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Neuroreport. 2002 Aug 27;13(12):1547-51.

5-HT(2C) receptor activation by m-chlorophenylpiperazine detected in humans with fMRI.

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Neuroscience and Psychiatry Unit, The University of Manchester, UK.


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.

[Indexed for MEDLINE]

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