[11C]2-2-(Dimethylaminomethyl)phenylthio)-5-fluorophenylamine
- PMID: 20641346
- Bookshelf ID: NBK23143
[11C]2-2-(Dimethylaminomethyl)phenylthio)-5-fluorophenylamine
Excerpt
A number of neuropsychiatric disorders, including major depression, schizophrenia, Alzheimer’s disease, and Parkinson’s disease (1-3), involve a dysfunction of the brain’s serotonin system. The serotonergic neurons – present in large areas of the brain, including the hypothalamus, thalamus, and cerebral cortex – bear a protein called ‘serotonin transporter’ (SERT) (4).
The SERT is a specific marker for the number and integrity of presynaptic terminals of serotonin-producing neurons. It regulates neurotransmission by removing released serotonin from the extracellular space back into the presynaptic neuron. Commonly prescribed antidepressants are selective serotonin reuptake inhibitors, and their effects are obtained through interaction with the SERT (5).
A variety of radioligands for positron emission tomography (PET) have been evaluated for imaging the SERT. The most recent include [11C]DASB, [11C]AFM, [11C]AFE, [11C]ADAM, [11C]HOMADAM. 2-(2-(Dimethylaminomethyl)phenylthio)-5-fluorophenylamine (AFA), a novel PET radioligand, can be labeled with either 11C or 18F. In vitro, it has shown rapid brain uptake kinetics as well as a high affinity for SERT, with lower affinities for the norepinephrine transporter (NET) and dopamine transporter (DAT).
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