Corticotropin-releasing factor (CRF, nomenclature as agreed by the NC-IUPHAR subcommittee on Corticotropin-releasing Factor Receptors [11]) receptors are activated by the endogenous peptides corticotrophin-releasing hormone (CRH, P06850), a 41 amino-acid peptide, urocortin 1 (UCN, P55089), 40 amino-acids, urocortin 2 (UCN2, Q96RP3), 38 amino-acids and urocortin 3 (UCN3, Q969E3), 38 amino-acids. CRF₁ and CRF₂ receptors are activated non-selectively by CRH and UCN. CRF₂ receptors are selectively activated by UCN2 and UCN3. Binding to CRF receptors can be conducted using radioligands [¹²⁵I]Tyr⁰-CRF or [¹²⁵I]Tyr⁰-sauvagine with K_d values of 0.1-0.4 nM. CRF₁ and CRF₂ receptors are non-selectively antagonized by α-helical CRF, D-Phe-CRF-(12-41) and astressin. CRF₁ receptors are selectively antagonized by small molecules NBI27914, R121919, antalarmin, CP 154,526, CP 376,395. CRF₂ receptors are selectively antagonized by antisauvagine and astressin 2B.

A CRF binding protein has been identified (CRHBP, P24387) to which both corticotrophin-releasing hormone (CRH, P06850) and urocortin 1 (UCN, P55089) bind with high affinities, which has been suggested to bind and inactivate circulating corticotrophin-releasing hormone (CRH, P06850) [8,17].

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Subcommittee members: Richard L. Hauger (Chairperson) VA Healthcare System and Department of Psychiatry University of California San Diego 9500 Gilman Drive La Jolla CA 92093-0603 USA Frank M. Dautzenberg (Chairperson) CNS Research Johnson & Johnson Research & Development Turnhoutseweg 30, Discovery Research Center -020, Room 1L6 Beerse B-2340 Belgium Dimitri E. Grigoriadis Neurocrine Biosciences Inc. 10555 Science Center Dr. San Diego California 92121 USA Victoria B. Risbrough UC San Diego Department of Psychiatry 9500 Gilman Drive, MC 0603 La Jolla, CA 92093-0603 USA Rita J. Valentino Children's Hospital of Philadelphia 3615 Civic Center Blvd. Abramson Bldg., 402C Philadelphia, PA 19104

Other contributors: Thomas Steckler CNS Research Johnson & Johnson Research & Development Turnhoutseweg 30, Discovery Research Center -020, Room 1L6 Beerse B-2340 Belgium Wylie W. Vale (1941-2012) formally of The Salk Institute, La Jolla, California