INHIBITION OF IGE-MEDIATED N-ACETYLGLUCOSAMINIDASE AND SEROTONIN RELEASE FROM RAT BASOPHILIC LEUKEMIA-CELLS (RBL-2H3) BY TENIDAP - A NOVEL ANTIINFLAMMATORY AGENT

被引：16

作者：

CONKLYN, MJ

KADIN, SB

SHOWELL, HJ

机构：

[1] PFIZER INC,DIV CENT RES,DEPT IMMUNOL & INFECT DIS,GROTON,CT 06340

[2] PFIZER INC,DIV CENT RES,DEPT MED CHEM,GROTON,CT 06340

来源：

INTERNATIONAL ARCHIVES OF ALLERGY AND APPLIED IMMUNOLOGY | 1990年 / 91卷 / 04期

关键词：

D O I：

10.1159/000235143

中图分类号：

R392 [医学免疫学];

学科分类号：

100102 ;

摘要：

Tenidap [(Z)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1 H-indole-1 -carbox-amide] is a novel anti-inflammatory compound of the oxindole class that currently is undergoing clinical evaluation in man. Here we demonstrate that tenidap inhibits (IC50 = ~10μM) IgE-mediated secretion of granule constituents from the rat mast cell tumor line RBL-2H3. The inhibitory effect is rapid in onset, readily reversible, and appears to be unique when compared to a representative selection of other acidic (carboxylic acids, pyrazoles and oxicams) nonsteroidal anti-inflammatory compounds. © 1990 S. Karger AG, Basel.

引用

页码：369 / 373

页数：5

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