Corticotropin-releasing hormone receptor type 1 (CRHR1)

Corticotropin-releasing hormone receptor 1 (CRHR1) is a membrane-bound G protein-coupled receptor of the class B secretin family, composed of 7 transmembrane helices. Primarily found in the brain, pituitary, and other tissues, it is activated by corticotropin-releasing hormone (CRH) and related peptides, initiating a cascade that regulates the neuroendocrine, behavioral, and immune responses to stress, notably by activating the hypothalamic–pituitary–adrenal (HPA) axis via cAMP and other signaling pathways. CRHR1 is a major molecular target in research and development for stress, anxiety, depression, and several other disorders, though therapeutic development has been challenging, mostly due to difficulties in achieving receptor selectivity, CNS penetration, and adequate safety profile.

Other names

CRHR1CRF1 receptorCRF1RCorticotropin-releasing factor receptor 1Corticotropin-releasing hormone receptor type 1

Antagonists block CRHR1 and inhibit binding/activation by corticotropin-releasing factor (CRF) and related peptides (urocortins), suppressing downstream signaling (e.g. cAMP production, stress response). Agonists (less clinically relevant): stimulate CRHR1, activating HPA axis and stress response pathways.