[18F]NCFHEB/[18F]Flubatine a potential PET marker of early Alzheimer`s disease
The nicotinic α4β2 acetylcholine receptors are an important target for diagnostic neuroimaging and drug development because of their involvement in learning and memory processes, neuropsychiatric diseases such as Alzheimer´s disease, Parkinsons´s disease, Tourette´s syndrome, epilepsy, autism, attention-deficit hyperactivity disorder, schizophrenia, and depression, as well as drug addiction and pain. In our group, a highly affine and selective α4β2 nAChR targeting radiotracer has been developed which is related on the structure of the alkaloid epibatidine. The two radiolabeled stereoisomers of norchloro-fluoro-homoepibatidine, (+)-[18F]flubatine and (-)-[18F]flubatine, were investigated in piglets in dynamic PET studies. (-)-[18F]flubatine proofed to possess radiotracer properties superior to the clinically used 2-[18F]F-A85380, and is currently assessed in man to quantitatively image α4β2nAChR in the living brain.
Department of Nuclear Medicine and Department of Psychiatry, University of Leipzig
Central Institute for Electronics, Research Center Juelich
Advanced Biochemical Compounds ABX GmbH, Radeberg
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