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Vol. 288, Issue 2, 729-734, February 1999
The Clayton Foundation Laboratories for Peptide Biology, Salk
Institute for Biological Studies, La Jolla, California
The characteristics of a high-affinity antagonist radioligand are
compared with those a high-affinity agonist in binding to the cloned
corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2) and to the native receptors that exist in rat cerebellum and
brain stem. The relative potencies of CRF antagonists and agonists
to the two types of cloned CRF receptors overexpressed stably in
Chinese hamster ovary cells are determined using the antagonist radioligand 125I-
[DTyr1]astressin (Ast*), and the agonist
radioligand, 125I -[Tyr0]rat urocortin
(Ucn*). The inhibitory binding constants
(Ki) of astressin and urocortin are 1 to 2 nM for all receptors and are independent of which radioligand is
employed. Astressin binds with high affinity to the native
cerebellar/brain stem receptor and relative potencies of selected CRF
analogs determined with Ast* on the native receptor are similar to
those obtained for the cloned CRF-R1. The specific binding of Ast* to
endogenous brain receptors is greater than that of Ucn*, resulting in
more sites being detected by the antagonist than by the agonist. In contrast to another CRF agonist, the binding of Ucn* to the cloned receptors is relatively insensitive to guanyl nucleotides at both 20°C and 37°C; however, its binding to the native receptor is displaced by guanyl nucleotides at 37°C and, to a lesser degree, at
20°C. As expected, the binding of the antagonist Ast* is not affected
by guanyl nucleotides. 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.
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