IUPHAR/BPS Guide to Pharmacology CITE

Corticotropin-releasing factor receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

Frank M. Dautzenberg1, Dimitri E. Grigoriadis2, Richard L. Hauger3, Victoria B. Risbrough3, Thomas Steckler1, Wylie W. Vale4 and Rita J. Valentino5
  1. Johnson & Johnson Pharmaceutical Research & Development, Belgium
  2. Neurocrine Biosciences, USA
  3. University of California San Diego, USA
  4. Salk Institute, USA
  5. Children's Hospital of Philadelphia, USA


Corticotropin-releasing factor (CRF, nomenclature as agreed by the NC-IUPHAR subcommittee on Corticotropin-releasing Factor Receptors [30]) receptors are activated by the endogenous peptides corticotrophin-releasing hormone, a 41 amino-acid peptide, urocortin 1, 40 amino-acids, urocortin 2, 38 amino-acids and urocortin 3, 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.


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Database links

Corticotropin-releasing factor receptors
Introduction to Corticotropin-releasing factor receptors
            CRF1 receptor
            CRF2 receptor


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