain. CRH binds to CRHR1 with high affinity, and activation of CRHR1 by CRH increases cAMP intracellular levels and activates protein kinase A. CRHR1 also couples to activation of MAPK as well as protein kinase C in an isoenzyme-specific manner. Selective CRHR1 antagonists offer new possibilities for the treatment of anxiety and depression.

CRF2 is expressed in the brain, blood vessels and intestine. CRF plays an integral role in the coordinating endocrine and behavioral responses to stress as well as in the pathophysiology of several neurophsychiatric diseases such as depression, anxiety and addiction. CRF2 is involved in stress responses, cardiovascular function and gastric motility. Recent clinical data suggest that CRF- related agents may be promising in the treatment of various endocrine, psychiatric, neurologic and inflammatory diseases. CRF2 agonists may be useful in the treatment of upper-GI inflammatory diseases.

Corticotropin-Releasing Factor Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
Corticotrophin-Releasing FactorCRF1humanHEK293TC1040DC1040MC1040
CRF1humanHEK293T Gαqi5CG1040DCG1040MCG1040