Literature DB >> 18372185

A remote controlled system for the preparation of 7 alpha-[18F]fluoro-17 alpha-methyl 5 alpha-dihydrotestosterone ([18F]FMDHT) using microwave.

Sudha Garg1, Andrew J H Lynch, Aniruddha K Doke, Richard C Minton, Pradeep K Garg.   

Abstract

For non-invasive imaging of the prostate cancer, we synthesized 7 alpha-fluoro-17 alpha-methyl 5 alpha-dihydrotestosterone ([(18)F]FMDHT) for androgen receptor mediated PET imaging. Preliminary in vitro and in vivo evaluations of this compound show promise. We designed and implemented a remote controlled system for reliable, efficient, and safe handling of radioactivity during the radiochemical synthesis of [(18)F]FMDHT. The key features of this report are the microwave assisted radiochemical synthesis, increased radiochemical yields, improved radiochemical purity, reduced overall synthesis time, and remote controlled automation of the entire synthesis. The overall synthesis using microwave reaction took 60-70 min and provided the desired product in 20-30% radiochemical yields with >99% radiochemical purity.

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Year:  2008        PMID: 18372185      PMCID: PMC2390846          DOI: 10.1016/j.apradiso.2008.01.017

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN: 0969-8043            Impact factor:   1.513


  11 in total

1.  [7alpha-18F]fluoro-17alpha-methyl-5alpha-dihydrotestosterone: a ligand for androgen receptor-mediated imaging of prostate cancer.

Authors:  P K Garg; D C Labaree; R M Hoyte; R B Hochberg
Journal:  Nucl Med Biol       Date:  2001-01       Impact factor: 2.408

2.  Microwave-assisted (radio)halogenation of nitroimidazole-based hypoxia markers.

Authors:  P Kumar; L I Wiebe; M Asikoglu; M Tandon; A J B McEwan
Journal:  Appl Radiat Isot       Date:  2002-11       Impact factor: 1.513

3.  Rapid and efficient synthesis of 1,2,4-oxadiazoles utilizing polymer-supported reagents under microwave heating.

Authors:  Ying Wang; Reagan L Miller; Daryl R Sauer; Stevan W Djuric
Journal:  Org Lett       Date:  2005-03-03       Impact factor: 6.005

4.  Microwave-enhanced nucleophilic fluorination in the synthesis of fluoropyridyl derivatives of [3,2-c]pyrazolo-corticosteroids, potential glucocorticoid receptor-mediated imaging agents.

Authors:  Michael G C Kahn; Emmanuel Konde; Francis Dossou; David C Labaree; Richard B Hochberg; Robert M Hoyte
Journal:  Bioorg Med Chem Lett       Date:  2006-04-27       Impact factor: 2.823

Review 5.  Fluorine-18-labelled fluoropyridines: advances in radiopharmaceutical design.

Authors:  F Dollé
Journal:  Curr Pharm Des       Date:  2005       Impact factor: 3.116

6.  Synthesis and preliminary evaluation of para- and meta-[18F]fluorobenzylguanidine.

Authors:  P K Garg; S Garg; M R Zalutsky
Journal:  Nucl Med Biol       Date:  1994-01       Impact factor: 2.408

7.  Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.

Authors:  F Doll; L Dolci; H Valette; F Hinnen; F Vaufrey; I Guenther; C Fuseau; C Coulon; M Bottlaender; C Crouzel
Journal:  J Med Chem       Date:  1999-06-17       Impact factor: 7.446

8.  The androgen axis in recurrent prostate cancer.

Authors:  James L Mohler; Christopher W Gregory; O Harris Ford; Desok Kim; Catharina M Weaver; Peter Petrusz; Elizabeth M Wilson; Frank S French
Journal:  Clin Cancer Res       Date:  2004-01-15       Impact factor: 12.531

Review 9.  Molecular biology of the androgen receptor.

Authors:  Edward P Gelmann
Journal:  J Clin Oncol       Date:  2002-07-01       Impact factor: 44.544

10.  In vivo biodistribution of an androgen receptor avid PET imaging agent 7-alpha-fluoro-17 alpha-methyl-5-alpha-dihydrotestosterone ([(18)F]FMDHT) in rats pretreated with cetrorelix, a GnRH antagonist.

Authors:  Sudha Garg; Aniruddha Doke; Kimberly W Black; Pradeep K Garg
Journal:  Eur J Nucl Med Mol Imaging       Date:  2007-10-13       Impact factor: 9.236

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  1 in total

1.  Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe.

Authors:  Pradeep K Garg; Rachid Nazih; Yanjun Wu; Vladimir P Grinevich; Sudha Garg
Journal:  EJNMMI Res       Date:  2017-08-08       Impact factor: 3.138

  1 in total

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