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

页码：2150 / 2152

页数：3

共 18 条

[1] Baumann M. H., 1994, Society for Neuroscience Abstracts, V20, P1028
[2] INTRAVENOUS ADMINISTRATION OF THE SEROTONIN AGONIST M-CHLOROPHENYLPIPERAZINE (MCPP) INCREASES EXTRACELLULAR SEROTONIN IN THE DIENCEPHALON OF AWAKE RATS
BAUMANN, MH
RUTTER, JJ
AUERBACH, SB
[J]. NEUROPHARMACOLOGY, 1993, 32 (12) : 1381 - 1386
[3] HIGH-AFFINITY BINDING OF [I-125] RTI-55 TO DOPAMINE AND SEROTONIN TRANSPORTERS IN RAT-BRAIN
BOJA, JW
MITCHELL, WM
PATEL, A
KOPAJTIC, TA
CARROLL, FI
LEWIN, AH
ABRAHAM, P
KUHAR, MJ
[J]. SYNAPSE, 1992, 12 (01) : 27 - 36
[4] BONNANO G, 1994, J NEUROCHEM, V63, P1163
[5] 1-(META-CHLOROPHENYL)PIPERAZINE (META CPP) INTERACTIONS WITH NEUROTRANSMITTER RECEPTORS IN THE HUMAN-BRAIN
HAMIK, A
PEROUTKA, SJ
[J]. BIOLOGICAL PSYCHIATRY, 1989, 25 (05) : 569 - 575
[6] META-CHLOROPHENYLPIPERAZINE AS A PROBE OF SEROTONIN FUNCTION
KAHN, RS
WETZLER, S
[J]. BIOLOGICAL PSYCHIATRY, 1991, 30 (11) : 1139 - 1166
[7] IDENTIFICATION AND DISTRIBUTION OF 5-HT3 RECEPTORS IN RAT-BRAIN USING RADIOLIGAND BINDING
KILPATRICK, GJ
JONES, BJ
TYERS, MB
[J]. NATURE, 1987, 330 (6150) : 746 - 748
[8] BINDING OF I-125 IODOVINYLTETRABENAZINE TO CNS VESICULAR MONOAMINE TRANSPORT SITES
KUNG, MP
CANNEY, DJ
FREDERICK, D
ZHUANG, Z
BILLINGS, JJ
KUNG, HF
[J]. SYNAPSE, 1994, 18 (03) : 225 - 232
[9] MURPHY DL, 1991, PHARMACOL REV, V43, P527
[10] PETTIBONE DJ, 1984, BIOCHEM PHARMACOL, V9, P1531

← 1 2 →