Rapid and reproducible radiosynthesis of [18F] FHBG

被引:38
作者
Ponde, DE [1 ]
Dence, CS [1 ]
Schuster, DP [1 ]
Welch, MJ [1 ]
机构
[1] Washington Univ, Sch Med, Edward Mallinckrodt Inst Radiol, Div Radiol Sci, St Louis, MO 63110 USA
关键词
F-18] FHBG; PET; thymidine kinase; gene therapy; solid phase purification; Oasis (R) HLB; microwave;
D O I
10.1016/S0969-8051(03)00096-9
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
9-(4-[F-18] Fluoro-3-hydroxymethylbutyl) guanine ([F-18] FHBG), an imaging agent for gene therapy using PET, was prepared in a one-pot, two-step synthesis. Microwave (MW) mediated nucleophilic fluorination of N-2, monomethoxytrityl-9-[4-(tosyl)-3-monomethoxytrityl-methylbutyl] guanine using no-carrier-added [F-18] fluoride, followed by deprotection with hydrochloric acid and HPLC purification, gave [F-18] FHBG. The radiochemical yield (decay corrected) was 12 +/- 5% (n = 35), the synthesis time was 55-60 min, and the radiochemical purity was >99%. The compound was used for lung imaging and was injected into Sprague-Dawley rats previously infected with the herpes simplex virus type 1 thymidine kinase (HSV1-tk) reporter gene. MicroPET imaging showed accumulation confined to the lungs. (C) 2004 Elsevier Inc. All rights reserved.
引用
收藏
页码:133 / 138
页数:6
相关论文
共 18 条
[1]   Synthesis and preliminary evaluation of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG):: A new potential imaging agent for viral infection and gene therapy using PET [J].
Alauddin, MM ;
Conti, PS .
NUCLEAR MEDICINE AND BIOLOGY, 1998, 25 (03) :175-180
[2]  
CHENG YC, 1983, J BIOL CHEM, V258, P2460
[3]   PREPARATION OF NCA [17-F-18]-FLUOROHEPTADECANOIC ACID IN HIGH YIELDS VIA AMINOPOLYETHER SUPPORTED, NUCLEOPHILIC FLUORINATION [J].
COENEN, HH ;
KLATTE, B ;
KNOCHEL, A ;
SCHULLER, M ;
STOCKLIN, G .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1986, 23 (05) :455-466
[4]  
Dence C. S., 1995, Journal of Labelled Compounds and Radiopharmaceuticals, V37, P115
[5]   Imaging adenoviral-directed reporter gene expression in living animals with positron emission tomography [J].
Gambhir, SS ;
Barrio, JR ;
Phelps, ME ;
Iyer, M ;
Namavari, M ;
Satyamurthy, N ;
Wu, L ;
Green, LA ;
Bauer, E ;
MacLaren, DC ;
Nguyen, K ;
Berk, AJ ;
Cherry, SR ;
Herschman, HR .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1999, 96 (05) :2333-2338
[6]   Imaging gene expression: Principles and assays [J].
Gambhir, SS ;
Barrio, JR ;
Herschman, HR ;
Phelps, ME .
JOURNAL OF NUCLEAR CARDIOLOGY, 1999, 6 (02) :219-233
[7]   NO-CARRIER-ADDED SYNTHESIS OF 3-[F-18]FLUORO-1-(2-NITRO-1-IMIDAZOLYL)-2-PROPANOL - A POTENTIAL PET AGENT FOR DETECTING HYPOXIC BUT VIABLE TISSUES [J].
HWANG, DR ;
DENCE, CS ;
BONASERA, TA ;
WELCH, MJ .
APPLIED RADIATION AND ISOTOPES, 1989, 40 (02) :117-126
[8]   APPLICATION OF MICROWAVE TECHNOLOGY TO THE SYNTHESIS OF SHORT-LIVED RADIOPHARMACEUTICALS [J].
HWANG, DR ;
MOERLEIN, SM ;
LANG, L ;
WELCH, MJ .
JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS, 1987, (23) :1799-1801
[9]   APPLICATION OF MICROWAVE-HEATING TO THE SYNTHESIS OF [F-18] FLUOROMISONIDAZOLE [J].
MCCARTHY, TJ ;
DENCE, CS ;
WELCH, MJ .
APPLIED RADIATION AND ISOTOPES, 1993, 44 (08) :1129-1132
[10]  
PENUELAS I, 2003, MOL IMAGING BIOL, V4, P415, DOI DOI 10.1016/S1536-1632(02)00086-0