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Titolo:
[(125) I]3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester ([I-125]EINT): A potent and selective radioligand for the brain serotonin transporter
Autore:
Navarro, HA; Xu, H; Zhong, D; Blough, BE; Ross, WP; Kuhar, MJ; Carroll, FI;
Indirizzi:
Res Triangle Inst, Ctr Organ & Med Chem Chem & Life Sci, Res Triangle Pk, NC 27709 USA Res Triangle Inst Res Triangle Pk NC USA 27709 Triangle Pk, NC 27709 USA Emory Univ, Yerkes Reg Primate Res Ctr, Atlanta, GA 30322 USA Emory Univ Atlanta GA USA 30322 eg Primate Res Ctr, Atlanta, GA 30322 USA
Titolo Testata:
SYNAPSE
fascicolo: 3, volume: 41, anno: 2001,
pagine: 241 - 247
SICI:
0887-4476(200109)41:3<241:[IBBAM>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
H-3 PAROXETINE BINDING; HIGH-AFFINITY; RAT-BRAIN; DOPAMINE TRANSPORTER; LIGAND-BINDING; I-125 RTI-55; IN-VIVO; ANALOGS; NOREPINEPHRINE; COCAINE;
Keywords:
serotonin transporter; radioligand; receptor binding; tropane; in vivo;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Navarro, HA Res Triangle Inst, Ctr Organ & Med Chem Chem & Life Sci, POB 12194, Res Triangle Pk, NC 27709 USA Res Triangle Inst POB 12194 Res Triangle Pk NC USA 27709 9 USA
Citazione:
H.A. Navarro et al., "[(125) I]3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester ([I-125]EINT): A potent and selective radioligand for the brain serotonin transporter", SYNAPSE, 41(3), 2001, pp. 241-247

Abstract

The binding characteristics of [I-125] 3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta -carboxylic acid methyl ester ([I-125]EINT), a high-affinity selective ligand for the serotonin transporter (5-HTT), and its binding characteristics to rat brain membranes were determined. [I-125]EINT binding to rat cerebral cortex membranes was saturable and reversible, and its specificbinding represented approximately 90% of the total binding. [I-125]EINT labeled a single site with K-d = 0.22 +/- 0.03 nM and B-max = 583 +/- 38 fmol/mg protein. Kinetic analysis revealed a t(1/2) for association and dissociation of 20 and 24 min, respectively. Pharmacological characterization of [I-125]EINT confirmed its high specificity for the 5-HTT. The pattern of brain region distribution in vivo of intravenously administered [I-125]EINT indicated greater accumulation of the radioligand in 5-HTT-rich brain regions. However, the signal-to-background ratio was low. Thus, [I-125]EINT appears to be a useful radioligand for studying the 5-HTT in vitro, but it may not be a good in vivo ligand. Synapse 41:241-247, 2001. (C) 2001 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 22:10:58