1-(m-chlorophenyl)piperazine (mCPP) interactions with neurotransmitter receptors in the human brain.
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.
Hamik
A
A
Department of Neurology, Stanford University Medical Center, CA 94305.
Peroutka
S J
SJ
D000328:Adult; D000368:Aged; D001921:Brain / Q000378:metabolism*; D005260:Female; D005625:Frontal Lobe / Q000378:metabolism; D005917:Globus Pallidus / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D010879:Piperazines / Q000378:metabolism*; D011869:Radioligand Assay; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000378:metabolism
D010879:Piperazines; D011942:Receptors, Adrenergic, alpha; D017981:Receptors, Neurotransmitter; D011985:Receptors, Serotonin; C015068:1-(3-chlorophenyl)piperazine