期刊
JOURNAL OF ANTIBIOTICS
卷 55, 期 10, 页码 847-854出版社
JAPAN ANTIBIOT RES ASSN
DOI: 10.7164/antibiotics.55.847
关键词
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A novel kappa 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-proline, and two L-phenylalanine. Compound I was a selective binding inhibitor for the kappa opioid receptor: 47 nM (IC50) for kappa, 260 nM for mu, and 2,600 nM for delta. In the electrically-stimulated twitch response assay of rabbit vas deferens I recovered the suppression by a kappa agonist asimadoline with an ED50 of 1.3 muM, indicating that it is a kappa antagonist.
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