18F-(+)-FP-DTBZ:A Potential PET Imaging Agent for Vesicular Monoamine Transporters

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户：sunhuai

【摘要】

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【作者】

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Zih-Rou Huang Ling-Wei Hsin

【机构】

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Institute of Pharmaceutical Sciences,National Taiwan University,Taipei 100

【出处】

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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会

【发表日期】

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2012年8期

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　　In August 2008,racemic tetrabenazine ((±)-3-(2-methylpropyl)-9,10-dimethoxy-1,3,4,6,7,11 b-hexahydro-2H-benzo[a]quinolizin-2-one,(±)-TBZ) was approved for the treatment of chorea associated with Huntingtons disease in USA.The primary pharmacological action of TBZ and its active metabolites is to deplete the levels of monoamines(i.e.dopamine,serotonin,and norepinephrine) within the central nervous system by inhibiting the vesicular monoamine transporter 2(VMAT2).(2R,3R,l lbR)-9-Fluoropropyl-(+)-dihydrotetrabenazine((+)-FP-DTBZ) was found to have nanomolar binding affinity to VMAT2(Ki=6.76 nM).

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18F-(+)-FP-DTBZ:A Potential PET Imaging Agent for Vesicular Monoamine Transporters

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