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Titolo:
[F-18]CFT ([F-18]WIN-35,428), A RADIOLIGAND TO STUDY THE DOPAMINE TRANSPORTER WITH PET - BIODISTRIBUTION IN RATS
Autore:
HAAPARANTA M; BERGMAN J; LAAKSO A; HIETALA J; SOLIN O;
Indirizzi:
UNIV TURKU,MED CYCLOTRON PET CTR,RADIOPHARMACEUT LAB FIN-20520 TURKU FINLAND UNIV TURKU,PET,MED RES LAB FIN-20520 TURKU FINLAND UNIV TURKU,INST PHARMACOL FIN-20520 TURKU FINLAND ABO AKAD UNIV,ACCELERATOR LAB FIN-20500 TURKU FINLAND
Titolo Testata:
Synapse
fascicolo: 4, volume: 23, anno: 1996,
pagine: 321 - 327
SICI:
0887-4476(1996)23:4<321:[(ARTS>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; COCAINE RECOGNITION SITES; CFT )H-3>WIN 35,428; MONKEY BRAIN; H-3 CFT; BINDING-SITES; C-11 WIN-35,428; REUPTAKE SITES; INVIVO; ANALOGS;
Keywords:
F-18; DOPAMINE REUPTAKE SITES; POSITRON EMISSION TOMOGRAPHY; ANIMAL; AUTORADIOGRAPHY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
M. Haaparanta et al., "[F-18]CFT ([F-18]WIN-35,428), A RADIOLIGAND TO STUDY THE DOPAMINE TRANSPORTER WITH PET - BIODISTRIBUTION IN RATS", Synapse, 23(4), 1996, pp. 321-327

Abstract

We describe the F-18-radiolabelling synthesis (F-18; T-1/2=109.8 min)of 2-beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane (also known as CFT or WIN 35,428) and the biodistribution of this compound in rats. F-18-labelled CFT has high chemical and radiochemical purity and relatively high specific radioactivity [specific radioactivity up to 14.8 GBq/mu mol (400 mCi/mu mol) at end of synthesis]. Striatum to cerebellumradioactivity uptake ratios were calculated from digitised images of rat brain slices recorded with a phosphoimaging device, the maximum ratio of about 10 was obtained at 2 h postinjection. Pretreatment of therats with a specific dopamine transport inhibitor, GBR 12909, showed that CFT binding is specific in striatum. The highest accumulation of F-18-radioactivity was found in the liver, urine, striatum, and kidneyof the rat. Clearance from blood was rapid. The uptake in bone was low, indicating that [F-18]CFT is not defluorinated. The relatively longhalf-life of F-18 makes it possible to study the uptake of [F-18]CFT in the brain, as equilibrium between specific and non-specific bindingis reached. This will improve the signal to noise ratio as compared to positron emission tomography (PET) studies with [C-11]CFT (C-11; T-1/2=20.4 min). CFT labelled with F-18 is clearly a promising radioligand for PET studies of the dopamine transporter system in humans. (C) 1996 Wiley-Liss, Inc.

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Documento generato il 07/04/20 alle ore 04:04:54