Corticotropin-releasing factor (CRF) receptors type 1 (CRF 1 ) and type 2 (CRF 2 ) differ from each other in their pharmacological properties. The human and ovine CRF versions bind to CRF 1 receptors with significantly higher affinity than to CRF 2 receptors. Recently antisauvagine-30, an N-terminally truncated version of the CRF analog sauvagine, was characterized as a specific antagonist to mouse CRF 2B . We have synthesized the radiolabeled version 125 I-antisauvagine-30 and tested it for its affinity at human CRF 1 (hCRF 1 ), hCRF 2A , Xenopus CRF 1 (xCRF 1 ) and xCRF 2 receptors. In control binding studies 125 I-labeled hCRF, sauvagine and astressin were also bound to these receptors. 125 I-antisauvagine-30 exclusively bound to hCRF 2A and xCRF 2 but not to hCRF 1 and xCRF 1 receptors. 125 I-antisauvagine-30 binding to hCRF 2A and xCRF 2 receptors was saturable and of high affinity (hCRF 2A : K d =125 pM; xCRF 2 : K d =1.1 nM). In displacement binding experiments using 125 I-antisauvagine-30 as radioligand several CRF analogs bound to hCRF 2A and xCRF 2 receptors with similar rank orders as reported with other CRF radioligands. Finally, preliminary studies using 125 I-antisauvagine-30 binding to membrane homogenates prepared from different rat brain structures showed that the peptide bound specifically to brain areas expressing CRF 2 receptors. These data demonstrate that 125 I-antisauvagine-30 is the first high-affinity ligand to specifically label CRF 2 receptors.
Neuropharmacology – Elsevier
Published: Jan 1, 2001
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