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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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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 Kd 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.
CRF1 receptor C
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CRF2 receptor C
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Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.
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].