5-HT(2C) receptor activation by m-chlorophenylpiperazine detected in humans with fMRI.
Functional brain imaging using selective drug probes offers the opportunity to investigate regional neuronal activation linked to receptor stimulation or inhibition. In a placebo-controlled, balanced order design in eight male volunteers, the 5-HT(2c) agonist, m-chlorophenylpiperazine (mCPP) increased blood oxygen level dependent (BOLD) signal in the hypothalamus, caudate, pallidum, amygdala and pyriform cortex, anterior cingulate gyrus and choroid plexus (p < 0.001 uncorrected), areas with high density of 5-HT(2c) receptors. Activation in the hypothalamus correlated significantly with the prolactin response (p < 0.05 small volume corrected). In a subsequent Go/NoGo task, mCPP enhanced activation in right lateral orbitofrontal cortex (p < 0.05 small volume corrected). These findings suggest that pharmacoMRI is a potentially powerful tool for investigating neurotransmitter function in humans.
Anderson
I M
IM
Neuroscience and Psychiatry Unit, The University of Manchester, UK.
Clark
L
L
Elliott
R
R
Kulkarni
B
B
Williams
S R
SR
Deakin
J F W
JF
D001921:Brain / Q000000981:diagnostic imaging* / Q000502:physiology*; D006801:Humans; D008279:Magnetic Resonance Imaging; D010879:Piperazines / Q000008:administration & dosage*; D011597:Psychomotor Performance / Q000502:physiology; D011877:Radionuclide Imaging; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin / Q000378:metabolism*; D012701:Serotonin / Q000502:physiology; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage*
D010879:Piperazines; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D012701:Serotonin; C015068:1-(3-chlorophenyl)piperazine