Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain

被引：35

作者：

Dominguez, E

Iyengar, S

Shannon, HE

Bleakman, D

Alt, A

Arnold, BM

Bell, MG

Bleisch, TJ

Buckmaster, JL

Castano, AM

Del Prado, M

Escribano, A

Filla, SA

Ho, KH

Hudziak, KJ

Jones, CK

Martinez-Perez, JA

Mateo, A

Mathes, BM

Mattiuz, EL

Ogden, AML

Simmons, RMA

Stack, DR

Stratford, RE

Winter, MA

Wu, ZP

Ornstein, PL

机构：

[1] Ctr Invest Lilly, Madrid 28108, Spain

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

[3] Allelix Biopharmaceut, Mississauga, ON L4V 1P1, Canada

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 13期

关键词：

D O I：

10.1021/jm0491952

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors. Their ester prodrugs 6 and 8 were orally active in three models of pain: reversal of formalin-induced paw licking, carrageenan-induced thermal hyperalgesia, and capsaicin-induced mechanical hyperalgesia.

引用

页码：4200 / 4203

页数：4

共 26 条

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