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

Neuroreport
M H BaumannJ K Staley

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]3 beta-(4-iodophenyl)tropan-2 beta-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.

Citations

Jun 17, 2010·Psychopharmacology·Reem K JanBruce R Russell
Mar 13, 2002·Pharmacology, Biochemistry, and Behavior·Richard B Rothman, Michael H Baumann
Aug 7, 2002·Pharmacology & Therapeutics·Richard B Rothman, Michael H Baumann
Jun 12, 2003·Psychiatry Research·George I PapakostasMaurizio Fava
Mar 12, 2004·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·George I PapakostasMaurizio Fava
Dec 18, 2008·Experimental and Clinical Psychopharmacology·Richard B RothmanMichael H Baumann
Jun 19, 2007·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Roland F StaackBurkhard Rolf
Sep 6, 2008·Progress in Brain Research·Richard B RothmanMichael H Baumann
Dec 24, 2002·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Neera GhaziuddinJohn Greden
Oct 11, 2012·Nature Reviews. Neuroscience·Roger K PitmanIsrael Liberzon
Nov 21, 2000·Annals of the New York Academy of Sciences·M H BaumannR B Rothman
Nov 4, 2017·Pharmacology & Therapeutics·Laura HondebrinkRemco H S Westerink

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