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Target intelligence / Profile preview
Corticotropin-releasing factor receptor 1 (CRF1/CRHR1)
- Target
- CRF1/CRHR1
- Molecular classification
- G protein-coupled receptor, Class B GPCR, Receptor
01
Overview
Corticotropin-releasing factor receptor 1 (CRF1/CRHR1) is a Class B G-protein coupled receptor and the primary receptor for corticotropin-releasing hormone/factor (CRH/CRF), a key mediator of endocrine, autonomic, behavioral, and immune responses to stress. Activation of CRF1 initiates rapid stress response via ACTH release, leading to glucocorticoid production by the adrenal cortex. It is a major drug target for neuropsychiatric disorders like depression and anxiety due to its central role in mediating stress responses.
- Other names
- CRFR1CRH-R1CRH receptor 1
02
Mechanism of action
Agonist or antagonist binding modulates intracellular signaling cascades (cAMP/PKA-CREB, MAPK/ERK, PKC) affecting gene transcription and cellular function.
03
Biological functions
Stress responseHPA axis regulationACTH releaseAnxiety modulationFear learningMemory modulationArousal regulationSignal transduction
04
Disease associations
DepressionAnxiety disordersNeuropsychiatric disorders
05
Safety considerations
Knockout mice lacking functional CRF1 die shortly after birth due to lung dysplasiaPotential for off-target effects due to widespread expressionComplex role in stress response requires careful consideration during drug development
06
Interacting drugs
CP-376395
2 more in the full profile.
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