Simple, rapid and reliable preparation of [¹¹C]-(+)-α-DTBZ of high quality for routine applications.
[¹¹C]-(+)-α-DTBZ has been used as a marker of dopaminergic terminal densities in human striatum and expressed in islet beta cells in the pancreas. We aimed to establish a fully automated and simple procedure for the synthesis of [¹¹C]-(+)-α-DTBZ for routine applications. [¹¹C]-(+)-α-DTBZ was synthesized from a 9-hydroxy precursor in acetone and potassium hydroxide with [¹¹C]-methyl triflate and was purified by solid phase extraction using a Vac tC-18 cartridge. Radiochemical yields based on [¹¹C]-methyl triflate (corrected for decay) were 82.3% ± 3.6%, with a specific radioactivity of 60 GBq/μmol. Time elapsed was less than 20 min from end of bombardment to release of the product for quality control.
Department of Nuclear Medicine, the PLA General Hospital, Beijing 100853, China. zhangjm301@163.com.
Jinming
J
Zhang
Xiaojun
X
Zhang
Yungang
Y
Li
Jiahe
J
Tian
D000818:Animals; D002250:Carbon Radioisotopes; D051379:Mice; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000493:pharmacokinetics; D013747:Tetrabenazine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000302:isolation & purification; D014018:Tissue Distribution
C575320:(11C)-(+)-alpha-dihydrotetrabenazine; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D013747:Tetrabenazine