In:
Journal of Labelled Compounds and Radiopharmaceuticals, Wiley, Vol. 57, No. 8 ( 2014-06-30), p. 525-532
Abstract:
The cholinergic system is involved in neurodegenerative diseases, and visualization of cholinergic innervations with positron emission tomography (PET) would be a useful tool in understanding these diseases. A ligand for the vesicular acetylcholine transporter (VAChT), acknowledged as a marker for cholinergic neurons, could serve as such a PET tracer. The aim was to find a VAChT PET tracer using a library concept to create a small but diverse library of labeled compounds. From the same precursor and commercially available aryl iodides 6a–f, six potential VAChT PET tracers, [ 11 C]‐(±)5a–f, were 11 C‐labeled by a palladium (0)‐mediated aminocarbonylation, utilizing a standard protocol. The labeled compounds [ 11 C]‐(±)5a–f were obtained in radiochemical purities 〉 95% with decay‐corrected radiochemical yields and specific radioactivities between 4–25% and 124–597 GBq/µmol, respectively. Autoradiography studies were then conducted to assess the compounds binding selectivity for VAChT. Labeled compounds [ 11 C]‐(±)5d and [ 11 C]‐(±)5e showed specific binding but not enough to permit further preclinical studies. To conclude, a general method for a facile synthesis and labeling of a small piperazine‐based library of potential PET tracers for imaging of VAChT was shown, and in upcoming work, another scaffold will be explored using this approach
Type of Medium:
Online Resource
ISSN:
0362-4803
,
1099-1344
Language:
English
Publisher:
Wiley
Publication Date:
2014
detail.hit.zdb_id:
1491841-9
SSG:
15,3
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