Reference : Synthesis and biodistribution of [5-131I]iodotropapride: a potential D2 dopamine recepto...
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
http://hdl.handle.net/2268/5371
Synthesis and biodistribution of [5-131I]iodotropapride: a potential D2 dopamine receptor imaging agent.
English
Cantineau, Robert [> > > >]
Guillaume, Marcel [> > > >]
Damhaut, Philippe [Université de Liège - ULg > > Centre de recherches du cyclotron >]
Lemaire, Christian mailto [Université de Liège - ULg > > Centre de recherches du cyclotron >]
Plenevaux, Alain mailto [> > > >]
Gauthier, Françoise [> > > >]
Pourrias, Bernard [> > > >]
Christiaens, Léon [> > > >]
1994
Nuclear Medicine & Biology
Pergamon Press
21
2
255-62
Yes (verified by ORBi)
International
0969-8051
Oxford
United Kingdom
[en] Animals ; Brain/metabolism ; Cerebellum/metabolism ; Frontal Lobe/metabolism ; Iodine Radioisotopes/diagnostic use ; Male ; Nortropanes/metabolism/pharmacokinetics ; Octanols ; Protein Binding ; Radiopharmaceuticals/metabolism/pharmacokinetics ; Rats ; Rats, Wistar ; Receptors, Dopamine D2/metabolism ; Tissue Distribution/physiology ; Water
[en] [5-131I]Iodotropapride is a benzamidic compound which displays high affinity and selectivity for dopaminergic receptors. It was prepared from the corresponding brominated compound by a nucleophilic substitution with [131I]iodine (t1/2 = 8.02 days, E gamma = 364 keV) based on the use of Cu(I) as catalyst and high specific activity of [131I]NaI. After i.v. injection in rats the tracer crosses the blood-brain barrier (0.42 +/- 0.06% of injected dose in the total brain) and demonstrates a high affinity binding to the striatum. The striatum-to-cerebellum ratio increases with time and reaches values of 9 and 22 at 30 and 120 min after injection, respectively. This specific uptake in the striatum is saturable and can be blocked by pretreatment with different D2 antagonists. When labeled with 123I (t1/2 = 13 h, E1 = 159 keV), the corresponding [123I]iodotropapride may be useful for the investigation of the D2 dopamine receptors in humans with single photon emission computer tomography (SPECT).
Centre de Recherches du Cyclotron - CRC
Fonds de la Recherche Scientifique (Communauté française de Belgique) - F.R.S.-FNRS
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/5371

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