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Titolo:
PET examination of three potent cocaine derivatives as specific radioligands for the serotonin transporter
Autore:
Helfenbein, J; Sandell, J; Halldin, C; Chalon, S; Emond, P; Okubo, Y; Chou, YH; Frangin, Y; Douziech, L; Gareau, L; Swahn, CG; Besnard, JC; Farde, L; Guilloteau, D;
Indirizzi:
Karolinska Hosp, Dept Clin Neurosci, Psychol Sect, Karolinska Inst, S-17176 Stockholm, Sweden Karolinska Hosp Stockholm Sweden S-17176 Inst, S-17176 Stockholm, Sweden Univ Tours, INSERM U316, Tours, France Univ Tours Tours FranceUniv Tours, INSERM U316, Tours, France
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 5, volume: 26, anno: 1999,
pagine: 491 - 499
SICI:
0969-8051(199907)26:5<491:PEOTPC>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; NOR-BETA-CIT; HIGH-AFFINITY; HUMAN BRAIN; DOPAMINE TRANSPORTER; SELECTIVE COMPOUNDS; ALZHEIMERS-DISEASE; BINDING-PROPERTIES; LIGAND-BINDING; REUPTAKE SITES;
Keywords:
cocaine derivative; serotonin transporter; 5-HTT; PET; monkey; brain;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Sandell, J Karolinska Hosp, Dept Clin Neurosci, Psychol Sect, Karolinska Inst, S-17176 Stockholm, Sweden Karolinska Hosp Stockholm Sweden S-17176 76 Stockholm, Sweden
Citazione:
J. Helfenbein et al., "PET examination of three potent cocaine derivatives as specific radioligands for the serotonin transporter", NUCL MED BI, 26(5), 1999, pp. 491-499

Abstract

Several positron emission tomography (PET) radioligands based on the aryl tropane structure have been used for studies on monoamine reuptake sites. RTI-364, RTI-330, and RTI-357 (3-beta-(4'-n-propyl-, 4'-iso-propyl-, and 4'-iso-propenyl-phenyl)nortropane-2-beta-carboxylic acid methyl ester) are three recently synthesized cocaine analogues with higher affinity for the serotonin (5-HTT) than the dopamine transporter (DAT). Unlabelled RTI-364 and RTI-330 were prepared in a two-step synthesis. The key step was the additionof the appropriate propyl Grignard reagent to anhydroecgonine methyl ester. RTI-357 was prepared in a three-step synthesis with a palladium-catalyzedcoupling reaction of beta-CIT and isopropenylzinc bromide as key step. Hydrolysis of the ester functions gave the carboxylic acid analogues of RTI-364, RTI-330, and RTI-357, which were labelled with C-11 using [C-11]methyl iodide in dimethyl formamide (DMF) and tetrabutylammonium hydroxide (TBAH) as base. All three compounds entered the monkey brain in a high degree (similar to 5-10%). There was a low uptake of [C-11]RTI-364 in serotonin-rich brain areas, whereas [C-11]RTI-330 and [C-11]RTI-357 showed a marked uptake of radioactivity in the thalamus and the brainstem, regions known to containserotonin transporters, Transient equilibrium was reached at 15 and 40 minfor [C-11]RTI-330 and [C-11]RTI-357, respectively. After pretreatment withcitalopram, the ratio of radioactivity in the thalamus and the brainstem to the cerebellum were markedly reduced for [C-11]RTI-357 but not for [C-11]RTI-330. The results indicate that [C-11]RTI-357 is a potential PET radioligand for quantitation of the serotonin reuptake site. (C) 1999 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 21:28:16