Corticotropin-releasing factor (CRF, nomenclature as agreed by the NC-IUPHAR subcommittee on Corticotropin-releasing Factor Receptors [7]) 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 corticotrophin-releasing hormone (CRH, P06850) and urocortin 1 (UCN, P55089). Binding to CRF receptors can be conducted using [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.

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) [11].

* Key recommended reading is highlighted with an asterisk

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* Hauger RL, Grigoriadis DE, Dallman MF, Plotsky PM, Vale WW, Dautzenberg FM. (2003) International Union of Pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ligands. Pharmacol Rev., 55: 21-26. [PMID:12615952]

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Tsatsanis C, Dermitzaki E, Venihaki M, Chatzaki E, Minas V, Gravanis A, Margioris AN. (2007) The corticotropin-releasing factor (CRF) family of peptides as local modulators of adrenal function. Cell. Mol. Life Sci., 64 (13): 1638-55. [PMID:17453142]

* Valentino RJ, Bangasser D, Van Bockstaele EJ. (2013) Sex-biased stress signaling: the corticotropin-releasing factor receptor as a model. Mol. Pharmacol., 83 (4): 737-45. [PMID:23239826]

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Ziegler CG, Krug AW, Zouboulis CC, Bornstein SR. (2007) Corticotropin releasing hormone and its function in the skin. Horm. Metab. Res., 39 (2): 106-9. [PMID:17326006]

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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 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