INHIBITORY EFFECTS OF EMEDASTINE DIFUMARATE ON HISTAMINE-RELEASE

被引：25

作者：

SAITO, T ^{[1
]}

HAGIHARA, A ^{[1
]}

IGARASHI, N ^{[1
]}

MATSUDA, N ^{[1
]}

YAMASHITA, A ^{[1
]}

ITO, K ^{[1
]}

MIO, M ^{[1
]}

TASAKA, K ^{[1
]}

机构：

[1] OKAYAMA UNIV,FAC PHARMACEUT SCI,DEPT PHARMACOL,OKAYAMA 700,JAPAN

来源：

JAPANESE JOURNAL OF PHARMACOLOGY | 1993年 / 62卷 / 02期

关键词：

EMEDASTINE DIFUMARATE; HISTAMINE RELEASE; SUBSTANCE-P; MAST CELL; INTRACELLULAR CA-2+;

D O I：

10.1254/jjp.62.137

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The inhibitory effects of emedastine difumarate on histamine release were studied in rat peritoneal mast cells. Emedastine significantly inhibited substance P (SP)-induced histamine release at concentrations above 10(-9) M in the presence of extracellular Ca2+ and at concentrations above 10(-11) M in its absence. At concentrations of 10(-8) M or higher, emedastine significantly inhibited SP-induced Ca2+ release from intracellular Ca stores and SP-induced Ca-45 uptake into mast cells. Emedastine also inhibited passive peritoneal anaphylaxis in rats and guinea pigs. We conclude that the clinical antiallergic effects of emedastine involve the inhibition of histamine release and that this inhibition is mediated by the inhibition of Ca2+ release from intracellular Ca stores and the inhibition of Ca2+ influx into mast cells.

引用

页码：137 / 143

页数：7

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