DESENSITIZATION OF HISTAMINE-H1 RECEPTOR-MEDIATED CYCLIC-GMP PRODUCTION IN GUINEA-PIG LUNG

被引:8
作者
LEURS, R [1 ]
BROZIUS, MM [1 ]
JANSEN, W [1 ]
BAST, A [1 ]
TIMMERMAN, H [1 ]
机构
[1] FREE UNIV AMSTERDAM,FAC CHEM,DEPT PHARMACOCHEM,DE BOELELAAN 1083,1081 HV AMSTERDAM,NETHERLANDS
来源
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1992年 / 225卷 / 02期
关键词
HISTAMINE-H1; RECEPTOR; DESENSITIZATION; CGMP; LUNG (GUINEA-PIG); PROTEIN KINASE-C;
D O I
10.1016/0922-4106(92)90093-B
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Histamine H-1 receptor-mediated production of cGMP in guinea-pig lung tissue becomes rapidly desensitized after previous exposure to histamine. This desensitization is clearly concentration dependent and appears to be homologous. Responses to histamine are also inhibited by previous treatment with phorbol 12,13-dibutyrate. Yet, the time course of the inhibition is considerably slower and the maximal inhibition is significantly less compared to receptor desensitization. Moreover, the effects of the phorbol ester are not confined to H-1 receptor responses. Since the effects of receptor desensitization are also not prevented by several protein kinase C inhibitors, the development of homologous H-1 receptor desensitization is not dependent upon protein kinase C activation, but is caused by a yet unidentified mechanism.
引用
收藏
页码:137 / 141
页数:5
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