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Titolo:
PREPARATION OF [BR-76]FLB-457 AND [BR-76]FLB-463 FOR EXAMINATION OF STRIATAL AND EXTRASTRIATAL DOPAMINE D-2 RECEPTORS WITH PET
Autore:
LOCH C; HALLDIN C; BOTTLAENDER M; SWAHN CG; MORESCO RM; MAZIERE M; FARDE L; MAZIERE B;
Indirizzi:
CEA,SERV HOSP FREDERIC JOLIOT,DEPT RECH MED,4 PL GEN LECLERC F-91406 ORSAY FRANCE KAROLINSKA HOSP,PSYCHIAT SECT,DEPT CLIN NEUROSCI,KAROLINSKA INST S-10401 STOCKHOLM SWEDEN
Titolo Testata:
Nuclear medicine and biology
fascicolo: 6, volume: 23, anno: 1996,
pagine: 813 - 819
SICI:
0969-8051(1996)23:6<813:PO[A[F>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
POTENTIAL ANTIPSYCHOTIC AGENTS; POSITRON EMISSION TOMOGRAPHY; LIVING HUMAN-BRAIN; I-125 EPIDEPRIDE; ANTIDOPAMINERGIC PROPERTIES; BR-76 BROMOLISURIDE; D2 RECEPTORS; BINDING; RADIOLIGANDS; LIGAND;
Keywords:
BR-76; SUBSTITUTED BENZAMIDE; DOPAMINE D-2 RECEPTOR ANTAGONIST; EXTRASTRIATAL BINDING; POSITRON EMISSION TOMOGRAPHY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
33
Recensione:
Indirizzi per estratti:
Citazione:
C. Loch et al., "PREPARATION OF [BR-76]FLB-457 AND [BR-76]FLB-463 FOR EXAMINATION OF STRIATAL AND EXTRASTRIATAL DOPAMINE D-2 RECEPTORS WITH PET", Nuclear medicine and biology, 23(6), 1996, pp. 813-819

Abstract

Both FLB 457 and FLB 463, two substituted benzamides with high affinity for the dopamine D-2 receptors, were labeled with bromine-76 for PET investigations. [Br-76]FLB 457 was prepared by electrophilic substitution of the tributyltin precursor. The radiochemical yield was 80%. [Br-76]FLB 463 was prepared by a direct electrophilic substitution enhanced by the hydroxyl group of the debromo analogue, with a total radiochemical yield of 50%. Radiochemical and chemical purity values of theradioligands as analyzed by radio-TLC and HPLC were >99%, and the specific radioactivity was similar to 40 GBq/mu mol. During PET examinations of [Br-76]FLB 457 and [Br-76]FLB 463 binding in baboons there was a rapid and high uptake in the striatum. The striatal radioactivity concentration reached a plateau 1 h postinjection (p.i.). The striatum-to- cerebellum radioactivity concentration ratio increased from 11 at 1h p.i., to 28 at 4 h p.i. for [Br-76]FLB 457, owing to a continuous wash out from the cerebellum. For [Br-76]FLB 463 the corresponding value increased from 10 to 19.5. [Br-76]FLB 457 has in contrast to [Br-76]FLB 463 a high uptake in thalamic structures and has therefore an additional potential as a radioligand for PET examination of extrastriataldopamine D-2 receptors in the living human brain.

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Documento generato il 26/01/20 alle ore 01:10:22