Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor

被引：37

作者：

McDonnell, ME

Zhang, SP

Dubin, AE

Dax, SL

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, Spring House, PA 19477 USA

[2] Johnson & Johnson Pharmaceut Res & Dev, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(02)00127-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using a 'directed' iodination procedure, novel iodo-resiniferatoxin congeners were synthesized from 4-acetoxy-3-methoxyphenylacetic acid and resiniferinol- 9.13,14-ortho-phenylacetate (ROPA). The 2-iodo-4-hydroxy-5-methoxyphenlacetic acid ester of resiniferinol 5 displayed high affinity binding (K-i=0.71 nM) for the human vanilloid VR1 receptor and functioned as a partial agonist. (C) 2002 Elsevier Science Ltd. All rights reserved.

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收藏

页码：1189 / 1192

页数：4

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