In August 2008, racemic tetrabenazine (3-(2-methylpropyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizin-2-one, (�)-TBZ) was approved for the treatment of chorea associated with Huntington's disease in USA. The primary pharmacological action of TBZ and its active metabolites, such as dihydrotetrabenazine (DTBZ), is to deplete the levels of monoamines within the central nervous system by inhibiting the human vesicular monoamine transporter 2 (VMAT2). Therefore, radiotracers derived from TBZ can be potential biomarkers of VMAT2 for positron emission tomography (PET) imaging. (2R, 3R, 11bR)-9-Fluoropropyl-(+)-dihydrotetrabenazine (FP-(+)-DTBZ) was found to have nanomolar binding affinity to VMAT2 (Kd = 6.76 nM) and could differentiate normal controls from Parkinson's disease subjects. In this report, asymmetric synthesis of 18F-FP-DTBZ and PET imaging study using 18F-FP-(�)-DTBZ and 18F-FP-(+)-DTBZ on male Sprague�Dawley rats are presented.                                             

Asymmetric synthesis of <sup>18</sup>F-FP-(+)-DTBZ as potential PET imaging agent for vesicular monoamine transporter

246th National Meeting (2013)

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Asymmetric synthesis of 18F-FP-(+)-DTBZ as potential PET imaging agent for vesicular monoamine transporter

Asymmetric synthesis of ¹⁸F-FP-(+)-DTBZ as potential PET imaging agent for vesicular monoamine transporter