Literature DB >> 25720955

Microwave-assisted radiosynthesis of [(18) F]ASEM, a radiolabeled α7-nicotinic acetylcholine receptor antagonist.

Hayden T Ravert1, Daniel P Holt, Yongjun Gao, Andrew G Horti, Robert F Dannals.   

Abstract

An improvement of the original radiochemical synthesis of [(18) F]ASEM, an α7-nicotinic acetylcholinergic receptor radioligand, is reported. The new procedure utilizes microwave-assisted radiofluorination. In addition, a new preparative HPLC method was developed to eliminate a chemical impurity in the final product. Quality control procedures were also enhanced to improve detection of product with enhanced resolution of potential impurities. [(18) F]ASEM was produced in 20.1 ± 8.9% non-decay corrected (NDC) yield with an average synthesis time of 57 min and an average specific radioactivity of 856 ± 332 GBq/µmol (23 ± 9 Ci/µmol).
Copyright © 2015 John Wiley & Sons, Ltd.

Entities:  

Keywords:  PET chemistry; [18F]ASEM; microwave; radiosynthesis; α7-nAChR

Mesh:

Substances:

Year:  2015        PMID: 25720955     DOI: 10.1002/jlcr.3275

Source DB:  PubMed          Journal:  J Labelled Comp Radiopharm        ISSN: 0362-4803            Impact factor:   1.921


  4 in total

1.  An improved synthesis of the radiolabeled prostate-specific membrane antigen inhibitor, [(18) F]DCFPyL.

Authors:  Hayden T Ravert; Daniel P Holt; Ying Chen; Ronnie C Mease; Hong Fan; Martin G Pomper; Robert F Dannals
Journal:  J Labelled Comp Radiopharm       Date:  2016-07-29       Impact factor: 1.921

Review 2.  Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.

Authors:  Alina Kassenbrock; Neil Vasdev; Steven H Liang
Journal:  Curr Top Med Chem       Date:  2016       Impact factor: 3.295

Review 3.  Development of [(18)F]ASEM, a specific radiotracer for quantification of the α7-nAChR with positron-emission tomography.

Authors:  Andrew G Horti
Journal:  Biochem Pharmacol       Date:  2015-07-29       Impact factor: 5.858

4.  Development of 11C-Labeled ASEM Analogues for the Detection of Neuronal Nicotinic Acetylcholine Receptors (α7-nAChR).

Authors:  Sangram Nag; Patricia Miranda-Azpiazu; Zhisheng Jia; Prodip Datta; Ryosuke Arakawa; Mohammad Mahdi Moein; Zhou Yang; Yaoquan Tu; Laetitia Lemoine; Hans Ågren; Agneta Nordberg; Bengt Långström; Christer Halldin
Journal:  ACS Chem Neurosci       Date:  2022-01-12       Impact factor: 5.780

  4 in total

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