INTERACTION OF CLOZAPINE WITH THE HISTAMINE H-3 RECEPTOR IN RAT-BRAIN

被引:31
作者
RODRIGUES, AA [1 ]
JANSEN, FP [1 ]
LEURS, R [1 ]
TIMMERMAN, H [1 ]
PRELL, GD [1 ]
机构
[1] CUNY MT SINAI SCH MED,DEPT PHARMACOL,NEW YORK,NY 10029
关键词
HISTAMINE H-3 RECEPTOR; CLOZAPINE; NEUROLEPTIC; RAT BRAIN SLICES; I-125] IODOPHENPROPIT; H-3] 5-HT RELEASE;
D O I
10.1111/j.1476-5381.1995.tb14934.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
We examined possible interactions between neuroleptics and the histamine H-3 receptor and found an interaction of clozapine with this receptor. In competition binding experiments, using the H-3 antagonist, [I-125]-iodophenpropit, we observed a K-i of 236 +/- 87 nM. Functionally, clozapine was studied on the H-3-mediated inhibition of [H-3]-5-hydroxytryptamine ([H-3]-5-HT) release from fat brain cortex slices. Clozapine acts as an antagonist with an apparent K-B value of 79.5 nM.
引用
收藏
页码:1523 / 1524
页数:2
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