The automated radiosynthesis of [18F]FP-TZTP

被引：19

作者：

Kiesewetter, DO ^{[1
]}

Vuong, BK ^{[1
]}

Channing, MA ^{[1
]}

机构：

[1] NIH, Positron Emmiss Tomog Dept, Ctr Clin, Bethesda, MD 20892 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2003年 / 30卷 / 01期

关键词：

FP-TZTP; fluorine-18; muscarinic receptors;

D O I：

10.1016/S0969-8051(02)00354-2

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

[F-18]FP-TZTP (3-(3-(3-[F-18]fluoropropylthio)-1.2.5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine) is a muscarinic ligand that displays in vivo selectivity for the M2 subtype. We hake developed a one-step radiosynthesis of [F-18]FP-TZTP that can be conducted with an automated synthesis unit. A number of hardware and software modifications to a Nuclear Interface C-11 Methylation System provided the equipment for the automated radiosynthesis. The manual synthesis produced [F-18]FP-TZTP in a radiochemical yield of 23.4% +/- 4.3% (EOS, n = 69) with a specific activity of 4377 +/- 2011 mCi/mumol (EOB, n = 100). The automated synthesis unit provided the product in a radiochemical yield of 18.8% +/- 2.4% (EOS, n = 25) with a specific activity of 4112 +/- 2572 mCi/mumol (EOB, n = 25). Published by Elsevier Science Inc. All rights reserved.

引用

页码：73 / 77

页数：5

共 6 条

[1] Muscarinic cholinergic receptor measurements with [18F]FP-TZTP:: Control and competition studies [J].

Carson, RE ;

Kiesewetter, DO ;

Jagoda, E ;

Der, MG ;

Herscovitch, P ;

Eckelman, WC .

JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM, 1998, 18 (10) :1130-1142

[2] PREPARATION OF F-18 LABELED MUSCARINIC AGONIST WITH M2 SELECTIVITY [J].

KIESEWETTER, DO ;

LEE, JT ;

LANG, LX ;

PARK, SG ;

PAIK, CH ;

ECKELMAN, WC .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (01) :5-8

[3]

Kiesewetter DO, 1999, SYNAPSE, V31, P29, DOI 10.1002/(SICI)1098-2396(199901)31:1<29::AID-SYN5>3.0.CO

[4]

2-9

[5] Identification of metabolites of fluorine-18-labeled M2 muscarinic receptor agonist, 3-(3-[(3-fluoropropyl)thio]-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine, produced by human and rat hepatocytes [J].

Ma, Y ;

Kiesewetter, DO ;

Jagoda, EM ;

Huang, BX ;

Eckelman, WC .

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 2002, 766 (02) :319-329

[6] NOVEL FUNCTIONAL-M1 SELECTIVE MUSCARINIC AGONISTS - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 3-(1,2,5-THIADIAZOLYL)-1,2,5,6-TETRAHYDRO-1-METHYLPYRIDINES [J].

SAUERBERG, P ;

OLESEN, PH ;

NIELSEN, S ;

TREPPENDAHL, S ;

SHEARDOWN, MJ ;

HONORE, T ;

MITCH, CH ;

WARD, JS ;

PIKE, AJ ;

BYMASTER, FP ;

SAWYER, BD ;

SHANNON, HE .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (12) :2274-2283

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