A novel κ opioid receptor binding inhibitor CJ-15, 208 (
I) was isolated from the fermentation broth of a fungus,
Ctenomyces serratus ATCC15502. The structure of
I was determined to be a cyclic tetrapeptide consisting of one tryptophan, one D-prohne, and two L-phenylalanine. Compound
I was a selective binding inhibitor for the κ opioid receptor: 47nM (IC
50) for κ, 260nM for μ, and 2, 600nM for δ. In the electrically-stimulated twitch response assay of rabbit vas deferens
I recovered the suppression by a κ agonist asimadoline with an ED
50 of 1.3μM, indicating that it is a κ antagonist.
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