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Syntheses and radiosyntheses of two carbon-11 labeled potent and selective radioligands for imaging vesicular acetylcholine transporter.

Abstract：

PURPOSE:The vesicular acetylcholine transporter (VAChT) is a specific biomarker for imaging presynaptic cholinergic neurons. The syntheses and C-11 labeling of two potent enantiopure VAChT inhibitors are reported here. PROCEDURES:Two VAChT inhibitors, (±)-2 and (±)-6, were successfully synthesized. A chiral HPLC column was used to resolve the enantiomers from each corresponding racemic mixture for in vitro characterization. The radiosyntheses of (-)-[(11)C]2 and (-)-[(11)C]6 from the corresponding desmethyl phenol precursor was accomplished using [(11)C]methyl iodide or [(11)C]methyl triflate, respectively. RESULTS:The synthesis of (-)-[(11)C]2 was accomplished with 40-50 % radiochemical yield (decay-corrected), SA > 480 GBq/μmol (EOB), and radiochemical purity >99 %. Synthesis of (-)-[(11)C]6 was accomplished with 5-10 % yield, SA > 140 GBq/μmol (EOB), and radiochemical purity >97 %. The radiosynthesis and dose formulation of each tracer was completed in 55-60 min. CONCLUSIONS:Two potent enantiopure VAChT ligands were synthesized and (11)C-labeled with good radiochemical yield and specific activity.

journal_name

Mol Imaging Biol

journal_title

Molecular imaging and biology

authors

Padakanti PK,Zhang X,Li J,Parsons SM,Perlmutter JS,Tu Z

doi

10.1007/s11307-014-0748-x

subject

Has Abstract

pub_date

2014-12-01 00:00:00

pages

765-72

issue

6

eissn

1536-1632

issn

1860-2002

journal_volume

16

pub_type

杂志文章

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