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Titolo:
Synthesis and evaluation of radiolabeled piperazine derivatives of vesamicol as SPECT agents for cholinergic neurons
Autore:
Bando, K; Taguchi, K; Ginoza, Y; Naganuma, T; Tanaka, Y; Koike, K; Takatoku, K;
Indirizzi:
Daiichi Radioisotope Labs Ltd, Res Ctr, Chiba 2891592, Japan Daiichi Radioisotope Labs Ltd Chiba Japan 2891592 , Chiba 2891592, Japan Toho Univ, Sch Pharmaceut Sci, Dept Chem Pharmacol, Funabashi, Chiba 2748510, Japan Toho Univ Funabashi Chiba Japan 2748510 , Funabashi, Chiba 2748510, Japan
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 3, volume: 28, anno: 2001,
pagine: 251 - 260
SICI:
0969-8051(200104)28:3<251:SAEORP>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
VESICULAR ACETYLCHOLINE TRANSPORTER; CENTRAL-NERVOUS-SYSTEM; ALZHEIMERS-DISEASE; RECEPTOR RADIOLIGANDS; RAT-BRAIN; AFFINITY; IMMUNOHISTOCHEMISTRY; ACETYLTRANSFERASE; BENZOVESAMICOL; ABNORMALITIES;
Keywords:
autoradiography; cholinergic; radioiodinated ligand; synaptic vesicle; vesamicol; vesicular acetylcholine transporter;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Bando, K Daiichi Radioisotope Labs Ltd, Res Ctr, 453-1 Shimo-Okura, Chiba 2891592, Japan Daiichi Radioisotope Labs Ltd 453-1 Shimo-Okura Chiba Japan2891592
Citazione:
K. Bando et al., "Synthesis and evaluation of radiolabeled piperazine derivatives of vesamicol as SPECT agents for cholinergic neurons", NUCL MED BI, 28(3), 2001, pp. 251-260

Abstract

To diagnose and investigate neurodegenerative diseases affecting cholinergic neuron density, piperazine derivatives of vesamicol were synthesized andevaluated. Previously, we reported that trans-5-iodo-2-hydroxy-3-[4-phenylpiperazinyl] tetralin (DRC140, 1) pos ses sed high selectivity for vesicular acetylcholine transporter (VAChT). In present study of the effect of alkyl substituents, we observed that the introduction of a methyl group into the ortho or meta positions of the phenyl group of 1 increased affinity for VAChT. trans-5-Iodo-2-hydroxy-3-[4-[2-methylphenyl] piperazinyl]tetralin (2)displayed high affinity and specificity for VAChT. The regional distributions of radioactivity in the rat brain correlated well with known patterns of central cholinergic innervation. [I-123]2 is a potentially useful compound for SPECT imaging. (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 26/01/20 alle ore 01:16:57