A high yield robotic synthesis of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG) and 9-[3-[18F]fluoro-1-hydroxy-2-propoxy)methyl]guanine([18F] FHPG) for gene expression imaging.
The aim of this study was to develop an automated synthesis of 9-(4-[(18)F]-fluoro-3-hydroxymethylbutyl)guanine ([(18)F]FHBG) and 9-[(3-[(18)F]fluoro-1-hydroxy-2-propoxy)methyl]guanine ([(18)F]FHPG) using a Scanditronix Anatech RB III robotic system. [(18)F]HF was produced via (18)O(p, n)(18)F using a Scanditronix MC17F cyclotron. On average, a typical run produced [(18)F]FHBG and [(18)F]FHPG with an uncorrected radiochemical yield of 19% and 16%, respectively, at end of synthesis (EOS) from irradiation of 95% enriched [(18)O]water. The total synthesis time was 80 min. The retention time of [(18)F]FHBG and [(18)F]FHPG (the radio-peak) was 3.9 and 4.0 min, respectively, which was consistent with the [(19)F]FHBG and [(19)F]FHPG ultraviolet peak. The radiochemical purity was greater than 97%. A robotic, automated method for [(18)F]FHBG and [(18)F]FHPG radiosynthesis is therefore feasible. The radiation burden for the operator can be reduced as much as possible. Sufficient radioactivities of [(18)F]FHBG and [(18)F]FHPG could be obtained for non-invasive monitoring the expression of transfected gene in vivo with positron emission tomography (PET).
Chang
C W
CW
Institute of Radiological Sciences, National Yang-Ming University, No. 155, 2nd Sec., Li-Nong St., Taipei, Taiwan.
Lin
M
M
Wu
S Y
SY
Hsieh
C H
CH
Liu
R S
RS
Wang
S J
SJ
Huang
K L
KL
Chen
C H
CH
Wang
H E
HE
D004867:Equipment Design; D019544:Equipment Failure Analysis; D015774:Ganciclovir / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000302:isolation & purification; D020869:Gene Expression Profiling / Q000295:instrumentation / Q000379:methods*; D006147:Guanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000302:isolation & purification; D007553:Isotope Labeling / Q000295:instrumentation* / Q000379:methods; D015336:Molecular Probe Techniques; D049268:Positron-Emission Tomography / Q000295:instrumentation / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D012371:Robotics / Q000295:instrumentation* / Q000379:methods; D013048:Specimen Handling / Q000295:instrumentation* / Q000379:methods
C104325:9-((3-fluoro-1-hydroxy-2-propoxy)methyl)guanine; C113308:9-(4-fluoro-3-hydroxymethylbutyl)guanine; D019275:Radiopharmaceuticals; D006147:Guanine; D015774:Ganciclovir