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Titolo:
IN-VIVO EVALUATION OF [F-18] 3-FLUOROPROPYL)-4-(4-CYANOPHENOXYMETHYL)PIPERIDINE - A SELECTIVE SIGMA-1 RECEPTOR RADIOLIGAND FOR PET
Autore:
WATERHOUSE RN; COLLIER TL;
Indirizzi:
DUKE UNIV,MED CTR,DEPT RADIOL,MSRB BOX 2610 DURHAM NC 27710 AUSTRALIAN NUCL SCI & TECHNOL ORG,RADIOPHARMACEUT DIV MENAI NSW 2234 AUSTRALIA
Titolo Testata:
Nuclear medicine and biology
fascicolo: 2, volume: 24, anno: 1997,
pagine: 127 - 134
SICI:
0969-8051(1997)24:2<127:IEO[3>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
MALIGNANT-MELANOMA; RAT-BRAIN; BINDING-SITES; HIGH-AFFINITY;
Keywords:
SIGMA RECEPTORS; PET; F-18; RADIOTRACERS; TUMOR IMAGING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
29
Recensione:
Indirizzi per estratti:
Citazione:
R.N. Waterhouse e T.L. Collier, "IN-VIVO EVALUATION OF [F-18] 3-FLUOROPROPYL)-4-(4-CYANOPHENOXYMETHYL)PIPERIDINE - A SELECTIVE SIGMA-1 RECEPTOR RADIOLIGAND FOR PET", Nuclear medicine and biology, 24(2), 1997, pp. 127-134

Abstract

3-Fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine (1) has been synthesized as a selective high affinity (Ki = 4.3 nM) ligand for sigma-1 receptors (Ki sigma-1/sigma 2 = 0.03), The corresponding radioligand, F-18-1, was synthesized via nucleophilic [F-18]fluoride displacement from the appropriate N-alkylmesylate precursor. After HPLC purification,F-18-1 was obtained in 56-70% EOB (n = 5) with a specific activity > 74,000 MBq/mu mol. In vivo distribution and pharmacological blocking studies using F-18-1 were performed in male Australian Albino Wistar rats. F-18-1 exhibited high brain uptake (2.47 +/- 0.37 %ID at 20 min PI) with no significant loss of radioactivity from the brain over the course of the study (4 h), The uptake of radioactivity in the brain, lung, heart, and kidney was reduced significantly by the pre administration sigma receptor-binding ligands, indicating the in vivo specificity of the ligand, The radiotracer also exhibited high uptake (11.14 +/- 1.99 %ID/g) in B16 melanoma tumours in nude mice, The mean tumour/ tissue ratios at 4 h for the blood, muscle, lung and brain were 123.8, 7.2, 2.5 and 2.6, respectively. In view of these results, F-18-1 shows promise for the in vivo tomographic evaluation of sigma receptors. (C) 1997 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 14/07/20 alle ore 11:12:09