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Titolo:
SYNTHESIS AND EVALUATION OF [F-18] LABELED BENZAMIDES - HIGH-AFFINITYSIGMA-RECEPTOR LIGANDS FOR PET IMAGING
Autore:
DENCE CS; JOHN CS; BOWEN WD; WELCH MJ;
Indirizzi:
WASHINGTON UNIV,SCH MED,MALLINCKRODT INST RADIOL,BOX 8225,510 S KINGSHIGHWAY BLVD ST LOUIS MO 63110 WASHINGTON UNIV,SCH MED,MALLINCKRODT INST RADIOL ST LOUIS MO 63110 GEORGE WASHINGTON UNIV,MED CTR WASHINGTON DC 20037 NIDDKD,NIH BETHESDA MD 20892
Titolo Testata:
Nuclear medicine and biology
fascicolo: 4, volume: 24, anno: 1997,
pagine: 333 - 340
SICI:
0969-8051(1997)24:4<333:SAEO[L>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
MALIGNANT-MELANOMA; AUTORADIOGRAPHIC LOCALIZATION; ANTIPSYCHOTIC-DRUGS; BINDING-SITES; GUINEA-PIG; BRAIN; TUMORS; CELLS;
Keywords:
F-18; POSITRON EMISSION TOMOGRAPHY; BENZAMIDES; SIGMA RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
34
Recensione:
Indirizzi per estratti:
Citazione:
C.S. Dence et al., "SYNTHESIS AND EVALUATION OF [F-18] LABELED BENZAMIDES - HIGH-AFFINITYSIGMA-RECEPTOR LIGANDS FOR PET IMAGING", Nuclear medicine and biology, 24(4), 1997, pp. 333-340

Abstract

We have synthesized and characterized four new fluorinated halobenzamides as sigma receptor ligands for use with positron emission tomography (PET). All the compounds were found to have high sigma-1 affinities(K-i = 0.38-0.98 nM), and the 4-fluoro substituted benzamides were found to he more potent sigma-2 ligands (K-i = 3.77-4.02 nM) than their corresponding 2-fluoro analogs (K-i = 20.3-22.8 nM). The [F-18] radiochemical syntheses of two of the analogs gave overall yields between 3-10% (EOS), radiochemical purities >99%, and specific activities between 800-1200 Ci/mmol (29.6-44.4 TBq/mmol). Rat biodistribution and blocking experiments were performed with 2-[F-18]( N-fluorobenzylpiperidin-4yl)-4-iodobenzamide, the analog with the best K-i value for sigma-1 sites (0.38 nM). Results of these experiments demonstrate specific uptake of the compound in tissues believed to contain sigma receptors, such as lungs, kidneys, heart, brain, and spleen and indicate its potential as a candidate for use in PET imaging of tissues containing these receptors. (C) 1997 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 09:05:45