Literature DB >> 3874833

Preparation of 11C-labelled Raclopride, a new potent dopamine receptor antagonist: preliminary PET studies of cerebral dopamine receptors in the monkey.

E Ehrin, L Farde, T de Paulis, L Eriksson, T Greitz, P Johnström, J E Litton, J L Nilsson, G Sedvall, S Stone-Elander.   

Abstract

A new dopamine receptor antagonist, Raclopride (S-(-)-3,5-dichloro-N-[(1-ethyl-2-pyrrolidinyl)]methyl-2-hydroxy- 6-methoxybenzamide, FLA 870) (1), has been labelled using [11C]ethyl iodide for alkylation of the nitrogen of the pyrrolidine ring in the corresponding secondary amine (5). The synthesis of 5 and an efficient method for the preparation of [11C]ethyl iodide are described. The 11C-labelled FLA 870 (1) was purified by HPLC and then used in positron emission tomography to visualize the dopamine receptor-rich areas of the monkey brain. The images obtained show selective accumulation of FLA 870 in striatum and a 10-fold separation between the binding to caudate vs cerebellum.

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Year:  1985        PMID: 3874833     DOI: 10.1016/0020-708x(85)90083-3

Source DB:  PubMed          Journal:  Int J Appl Radiat Isot        ISSN: 0020-708X


  23 in total

1.  Striatal and extrastriatal dopamine release measured with PET and [(18)F] fallypride.

Authors:  Mark Slifstein; Lawrence S Kegeles; Xiaoyan Xu; Judy L Thompson; Nina Urban; John Castrillon; Elizabeth Hackett; S-A Bae; Marc Laruelle; Anissa Abi-Dargham
Journal:  Synapse       Date:  2010-05       Impact factor: 2.562

Review 2.  From simultaneous to synergistic MR-PET brain imaging: A review of hybrid MR-PET imaging methodologies.

Authors:  Zhaolin Chen; Sharna D Jamadar; Shenpeng Li; Francesco Sforazzini; Jakub Baran; Nicholas Ferris; Nadim Jon Shah; Gary F Egan
Journal:  Hum Brain Mapp       Date:  2018-08-04       Impact factor: 5.038

3.  Determination of dopamine D₂ receptor occupancy by lurasidone using positron emission tomography in healthy male subjects.

Authors:  Dean F Wong; Hiroto Kuwabara; James Robert Brašić; Thomas Stock; Atul Maini; Emily G Gean; Antony Loebel
Journal:  Psychopharmacology (Berl)       Date:  2013-05-07       Impact factor: 4.530

Review 4.  Development of (18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography.

Authors:  Peter Brust; Jörg van den Hoff; Jörg Steinbach
Journal:  Neurosci Bull       Date:  2014-08-29       Impact factor: 5.203

5.  History of childhood adversity is positively associated with ventral striatal dopamine responses to amphetamine.

Authors:  Lynn M Oswald; Gary S Wand; Hiroto Kuwabara; Dean F Wong; Shijun Zhu; James R Brasic
Journal:  Psychopharmacology (Berl)       Date:  2014-01-22       Impact factor: 4.530

6.  Receptor binding of N-(methyl-11C) clozapine in the brain of rhesus monkey studied by positron emission tomography (PET).

Authors:  P Hartvig; S A Eckernäs; L Lindström; B Ekblom; U Bondesson; H Lundqvist; C Halldin; K Någren; B Långström
Journal:  Psychopharmacology (Berl)       Date:  1986       Impact factor: 4.530

7.  VMAT2 and dopamine neuron loss in a primate model of Parkinson's disease.

Authors:  Ming-Kai Chen; Hiroto Kuwabara; Yun Zhou; Robert J Adams; James R Brasić; Jennifer L McGlothan; Tatyana Verina; Neal C Burton; Mohab Alexander; Anil Kumar; Dean F Wong; Tomás R Guilarte
Journal:  J Neurochem       Date:  2007-11-05       Impact factor: 5.372

8.  Mechanisms of dopaminergic and serotonergic neurotransmission in Tourette syndrome: clues from an in vivo neurochemistry study with PET.

Authors:  Dean F Wong; James R Brasić; Harvey S Singer; David J Schretlen; Hiroto Kuwabara; Yun Zhou; Ayon Nandi; Marika A Maris; Mohab Alexander; Weiguo Ye; Olivier Rousset; Anil Kumar; Zsolt Szabo; Albert Gjedde; Anthony A Grace
Journal:  Neuropsychopharmacology       Date:  2007-11-07       Impact factor: 7.853

9.  Brain region binding of the D2/3 agonist [11C]-(+)-PHNO and the D2/3 antagonist [11C]raclopride in healthy humans.

Authors:  Ariel Graff-Guerrero; Matthaeus Willeit; Nathalie Ginovart; David Mamo; Romina Mizrahi; Pablo Rusjan; Irina Vitcu; Philip Seeman; Alan A Wilson; Shitij Kapur
Journal:  Hum Brain Mapp       Date:  2008-04       Impact factor: 5.038

10.  Increased synaptic dopamine in the putamen in restless legs syndrome.

Authors:  Christopher J Earley; Hiroto Kuwabara; Dean F Wong; Charlene Gamaldo; Rachel E Salas; James R Brašić; Hayden T Ravert; Robert F Dannals; Richard P Allen
Journal:  Sleep       Date:  2013-01-01       Impact factor: 5.849

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