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Anderson IM, Clark L, Elliott R, Kulkarni B, Williams SR, Deakin JF: 5-HT (2C) receptor activation by m-chlorophenylpiperazine detected in humans with fMRI. Neuroreport. 2002 Aug 27;13(12):1547-51. 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. |
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