Article (Scientific journals)
Synthesis and biodistribution of [5-131I]iodotropapride: a potential D2 dopamine receptor imaging agent.
Cantineau, Robert; Guillaume, Marcel; Damhaut, Philippe et al.
1994In Nuclear Medicine and Biology, 21 (2), p. 255-62
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Keywords :
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
Abstract :
[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).
Research center :
GIGA CRC (Cyclotron Research Center) In vivo Imaging-Aging & Memory - ULiège
Disciplines :
Chemistry
Author, co-author :
Cantineau, Robert
Guillaume, Marcel
Damhaut, Philippe;  Université de Liège - ULiège > Centre de recherches du cyclotron
Lemaire, Christian ;  Université de Liège - ULiège > Centre de recherches du cyclotron
Plenevaux, Alain  
Gauthier, Françoise
Pourrias, Bernard
Christiaens, Léon
Language :
English
Title :
Synthesis and biodistribution of [5-131I]iodotropapride: a potential D2 dopamine receptor imaging agent.
Publication date :
1994
Journal title :
Nuclear Medicine and Biology
ISSN :
0969-8051
Publisher :
Pergamon Press, Oxford, United Kingdom
Volume :
21
Issue :
2
Pages :
255-62
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Available on ORBi :
since 02 February 2009

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