1-(m-chlorophenyl)piperazine (mCPP) interactions with neurotransmitter receptors in the human brain

Biol Psychiatry. 1989 Mar 1;25(5):569-75. doi: 10.1016/0006-3223(89)90217-5.


The affinity of 1-(m-chlorophenyl)piperazine (mCPP) for 11 neurotransmitter receptor binding sites was determined in human brain membranes. mCPP is essentially equipotent at all 5-hydroxytryptamine (5-HT) receptor subtypes (IC50 values ranging from 360 to 1300 nM). The drug displays similar affinity (IC50 = 570 nM for alpha 2-adrenergic receptors labeled for 3H-rauwolscine. mCPP is less potent at alpha 1- and beta-adrenergic, dopamine, and muscarinic cholinergic receptors (IC50 values 2500-24,000 nM). mCPP is inactive at both benzodiazepine receptors and the 5-HT uptake sites at concentrations below 100,000 nM. These data demonstrate that mCPP displays similar potency for multiple neurotransmitter receptor binding sites in human brain.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Aged
  • Brain / metabolism*
  • Female
  • Frontal Lobe / metabolism
  • Globus Pallidus / metabolism
  • Humans
  • Kinetics
  • Male
  • Middle Aged
  • Piperazines / metabolism*
  • Radioligand Assay
  • Receptors, Adrenergic, alpha / metabolism
  • Receptors, Neurotransmitter / metabolism*
  • Receptors, Serotonin / metabolism


  • Piperazines
  • Receptors, Adrenergic, alpha
  • Receptors, Neurotransmitter
  • Receptors, Serotonin
  • 1-(3-chlorophenyl)piperazine