Yoon Young Hyun, Jeong Jae Min, Kim Hyung Woo, Hong Sung Hyun, Lee Yun-Sang, Kil Hee Sup, Chi Dae Yoon, Lee Dong Soo, Chung June-Key, Lee Myung Chul
Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul, South Korea.
Nucl Med Biol. 2003 Jul;30(5):521-7. doi: 10.1016/s0969-8051(03)00030-1.
We describe the synthesis of 2'-[(18)F]fluoroflumazenil (FFMZ), which differs from the typically used [(18)F]fluoroethylflumazenil (FEFMZ) for benzodiazepine receptor imaging. For one-pot one-step labeling, the precursors, 2'-tosyloxyflumazenil (TFMZ) and 2'-mesyloxyflumazenil (MFMZ), were synthesized in three steps. The precursors were successfully labeled with no-carrier-added (18)F-fluoride which was activated by repeated azeotropic distillation with Kryptofix 2.2.2./potassium carbonate in MeCN. An automated system for labeling and purification of [(18)F]FFMZ was developed. Labeling efficiency and radiochemical purity of [(18)F]FFMZ after synthesis by the automated system were 68% and 98%, respectively. Specific binding of [(18)F]FFMZ to central benzodiazepine receptor of rats was demonstrated by phosphoimaging.
我们描述了2'-[(18)F]氟马西尼（FFMZ）的合成，它与用于苯二氮䓬受体成像的典型的[(18)F]氟乙基氟马西尼（FEFMZ）不同。对于一锅一步法标记，前体2'-甲苯磺酰氧基氟马西尼（TFMZ）和2'-甲磺酰氧基氟马西尼（MFMZ）分三步合成。前体用无载体添加的(18)F氟化物成功标记，该氟化物通过与Kryptofix 2.2.2./碳酸钾在乙腈中反复共沸蒸馏来活化。开发了一种用于[(18)F]FFMZ标记和纯化的自动化系统。通过自动化系统合成后，[(18)F]FFMZ的标记效率和放射化学纯度分别为68%和98%。通过磷成像证明了[(18)F]FFMZ与大鼠中枢苯二氮䓬受体的特异性结合。
