THE SEROTONIN AGONIST M-CHLOROPHENYLPIPERAZINE (MCPP) BINDS TO SEROTONIN TRANSPORTER SITES IN HUMAN BRAIN

被引：49
|
作者：
BAUMANN, MH [1 ]
MASH, DC [1 ]
STALEY, JK [1 ]
机构：
[1] UNIV MIAMI,SCH MED,DEPT NEUROL,MIAMI,FL 33101
来源：
NEUROREPORT | 1995年 / 6卷 / 16期
关键词：
M-CHLOROPHENYLPIPERAZINE; 5-HT TRANSPORTERS; I-125] RTI-55; HUMAN BRAIN; D-FENFLURAMINE;
D O I：
10.1097/00001756-199511000-00013
中图分类号：
Q189 [神经科学];
学科分类号：
071006 ;
摘要：
THE serotonin (5-HT) agonist m-chlorophenylpiperazine (mCPP) is commonly used as a neuroendocrine challenge agent in humans, and it is well accepted that its mechanism of action involves direct stimulation of postsynaptic 5-HT receptors. In the present work, we demonstrate that mCPP also displays appreciable affinity (IC50 = 230 nM) for 5-HT transporters labeled by [I-125]3 beta-(4-iodophenyl)tropan-2 beta-carboxylic acid methyl ester ([I-125]RTI-55) in human occipital cortex. These data agree with reports that show mCPP increases extracellular 5-HT in rat brain via a mechanism involving 5-HT transporters. Our results indicate that mCPP may exhibit a presynaptic 5-HT action in man, and studies utilizing mCPP to assess 5-HT receptor sensitivity should be interpreted with caution.
引用
收藏
页码：2150 / 2152
页数：3
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