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Titolo:
PREPARATION AND BIOLOGICAL EVALUATION OF IODINE-125-IACFT - A SELECTIVE SPECT AGENT FOR IMAGING DOPAMINE TRANSPORTER SITES
Autore:
ELMALEH DR; FISCHMAN AJ; SHOUP TM; BYON C; HANSON RN; LIANG AY; MELTZER PC; MADRAS BK;
Indirizzi:
MASSACHUSETTS GEN HOSP,DIV NUCL MED,DEPT RADIOL,55 FRUUIT ST BOSTON MA 02114 HARVARD UNIV,SCH MED,DEPT RADIOL BOSTON MA 02115 NORTHEASTERN UNIV,DEPT CHEM BOSTON MA 02115 ORGANIX INC WOBURN MA 00000
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 7, volume: 37, anno: 1996,
pagine: 1197 - 1202
SICI:
0161-5505(1996)37:7<1197:PABEOI>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
COCAINE RECOGNITION SITES; SEROTONIN UPTAKE SITES; NONHUMAN-PRIMATES; BINDING-SITES; MONKEY BRAIN; I-125 RTI-55; H-3 CFT; ANALOGS; ESTERS; RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
34
Recensione:
Indirizzi per estratti:
Citazione:
D.R. Elmaleh et al., "PREPARATION AND BIOLOGICAL EVALUATION OF IODINE-125-IACFT - A SELECTIVE SPECT AGENT FOR IMAGING DOPAMINE TRANSPORTER SITES", The Journal of nuclear medicine, 37(7), 1996, pp. 1197-1202

Abstract

Parkinson's disease is a progressive neurodegenerative disorder that is associated with the loss of nerve terminals from specific brain areas, particularly in the caudate and putamen, which contains the highest concentrations of dopamine transporter sites. Previously, we synthesized and evaluated a series of C-11-labeled 2 beta-carbomethoxy-3 beta-aryltropane (WIN 35,428; CFT) derivatives as markers for the dopaminetransporter system. These ligands have high affinity and specificity for dopamine transporter sites in vitro and in vivo in laboratory animals. The goal of this study was the preparation and preliminary biological characterization of two new ligands based on the structure of WIN35,428, the E and Z isomers of N-iodoallyl-2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane (E and Z IACFT). Methods: E and Z IACFT were synthesized and radiolabeled with I-125. The ligands were characterized by in vitro assays of binding to dopamine and serotonin transportersand by autoradiography. Results: Iodine-125-IACFT was prepared in >60% radiochemical yield, and >98% radiochemical purity. Specific activity was 1500 Ci/mmole. In vitro, E-IACFT showed higher affinity for dopamine transporter sites than WIN 35,428 (6.6 versus 11 nM) and better selectivity than RTI-55. The Z isomer was found to have much lower affinity. One hour after an intravenous injection of I-125 IACFT in monkeys, ex vivo autoradiographs of the brain revealed high concentrations of tracer in dopamine rich regions such as the caudate-putamen. The striatum-to-cerebellum, striatum-to-cortex and striatum-to-thalamus ratios were 10.8, 7.2 and 8.3. Conclusion: These result suggest that radiolabeled E-IACFT may be a useful radioligand for SPECT imaging of dopamine transporter sites. IACFT could prove to be extremely useful for thenoninvasive evaluation of patients with early Parkinson's disease.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 16:15:06