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Titolo:
Single-photon emission tomography imaging of serotonin transporters in thenonhuman primate brain with [I-123]ODAM
Autore:
Acton, PD; Mu, M; Plossl, K; Hou, C; Siciliano, M; Zhuang, ZP; Oya, S; Choi, SR; 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:
EUROPEAN JOURNAL OF NUCLEAR MEDICINE
fascicolo: 10, volume: 26, anno: 1999,
pagine: 1359 - 1362
SICI:
0340-6997(199910)26:10<1359:SETIOS>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
DEPRESSION;
Keywords:
serotonin transporter; SSRI; 5-hydroxytryptamine; single-photon emission tomography; baboon;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
9
Recensione:
Indirizzi per estratti:
Indirizzo: Acton, PD Univ Penn, Dept Radiol, 3700 Market St,Room 305, Philadelphia, PA 19104 USA Univ Penn 3700 Market St,Room 305 Philadelphia PA USA 19104 USA
Citazione:
P.D. Acton et al., "Single-photon emission tomography imaging of serotonin transporters in thenonhuman primate brain with [I-123]ODAM", EUR J NUCL, 26(10), 1999, pp. 1359-1362

Abstract

We have described previously a selective serotonin transporter (SERT) radioligand, [I-123]IDAM. We now report a similarly potent, but more stable IDAM derivative, 5-iodo-2-[2-[(dimethylamino)methyl]phenoxy]benzyl alcohol ([I-123]ODAM). The imaging characteristics of this radioligand were studied and compared against [I-123]IDAM. Dynamic sequences of single-photon emissiontomography (SPET) scans were obtained on three female baboons after injection of 375 MBq of [I-123]ODAM. Displacing doses (1 mg/kg) of the selective SEPT ligand (+)McN5652 were administered 120 min after injection of [I-123]ODAM. Total integrated brain uptake of [I-123]ODAM was about 30% higher than [I-123]IDAM. After 60-120 min, the regional distribution of tracer withinthe brain reflected the characteristic distribution of SEPT. Peak specificbinding in the midbrain occurred 120 min after injection, with an equilibrium midbrain to cerebellar ratio of 1.50+/-0.08, which was slightly lower than the value for [I-123]IDAM (1.80+/- 0.13). Both the binding kinetics andthe metabolism of [I-123]ODAM were slower than those of [I-123]IDAM. Following injection of a competing SEPT ligand, (+)McN5652, the tracer exhibitedwashout from areas with high concentrations of SEPT, with a dissociation kinetic rate constant k(off)=0.0085+/-0.0028 min(-1) in the midbrain. Similar studies using nisoxetine and methylphenidate showed no displacement, consistent with its low binding affinity to norepinephrine and dopamine transporters, respectively. These results suggest that [I-123]ODAM is suitable forselective SPET imaging of SEPT in the primate brain, with higher uptake and slower kinetics and metabolism than [I-123]IDAM, but also a slightly lower selectivity for SERT.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 19:08:53