연세의료원 / 박준영, 전중현*
Abstract
(E)-3-(Pyridin-2-yl ethynyl)cyclohex-2-enone O-(3-(2-[18 F]-fluoroethoxy)propyl) oxime ([18 F]-(E)-PSS232, [18 F]2a) is a recently developed radiotracer that can be used to visualize metabotropic glutamate receptor subtype 5 (mGlu5 ) in vivo. The mGlu5 has become an attractive therapeutic and diagnostic target owing to its role in many neuropsychiatric disorders. Several carbon-11-labeled and fluorine-18-labeled radiotracers have been developed to measure mGlu5 receptor occupancy in the human brain. The radiotracer [18 F]2a, which is used as an analogue for [11 C]ABP688 ([11 C]1) and has a longer physical half-life, is a selective radiotracer that exhibits high binding affinity for mGlu5 . Herein, we report the fully automated radiosynthesis of [18 F]2a using a commercial GE TRACERlab™ FX-FN synthesizer for routine production and distribution to nearby satellite clinics. Nucleophilic substitution of the corresponding mesylate precursor with cyclotron-produced [18 F]fluoride ion at 100°C in dimethyl sulfoxide (DMSO), followed by high-performance liquid chromatography (HPLC) purification and formulation, readily provided [18 F]2a with a radiochemical yield of 40 ± 2% (decay corrected, n = 5) at the end of synthesis. Radiochemical purity for the [18 F]-(E)-conformer was greater than 95%. Molar activity was determined to be 63.6 ± 9.6 GBq/μmol (n = 5), and the overall synthesis time was 70 minutes.
Author information
Park JY1, Son J1, Yun M1,2, Ametamey SM3, Chun JH2.
1
Department of Nuclear Medicine, Severance Hospital, Yonsei University Health System, Seoul, Republic of Korea.
2
Department of Nuclear Medicine, Yonsei University College of Medicine, Seoul, Republic of Korea.
3
Department of Applied Biosciences of ETH Zurich, Center for Radiopharmaceutical Sciences of ETH, PSI, and USZ, Zurich, Switzerland.
편집위원
신경정신계 장애를 생체영상화 하기 위한 PET 영상용 방사성의약품인 [18F]‐(E)‐PSS232 ((E)‐3‐(Pyridin‐2‐yl ethynyl)cyclohex‐2‐enone O‐(3‐(2‐[18F]‐fluoroethoxy)pro-pyl) oxime)의 자동화 합성법에 관한 논문입니다.
2018-02-07 13:16:26
편집위원
이는 metabotropic glutamate receptor subtype 5 (mGlu5)를 in vivo영상화 하지만 반감기가 20분으로 짧아서 사용하기 어려운 [11C]ABP688의 유사체로 개발된 F-18 표지 약품으로, mGlu5에 높은 binding affinity를 보여주며 반감기가 더 길기 때문에 향후 임상 적용 후 결과가 기대됩니다.
2018-02-07 13:17:53