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Mapping catechol-O-methyltransferase in vivo: initial studies with [18F]Ro41-0960
Y S Ding1, S J Gatley, J S Fowler
1Chemistry Dept., Brookhaven National Laboratory, Upton, NY, USA. ding@simbrain.chm.bnl.gov
Life Sciences
|January 1, 1996
Summary
This study investigated [18F]Ro41-0960, a COMT inhibitor, for brain imaging. Findings indicate negligible brain uptake, suggesting limited central action and potential for peripheral COMT imaging.
Area of Science:
- Radiochemistry
- Neuroscience
- Pharmacology
Background:
- Ro41-0960 is a potent COMT inhibitor designed to cross the blood-brain barrier.
- It is structurally similar to Ro40-7592, a drug in clinical trials for Parkinson's disease.
Purpose of the Study:
- To evaluate the brain penetration and COMT inhibitory potential of [18F]Ro41-0960 using PET imaging.
- To determine if [18F]Ro41-0960 can serve as a radiotracer for studying COMT activity in vivo.
Main Methods:
- Positron emission tomography (PET) studies in baboons and mice using F-18 labeled Ro41-0960.
- Analysis of brain and plasma ratios, region of interest analysis, and HPLC metabolite profiling.
Main Results:
- Negligible uptake of [18F]Ro41-0960 in the baboon brain (brain to plasma ratio ~0.025).
- High uptake observed in kidneys, with F-18 primarily as unchanged [18F]Ro41-0960 in mice.
- Brain F-18 primarily localized to cerebral blood vessels, not brain tissue.
Conclusions:
- [18F]Ro41-0960 shows limited brain penetration, questioning its central pharmacological effects.
- The study introduces the first positron-emitting radiotracer for COMT.
- [18F]Ro41-0960 shows promise for in vivo imaging of peripheral COMT activity.