2'-[18F]氟马西尼（[18F]FFMZ）作为一种潜在的用于正电子发射断层显像（PET）的GABA受体配体的生物学评价。
Biological evaluation of 2'-[18F]fluoroflumazenil ([18F]FFMZ), a potential GABA receptor ligand for PET.
作者信息
Mitterhauser Markus, Wadsak Wolfgang, Wabnegger Leila, Mien Leonhard-Key, Tögel Stefan, Langer Oliver, Sieghart Werner, Viernstein Helmut, Kletter Kurt, Dudczak Robert
机构信息
Institute for Brain Research, University of Vienna, and Hospital Pharmacy of the General Hospital, Austria.
出版信息
Nucl Med Biol. 2004 Feb;31(2):291-5. doi: 10.1016/j.nucmedbio.2003.09.003.
[(11)C]Flumazenil, a highly selective benzodiazepine antagonist is the most extensively used GABA(A) ligand for PET so far. To overcome half life disadvantages of (11)C a [(18)F]-labeled flumazenil derivative, 2'-[(18)F]fluoroflumazenil (FFMZ) was developed and biologically evaluated with respect to the GABA(A) receptor. Organ with the highest uptake was the pituitary gland. Brain uptake was high and followed the order cortex>thalamus>cerebellum>rest brain. Fluoroflumazenil displaced [(3)H]flumazenil binding from membrane GABA(A) receptors with an IC(50)value (3.5 nM) comparable to that of Flumazenil (2.8 nM). The presented data confirm the potential of [(18)F]FFMZ for PET imaging of the GABA-ergic system.
[11C]氟马西尼是一种高度选择性的苯二氮䓬拮抗剂，是迄今为止PET中使用最广泛的GABA(A)配体。为克服[11C]的半衰期缺点，开发了一种[18F]标记的氟马西尼衍生物，即2'-[18F]氟氟马西尼（FFMZ），并对其进行了关于GABA(A)受体的生物学评估。摄取量最高的器官是垂体。脑摄取量较高，顺序为皮质>丘脑>小脑>其余脑区。氟氟马西尼从膜GABA(A)受体上取代[3H]氟马西尼结合，其IC50值（3.5 nM）与氟马西尼（2.8 nM）相当。所呈现的数据证实了[18F]FFMZ用于GABA能系统PET成像的潜力。
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