Use of (-)-(18F)VAT as a Molecular Imaging Tool by PET

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(Last Updated On: October 21, 2017)
Molecular imaging tool

(-)-[18F]VAT as a molecular imaging tool used with PET in a neurodegenerative disease diagnosis. Image: Jin. H. et al., 2015

A team of brain researchers found a specialized molecular imaging tool while working on targeting a cellular process involved in neurodegeneration and cognitive dysfunction. This molecular imaging tool performs its job by binding to the transporter of the neurotransmitter acetylcholine, a mediator of the central nervous system.

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It was first realized that the biomarker vesicular acetylcholine transporter (VAChT) is the one involved in the loss of cholinergic neurons, a kind of nerve cells found in the cerebral cortex and other areas of the brain. Acetylcholine, a mediator of the central nervous system works either as an excitatory or as an inhibitory medium depending upon the environment.

Researchers were focusing on the inhibition of the cholinergic neurons, during which researchers evaluated a Positron Emission Tomology (PET) agent  (-)-[18F]VAT. This is a molecular imaging tool that leads to the breakdown of the neurons causing cognition.



Hongjun Jin, a researcher at the Department of Radiological Science at Washington University and the author of this study said that PET tracer for the vesicular acetylcholine transporter can be used to quantify the loss of cholinergic neurons its effect on the cognitive impairment in the patients with neurodegenerative disorders like Alzheimer’s disease, Parkinson’s disease, Huntington’s disease.

PET is a capable imaging tool for physiological processes at the cellular and molecular level. During this process, a scanning is carried out by injecting a radiotracer comprised of a minute amount of radioactive material (-)-[18F]VAT and the targeted molecular compound VAChT via an inhibitory pathway.

This study was carried out in a small group of rats and cynomolgus monkeys, where they were undergone with PET imaging using the molecular imaging agent (-)-[18F]VAT. The result of this study reveals the encouraging bio-distribution and exposure were below the acceptable limits. The imaging agent was highest in the striatum of the brain. It is stable, safe and capable of visualizing the VAChT. However, it is not yet approved for commercial use.

In conclusion, a PET molecular imaging tool for the VAChT like presynaptic markers can be a valuable tool for pre-clinical investigations of the cholinergic neurons and other biological processes based on the cholinergic neurotransmission and movement disorders like dystonia. However, a human trial of this molecular imaging tool is already in the way and with further validation procedures; it can be used to monitor the efficacy of cholinergic therapies in neurodegenerative disorders.

Reference:  Jin, H., Yue, X., Zhang, X., Li, J., Yang, H., Flores, H., … & Tu, Z. (2015). A promising F-18 labeled PET radiotracer (-)-[18F] VAT for assessing the VAChT in vivo. Journal of Nuclear Medicine, 56(supplement 3), 4-4.

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