Importance of phenolic address groups in opioid kappa receptor selective antagonists

被引：20

作者：

Thomas, JB

Fix, SE

Rothman, RB

Mascarella, SW

Dersch, CM

Cantrell, BE

Zimmerman, DM

Carroll, FI

机构：

[1] Res Triangle Inst, Res Triangle Pk, NC 27709 USA

[2] Eli Lilly & Co, Lilly Corp Ctr, Lilly Res Labs, Indianapolis, IN 46285 USA

[3] NIDA, Clin Psychopharmacol Sect, IRP, NIH, Baltimore, MD 21224 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 04期

关键词：

D O I：

10.1021/jm030467v

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In vitro characterization and comparison of JDTic, its dehydroxy analogue and nor-BNI, and its dehydroxy analogue demonstrates that the N-substituted 3,4-dimethyl-(3-hydroxyphenyl)-piperidine-derived antagonist, JDTic, relies more heavily on its phenol address group for affinity and antagonist activity relative to the corresponding naltrexone derived antagonists, nor-BNI. The structural flexibility of the former class of compound relative to the latter is postulated to underlie the difference.

引用

页码：1070 / 1073

页数：4

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