CLOZAPINE HAS SUBMICROMOLAR AFFINITY FOR 5-HT1A RECEPTORS IN HUMAN BRAIN-TISSUE

被引:64
作者
MASON, SL [1 ]
REYNOLDS, GP [1 ]
机构
[1] UNIV SHEFFIELD,DEPT BIOMED SCI,SHEFFIELD S10 2TN,S YORKSHIRE,ENGLAND
关键词
CLOZAPINE; 5-HT1A RECEPTORS; ANTIPSYCHOTIC DRUGS;
D O I
10.1016/0014-2999(92)90731-I
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The affinities of a range of antipsychotic drugs at human hippocampal 5-HT1A receptors, defined by specific [H-3]8-OH-DPAT binding, were determined. Clozapine demonstrated the highest affinity; all other antipsychotics studied demonstrated pK(i) values below 6.0. 5-HT1A receptors are found on cortical glutamatergic neurons, a dysfunction of which may occur in schizophrenia. Binding at this site indicates a possible mechanism contributing to the unique efficacy of clozapine in the treatment of some schizophrenic patients.
引用
收藏
页码:397 / 398
页数:2
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