Target intelligence / Profile preview

Corticotropin-releasing factor receptor 2 (CRF2) (CRF2)

Target
CRF2
Molecular classification
G protein-coupled receptor, Class B GPCR, Secretin receptor family
01

Overview

The Corticotropin-releasing factor receptor 2 (CRF2) is a member of the Class B G protein-coupled receptor family, primarily recognized for its role in the physiological response to stress and the maintenance of homeostasis (Source: UniProt Q13324). Unlike the closely related CRF1 receptor, which is the primary mediator of the hypothalamic-pituitary-adrenal (HPA) axis, CRF2 is activated predominantly by urocortins 2 and 3 and is expressed in both the brain and peripheral tissues like the heart and skeletal muscle (Source: PubMed PMID: 15740626). In the cardiovascular system, CRF2 activation promotes vasodilation and increases cardiac contractility, making it a target of interest for treating acute heart failure (Source: PubMed PMID: 21145459). Centrally, CRF2 signaling is involved in modulating anxiety-like behaviors and suppressing appetite, though its effects can be complex and sometimes oppose those of CRF1 (Source: PubMed PMID: 12662345). Therapeutic development has focused on CRF2 agonists for cardiovascular and metabolic benefits, while antagonists are investigated for their potential to treat stress-induced gastrointestinal and psychiatric disorders (Source: PubMed PMID: 25108367).

Other names
CRHR2CRH-R2Corticotropin-releasing hormone receptor 2CRF-R2CRFR2
02

Mechanism of action

Agonism of the receptor typically couples to Gs proteins, stimulating adenylyl cyclase and increasing intracellular cAMP levels, which mediates downstream physiological effects like vasodilation and positive inotropy.

03

Biological functions

Signal transductionStress response regulationCardiovascular homeostasisGastrointestinal motility regulationAppetite suppressionThermoregulation
04

Disease associations

Heart failureAnxiety disordersDepressionIrritable bowel syndromeObesitySarcopenia
05

Safety considerations

Cardiovascular instability (hypotension or tachycardia)Complex modulation of anxietyMetabolic shifts
06

Interacting drugs

Urocortin 2

5 more in the full profile.

07

Biomarkers

Circulating levels of Urocortin 2Circulating levels of Urocortin 3CRF-induced cAMP production

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