The serotonin agonist m-chlorophenylpiperazine (mCPP) binds to serotonin transporter sites in human brain

Michael H. Baumann; Deborah C. Mash; Julie K. Staley

doi:10.1097/00001756-199511000-00013

The serotonin agonist m-chlorophenylpiperazine (mCPP) binds to serotonin transporter sites in human brain

Michael H. Baumann
, Deborah C. Mash
, Julie K. Staley

Research output: Contribution to journal › Article › peer-review

Abstract

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 [¹²⁵I]3β-(4-iodophenyl)tropan-2β-carboxylic acid methyl ester ([¹²⁵I]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.

Original language	English
Pages (from-to)	2150-2152
Number of pages	3
Journal	NeuroReport
Volume	6
Issue number	16
DOIs	https://doi.org/10.1097/00001756-199511000-00013
State	Published - Nov 1995
Externally published	Yes

ASJC Scopus Subject Areas

General Neuroscience

Keywords

5HT transporters
Chlorophenylpiperazine
d-Fenfluramine
Human brain
[I]RTI-55

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10.1097/00001756-199511000-00013

Cite this

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title = "The serotonin agonist m-chlorophenylpiperazine (mCPP) binds to serotonin transporter sites in human brain",

abstract = "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 [125I]3β-(4-iodophenyl)tropan-2β-carboxylic acid methyl ester ([125I]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.",

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year = "1995",

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AU - Baumann, Michael H.

AU - Mash, Deborah C.

AU - Staley, Julie K.

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Y1 - 1995/11

N2 - 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 [125I]3β-(4-iodophenyl)tropan-2β-carboxylic acid methyl ester ([125I]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.

AB - 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 [125I]3β-(4-iodophenyl)tropan-2β-carboxylic acid methyl ester ([125I]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.

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KW - Chlorophenylpiperazine

KW - d-Fenfluramine

KW - Human brain

KW - [I]RTI-55

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The serotonin agonist m-chlorophenylpiperazine (mCPP) binds to serotonin transporter sites in human brain

Abstract

ASJC Scopus Subject Areas

Keywords

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