CJ-15,208, a novel kappa opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502.
J Antibiot (Tokyo)
; 55(10): 847-54, 2002 Oct.
Article
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| MEDLINE
| ID: mdl-12523817
ABSTRACT
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 microM, indicating that it is a kappa antagonist.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores Opioides kappa
/
Arthrodermataceae
/
Antagonistas de Narcóticos
Límite:
Animals
Idioma:
En
Revista:
J Antibiot (Tokyo)
Año:
2002
Tipo del documento:
Article
País de afiliación:
Japón