CJ-15,208, a novel kappa opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502

被引：51

作者：

Saito, T

Hirai, H

Kim, YJ

Kojima, Y

Matsunaga, Y

Nishida, H

Sakakibara, T

Suga, O

Sujaku, T

Kojima, N

机构：

[1] Pfizer Pharmaceut Inc, Nagoya Labs, PGRD, Exploratory Med Sci, Nagoya, Aichi 4702393, Japan

[2] Pfizer Pharmaceut Inc, Nagoya Labs, PGRD, Discovery Pharmacol 1, Nagoya, Aichi 4702393, Japan

[3] Meijo Univ, Fac Pharm, Tempaku Ku, Nagoya, Aichi 4688503, Japan

来源：

JOURNAL OF ANTIBIOTICS | 2002年 / 55卷 / 10期

关键词：

D O I：

10.7164/antibiotics.55.847

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

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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页码：847 / 854

页数：8

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