کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1879411 | 1042566 | 2009 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: An improved radiosynthesis of the muscarinic M2 radiopharmaceutical, [18F]FP-TZTP An improved radiosynthesis of the muscarinic M2 radiopharmaceutical, [18F]FP-TZTP](/preview/png/1879411.png)
The radioligand 3-(4-(3-[18F]fluoropropylthio)-1,2,5-thiadiazol-3-yl)-1-methyl-1,2,5,6-tetrahydropyridine ([18F]FP-TZTP) is an agonist with specificity towards subtype 2 of muscarinic acetylcholine (M2) receptors. It is currently the only radiotracer available for imaging M2 receptors in human subjects with positron emission tomography. The present study reports on an improved method for the synthesis of [18F]FP-TZTP, automated using a GE TRACERlab™ FXFN radiosynthesis module. A key facet was the use of a new precursor, 3-(4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazol-3-ylthio)propyl 4-methylbenzenesulfonate. The precursor was fluorinated via nucleophilic displacement of the tosyloxy group by potassium cryptand [18F]fluoride (K[18F]/K222) in CH3CN at 80 °C for 5 min, and purified by HPLC. Formulated [18F]FP-TZTP was prepared in an uncorrected radiochemical yield of 29±4%, with a specific activity of 138±41 GBq/μmol (3732±1109 mCi/μmol) at the end of synthesis (35 min; n=3). This methodology offers higher yields, faster synthesis times, an optimized precursor, and simpler automation than previously reported.
Journal: Applied Radiation and Isotopes - Volume 67, Issue 4, April 2009, Pages 611–616