IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F19/2019.4

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


Abstract

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.

Contents

This is a citation summary for Corticotropin-releasing factor receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

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Database links

Corticotropin-releasing factor receptors
http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=19
Introduction to Corticotropin-releasing factor receptors
http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=19
    Receptors
            CRF1 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=212
            CRF2 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=213

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