CRF2 Receptor Antagonists Small Molecules and Peptides

The corticotropin-releasing factor (CRF) 2 receptor is a member of the corticotropin-releasing factor family of G-protein-coupled receptors that also includes CRF₁. Three functional splice variants have been identified for the mammalian CRF₂ receptor; CRF_2a, CRF_2b and CRF_2c. All three splice variants display different tissue distribution but the pharmacological and biological properties remain unchanged.

The physiological functions of CRF₂ receptors are currently unclear but activation of these receptors is known to induce anxiety and hypersensitivity to stress, and increase glucagon and insulin secretion from islet cells. The human gene encoding the CRF₂ receptor is localized on chromosome 17 (17q12-q22).