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Visualisation of 11C-flunitrazepam displacement in the brain of the live baboon

Abstract

THE presence of specific benzodiazepine receptors in the brain of rat1,2, baboon3 and man4,5 has been demonstrated in vitro. These receptors have also been observed in vivo for diazepam6 and flunitrazepam7. However in such experiments, although the radioactive ligand is injected in the living animal the demonstration of the presence of specific receptors requires brain tissue sampling for quantitative measurement in vitro. The fact that carbon-11 is a positron emitter with a half life of 20 min which can be used for very high specific activity labelling of drugs, raises the possibility of external detection of radioactivity in a living subject by positron emission tomography8,9. Using this new methodology the present study demonstrates te displacement of 11C-flunitrazepam by lorazepam in the brain of live baboons.

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COMAR, D., MAZIERE, M., GODOT, J. et al. Visualisation of 11C-flunitrazepam displacement in the brain of the live baboon. Nature 280, 329–331 (1979). https://doi.org/10.1038/280329a0

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