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 journalArticlepeer-review

48 Scopus citations

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 languageEnglish (US)
Pages (from-to)2150-2152
Number of pages3
JournalNeuroreport
Volume6
Issue number16
DOIs
StatePublished - Nov 1995
Externally publishedYes

Keywords

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

ASJC Scopus subject areas

  • Neuroscience(all)

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