Literature DB >> 21666830

Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D2 Receptors

Anna W Sromek1, Yu-Gui Si, Tangzhi Zhang, Susan R George, Philip Seeman, John L Neumeyer.   

Abstract

The 2-fluoroalkoxy substituted catechol-aporphines 6, 8a-f and 11-monohydroxyaporphines 11a-e were synthesized and found to have high in vitro affinity and selectivity for the dopamine D(2) receptors. The catechol aporphines, 8b and 8d, and the monohydroxy aporphines, 11a-d, were identified as candidates for development as potential PET ligands.

Entities:  

Year:  2011        PMID： 21666830      PMCID： PMC3110009          DOI： 10.1021/ml1001689

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  36 in total

Review 1.  PET tracers for imaging of the dopaminergic system.

Authors:  Philip H Elsinga; Kentaro Hatano; Kiichi Ishiwata
Journal:  Curr Med Chem       Date:  2006       Impact factor: 4.530

2.  Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist.

Authors:  J L Neumeyer; Y G Gao; N S Kula; R J Baldessarini
Journal:  J Med Chem       Date:  1990-12       Impact factor: 7.446

3.  Synthesis and structural requirements of N-substituted norapomorphines for affinity and activity at dopamine D-1, D-2, and agonist receptor sites in rat brain.

Authors:  Y G Gao; V J Ram; A Campbell; N S Kula; R J Baldessarini; J L Neumeyer
Journal:  J Med Chem       Date:  1990-01       Impact factor: 7.446

4.  Syntheses and in vitro evaluation of fluorinated naphthoxazines as dopamine D2/D3 receptor agonists: radiosynthesis, ex vivo biodistribution and autoradiography of [(18)F]F-PHNO.

Authors:  Neil Vasdev; Philip Seeman; Armando Garcia; Winston T Stableford; José N Nobrega; Sylvain Houle; Alan A Wilson
Journal:  Nucl Med Biol       Date:  2007-01-17       Impact factor: 2.408

5.  Radiosynthesis and ex vivo evaluation of (R)-(-)-2-chloro-N-[1-11C-propyl]n-propylnorapomorphine.

Authors:  Mikael Palner; Patrick McCormick; Nic Gillings; Mikael Begtrup; Alan A Wilson; Gitte M Knudsen
Journal:  Nucl Med Biol       Date:  2009-10-03       Impact factor: 2.408

6.  Antiparkinson therapeutic potencies correlate with their affinities at dopamine D2(High) receptors.

Authors:  Philip Seeman
Journal:  Synapse       Date:  2007-12       Impact factor: 2.562

7.  Single photon emission computed tomographic imaging demonstrates loss of striatal dopamine transporters in Parkinson disease.

Authors:  R B Innis; J P Seibyl; B E Scanley; M Laruelle; A Abi-Dargham; E Wallace; R M Baldwin; Y Zea-Ponce; S Zoghbi; S Wang
Journal:  Proc Natl Acad Sci U S A       Date:  1993-12-15       Impact factor: 11.205

8.  Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues.

Authors:  Y G Gao; R J Baldessarini; N S Kula; J L Neumeyer
Journal:  J Med Chem       Date:  1990-06       Impact factor: 7.446

9.  Dopamine D2(High) receptors on intact cells.

Authors:  Philip Seeman
Journal:  Synapse       Date:  2008-04       Impact factor: 2.562

10.  Synthesis and dopamine receptor affinities of N-alkyl-11-hydroxy-2-methoxynoraporphines: N-alkyl substituents determine D1 versus D2 receptor selectivity.

Authors:  Yu-Gui Si; Matthew P Gardner; Frank I Tarazi; Ross J Baldessarini; John L Neumeyer
Journal:  J Med Chem       Date:  2008-02-06       Impact factor: 7.446
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  3 in total

1.  (18)F-MCL-524, an (18)F-Labeled Dopamine D2 and D3 Receptor Agonist Sensitive to Dopamine: A Preliminary PET Study.

Authors:  Sjoerd J Finnema; Vladimir Stepanov; Ryuji Nakao; Anna W Sromek; Tangzhi Zhang; John L Neumeyer; Susan R George; Philip Seeman; Michael G Stabin; Cathrine Jonsson; Lars Farde; Christer Halldin
Journal:  J Nucl Med       Date:  2014-05-01       Impact factor: 10.057

2.  Convenient synthesis of 18F-radiolabeled R-(-)-N-n-propyl-2-(3-fluoropropanoxy-11-hydroxynoraporphine.

Authors:  Anna W Sromek; Shaohui Zhang; Vamsidhar Akurathi; Alan B Packard; Wei Li; David Alagille; Thomas J Morley; Ronald Baldwin; Gilles Tamagnan; John L Neumeyer
Journal:  J Labelled Comp Radiopharm       Date:  2014-11-17       Impact factor: 1.921

Review 3.  Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging.

Authors:  Vladimir Shalgunov; Aren van Waarde; Jan Booij; Martin C Michel; Rudi A J O Dierckx; Philip H Elsinga
Journal:  Med Res Rev       Date:  2018-11-18       Impact factor: 12.944
  3 in total

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