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Titolo:
2-((2-((Dimethylamino)methyl)phenyl)thio-5-iodophenylamine (ADAM): An improved serotonin transporter ligand
Autore:
Oya, S; Choi, SR; Hou, C; Mu, M; Kung, MP; Acton, PD; Siciliano, M; Kung, HF;
Indirizzi:
Univ Penn, Dept Radiol, Philadelphia, PA 19104 USA Univ Penn PhiladelphiaPA USA 19104 pt Radiol, Philadelphia, PA 19104 USA Univ Penn, Dept Pharmacol, Philadelphia, PA 19104 USA Univ Penn Philadelphia PA USA 19104 Pharmacol, Philadelphia, PA 19104 USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 3, volume: 27, anno: 2000,
pagine: 249 - 254
SICI:
0969-8051(200004)27:3<249:2(AI>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; 5-HYDROXYTRYPTAMINE UPTAKE COMPLEX; NONHUMAN PRIMATE BRAIN; SELECTIVE LIGAND; I-123 IDAM; REUPTAKE SITES; C-11 MCN5652; POTENT; 5-IODO-6-NITROQUIPAZINE; SENSITIVITY;
Keywords:
brain imaging agents; antidepressants; radioiodination; SPECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Kung, HF Univ Penn, Dept Radiol, 3700 Mkt St,Room 305, Philadelphia, PA 19104 USA Univ Penn 3700 Mkt St,Room 305 Philadelphia PA USA 19104 9104 USA
Citazione:
S. Oya et al., "2-((2-((Dimethylamino)methyl)phenyl)thio-5-iodophenylamine (ADAM): An improved serotonin transporter ligand", NUCL MED BI, 27(3), 2000, pp. 249-254

Abstract

Serotonin transporters (SERT) are target-sites for commonly used antidepressants, such as fluoxetine, paroxetine, sertraline, and so on. Imaging of these sites in the living human brain may provide an important tool to evaluate the mechanisms of action as well as to monitor the treatment of depressed patients. Synthesis and characterization of an improved SERT imaging agent, ADAM (2-((2-((dimethylamino)methyl) phenyl) thio)-5-iodophenylamine)(7)was achieved. The new compound, ADAM(7), displayed an extremely potent binding affinity toward SERT (K-i = 0.013 nM, in membrane preparations of LLC-PK1-cloned cell lines expressing the specific monoamine transporter). ADAM(7) also showed more than 1,000-fold selectivity for SERT over norepinephrine transporter (NET) and dopamine transporter (DAT) (K-i = 699 and 840 nM, for NET and DAT, respectively). The radiolabeled compound [I-125]ADAM (7) showed an excellent brain uptake in rats (1.41% dose at 2 min post intravenous [IV] injection), and consistently displayed the highest uptake (between 60-240 min post IV injection) in hypothalamus, a region with the highest density of SERT. The specific uptake of [I-125]ADAM(7) in the hypothalamus exhibited the highest target-to nontarget ratio ([hypothalamus - cerebellum]/cerebellum was 3.97 at 120 min post IV injection). The preliminary imaging study of [I-123]ADAM in the brain of a baboon by single photon emission computed tomography (SPECT) at 180-240 min post IV injection indicated a specific uptake in midbrain region rich in SERT. These data suggest that the new ligand [I-123]ADAM(7) may be useful for SPECT imaging of SERT binding sitesin the human brain. NUCL MED BIOL 27;3:249-254, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 06:33:49