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Titolo:
[I-125/123] 5-Iodo-3-pyridyl ethers: syntheses and binding to neuronal nicotinic acetylcholine receptors
Autore:
Fan, H; Scheffel, UA; Rauseo, P; Xiao, YX; Dogan, AS; Yokoi, F; Hilton, J; Kellar, KJ; Wong, DF; Musachio, JL;
Indirizzi:
Johns Hopkins Univ, Sch Med, Dept Radiol, Div Nucl Med, Baltimore, MD 21287 USA Johns Hopkins Univ Baltimore MD USA 21287 cl Med, Baltimore, MD 21287 USA Johns Hopkins Univ, Sch Publ Hlth, Dept Environm Hlth Sci, Baltimore, MD 21205 USA Johns Hopkins Univ Baltimore MD USA 21205 th Sci, Baltimore, MD 21205 USA Georgetown Univ, Dept Pharmacol, Washington, DC 20007 USA Georgetown UnivWashington DC USA 20007 armacol, Washington, DC 20007 USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 8, volume: 28, anno: 2001,
pagine: 911 - 921
SICI:
0969-8051(200111)28:8<911:[5ESAB>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON-EMISSION-TOMOGRAPHY; IN-VIVO TRACER; ALZHEIMERS-DISEASE; ANALGESIC ACTIVITY; HUMAN BRAIN; AFFINITY; LIGAND; PYRIDINE; AGONIST; ANALOG;
Keywords:
iodine-123; nicotinic acetylcholine receptor; SPECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: Musachio, JL Johns Hopkins Univ, Sch Med, Dept Radiol, Div Nucl Med, Baltimore, MD 21287 USA Johns Hopkins Univ Baltimore MD USA 21287 more, MD 21287 USA
Citazione:
H. Fan et al., "[I-125/123] 5-Iodo-3-pyridyl ethers: syntheses and binding to neuronal nicotinic acetylcholine receptors", NUCL MED BI, 28(8), 2001, pp. 911-921

Abstract

Three 3-pyridyl ether nicotinic ligands-(S)-5-Iodo-3-[(2-pyrrolidinyl)-methoxy]pyridine (5-iodo-A-85865), (S)-5-Iodo-3-[1-(methyl)-2-pyrrolidinyl-methoxy]pyridine (5-todo-A-84543), and (S)-5-iodo-3-[1-methyl-(2-azetidinyl)-methoxy]pyridine (5-iodo-N-Me-A-85380) were labeled with I-125/I-123, and their ability to label high-affinity brain nicotinic acetylcholine receptors (nAChRs) was evaluated. The most promising ligand, [I-123/125] 5-iodo-A-85865, showed approximately 65% inhibition of radioactivity uptake in thalamusin mice pretreated with cytisine. Preliminary SPECT imaging studies with [I-123] 5-iodo-A-85865 revealed a distribution profile consistent with nAChRs (thalamus > frontal cortex > cerebellum) and a more rapid pharmacokineticprofile relative to azetidinyl 3-pyridyl ether based ligands. (C) 2001 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 17/09/19 alle ore 23:06:07