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 [34]) 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 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.

Contents

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts. For further details see [8].

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