Literature DB >> 35491085

Automated synthesis of (R)-[18 F]MH.MZ on the iPhase Flexlab reaction platform.

Adam J Rosenberg1,2, Yiu-Yin Cheung1, Fei Liu1, Todd E Peterson1,2, James Silverman3, Ciaran M Considine3, Daniel O Claassen3.   

Abstract

(R)-[18 F]MH.MZ ([18 F]MH.MZ) is a promising positron emission tomography (PET) radiotracer for in vivo study of the 5-HT2A receptor. To facilitate clinical trials, a fully automated radiosynthesis procedure for [18 F]MH.MZ was developed using commercially available materials on the iPhase Flexlab module. The overall synthesis time was 100 min with a radiochemical yield of 7 ± 0.9% (n = 3). The radiochemical purity was greater than 99% for [18 F]MH.MZ with a molar activity of 361 ± 57 GBq/μmol (n = 3). The protocol described herein reliably provides [18 F]MH.MZ that meets all relevant release criteria for a GMP radiopharmaceutical.
© 2022 John Wiley & Sons Ltd.

Entities:  

Keywords:  5-HT2A receptor; PET; automation; cGMP; fluorine-18; radiochemistry

Mesh:

Substances:

Year:  2022        PMID: 35491085      PMCID: PMC9177715          DOI: 10.1002/jlcr.3975

Source DB:  PubMed          Journal:  J Labelled Comp Radiopharm        ISSN: 0362-4803            Impact factor:   1.949


  14 in total

1.  Analyses of [(18)F] altanserin bolus injection PET data. I: consideration of radiolabeled metabolites in baboons.

Authors:  J C Price; B J Lopresti; N S Mason; D P Holt; Y Huang; C A Mathis
Journal:  Synapse       Date:  2001-07       Impact factor: 2.562

2.  18F-labeling and evaluation of novel MDL 100907 derivatives as potential 5-HT2A antagonists for molecular imaging.

Authors:  Fabian Debus; Matthias M Herth; Markus Piel; Hans-Georg Buchholz; Nicole Bausbacher; Vasko Kramer; Hartmut Lüddens; Frank Rösch
Journal:  Nucl Med Biol       Date:  2010-04-08       Impact factor: 2.408

3.  Synthesis and imaging validation of [¹⁸F]MDL100907 enabled by Ni-mediated fluorination.

Authors:  Hong Ren; Hsiao-Ying Wey; Martin Strebl; Ramesh Neelamegam; Tobias Ritter; Jacob M Hooker
Journal:  ACS Chem Neurosci       Date:  2014-06-03       Impact factor: 4.418

4.  Characterization of the serotonin 2A receptor selective PET tracer (R)-[18F]MH.MZ in the human brain.

Authors:  Vasko Kramer; Agnete Dyssegaard; Jonathan Flores; Cristian Soza-Ried; Frank Rösch; Gitte Moos Knudsen; Horacio Amaral; Matthias M Herth
Journal:  Eur J Nucl Med Mol Imaging       Date:  2019-10-12       Impact factor: 9.236

5.  A method for the in vivo investigation of the serotonergic 5-HT2 receptors in the human cerebral cortex using positron emission tomography and 18F-labeled setoperone.

Authors:  J Blin; G Sette; M Fiorelli; O Bletry; J L Elghozi; C Crouzel; J C Baron
Journal:  J Neurochem       Date:  1990-05       Impact factor: 5.372

6.  Time-efficient and convenient synthesis of [(18)F]altanserin for human PET imaging by a new work-up procedure.

Authors:  G Massarweh; M Kovacevic; P Rosa-Neto; A C Evans; M Diksic; R Schirrmacher
Journal:  Appl Radiat Isot       Date:  2009-08-04       Impact factor: 1.513

7.  Thin layer chromatographic detection of kryptofix 2.2.2 in the routine synthesis of [18F]2-fluoro-2-deoxy-D-glucose.

Authors:  T Chaly; J R Dahl
Journal:  Int J Rad Appl Instrum B       Date:  1989

8.  Direct comparison of [(18) F]MH.MZ and [(18) F] altanserin for 5-HT2A receptor imaging with PET.

Authors:  Hanne D Hansen; Anders Ettrup; Matthias M Herth; Agnete Dyssegaard; Cecilia Ratner; Nic Gillings; Gitte M Knudsen
Journal:  Synapse       Date:  2013-03-07       Impact factor: 2.562

9.  Optimization of 18 F-syntheses using 19 F-reagents at tracer-level concentrations and liquid chromatography/tandem mass spectrometry analysis: Improved synthesis of [18 F]MDL100907.

Authors:  Xiang Zhang; Ryan Dunlow; Burchelle N Blackman; Rolf E Swenson
Journal:  J Labelled Comp Radiopharm       Date:  2018-04-17       Impact factor: 1.921

10.  Quantification of 5-HT2A receptors in the human brain using [18F]altanserin-PET and the bolus/infusion approach.

Authors:  Lars H Pinborg; Karen H Adams; Claus Svarer; Søren Holm; Steen G Hasselbalch; Steven Haugbøl; Jacob Madsen; Gitte M Knudsen
Journal:  J Cereb Blood Flow Metab       Date:  2003-08       Impact factor: 6.200

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