Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin

  title={Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin},
  author={Juergen Gottowik and Val{\'e}rie Goetschy and St{\'e}phane Henriot and Eric A. Kitas and Gavin Kilpatrick},

Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of corticotropin-releasing factor receptors.

Because it is a high-affinity, specific CRF antagonist, astressin is eminently suitable as a ligand for detection and characterization of both endogenous and cloned CRF receptors.

Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): development of CRFR2beta-selective antisauvagine-30.

[DPhe11, His12]Svg(11-40), named antisauvagine-30, was the most potent and selective ligand to suppress agonist-induced adenylate cyclase activity in HEK cells expressing mCRFR2beta.

The neurobiology of urocortin

Functional, endogenously expressed corticotropin‐releasing factor receptor type 1 (CRF1) and CRF1 receptor mRNA expression in human neuroblastoma SH‐SY5Y cells

It is concluded that neuroblastoma SH‐SY5Y cells are endowed with nativeCRF1 receptors positively coupled to cAMP formation and constitute a useful functional model for the search of CRF1 selective compounds with potential anxiolytic/antidepressant activity.



125I-Tyro-sauvagine: a novel high affinity radioligand for the pharmacological and biochemical study of human corticotropin-releasing factor 2 alpha receptors.

The ability to label CRF2 alpha receptors with 125I-Tyr0-sauvagine in vitro represents a unique opportunity for the discovery of subtype-selective nonpeptide ligands, which would presumably target different aspects of CRF-mediated disorders.

Corticotropin-releasing factor receptors in the rat central nervous system: characterization and regional distribution.

Data from pharmacological studies indicated that the ability of a variety of CRF fragments and analogs to inhibit 125I-rCRF to olfactory bulb membranes correlates well with their reported relative potencies in stimulating pituitary adrenocorticotropic hormone secretion in vitro.

Cloning and characterization of human urocortin.

Synthetic human urocortin binds with high affinity to CRF receptor types 1, 2 alpha, and 2 beta, stimulates cAMP accumulation from cells stably transfected with these receptors, and acts in vitro to release ACTH from dispersed rat anterior pituitary cells.

Cloning and characterization of the human corticotropin-releasing factor-2 receptor complementary deoxyribonucleic acid.

The genomic structure and the corresponding complementary DNA (cDNA) sequence of the human CRF2 receptor is reported, and there is no evidence for the existence of aCRF2 beta receptor homolog in humans.

Localization of novel corticotropin-releasing factor receptor (CRF2) mRNA expression to specific subcortical nuclei in rat brain: comparison with CRF1 receptor mRNA expression

The anatomical distribution of CRF2 receptor mRNA indicates a role for this novel receptor in hypothalamic neuroendocrine, autonomic and general behavioral actions of central CRF and suggests distinctive functional roles for each receptor in CRF-related systems.

CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors.

  • D. SchulzR. Mansbach J. Heym
  • Biology, Psychology
    Proceedings of the National Academy of Sciences of the United States of America
  • 1996
It is proposed that a CRF antagonist such as CP-154,526 could affirm the role of CRF in certain psychiatric diseases and may be of significant value in the treatment of these disorders.

Cloning and characterization of a functionally distinct corticotropin-releasing factor receptor subtype from rat brain.

The isolation of a cDNA clone that encodes a second member of the corticotropin-releasing factor (CRF) receptor family, designated as the CRF2 receptor, demonstrates the presence of another functional CRF receptor, with significant differences in the pharmacological profile and tissue distribution from the CRFs.

Identification of a second corticotropin-releasing factor receptor gene and characterization of a cDNA expressed in heart.

Comparison of the amino acid sequences of CRF-RB and the previously cloned receptor reveals major differences in the N-terminal domain and in the extracellular loops, whereas the sequences of the intracellular loops are nearly identical.

Urocortin, a mammalian neuropeptide related to fish urotensin I and to corticotropin-releasing factor

This work characterized another mammalian member of the CRF family and localized its urotensin-like immunoreactivity to, and cloned related complementary DNAs from, a discrete rat midbrain region, and deduced a peptide that is related to u Rotensin and CRF, which is named urocortin, which could be an endogenous ligand for type-2 CRF receptors.