[18F] Cranial nerve inflammation target proton emission tomography radiotracer introduced with fluoromethyl group, synthesis of these, and evaluation method of biological results using the same.
The present invention relates to a cranial neuroinflammation target proton emission tomography radiotracer into which a [18F] fluoromethyl group is introduced, its synthesis, and a method for evaluating biological results using the same. In the present invention, [18F] fluoroiodomethane labeled with 18F is introduced into PBR28-OH, which is a prosthetic group, in two stages, or 18F is obtained in one stage with a high yield using a triazolium triflate precursor. An 18F-labeled radioactive tracer into which a fluoromethyl group was introduced was obtained by substitution. Comparative evaluation of pharmacokinetics of known [11C] PBR28 with in vitro binding affinity, lipophilicity, and cranial nerve inflammation model revealed that 18F-labeled radiotracer had similar binding affinity, lipophilicity to [11C] PBR28 Confirmed to have sex. Furthermore, in the PET image comparison evaluation in the cranial nerve inflammation model, it was confirmed that the 18F-labeled radioactive tracer had excellent selective / specific intake in the inflammatory area at an earlier time, and high stability was confirmed at the cranial nerve inflammation site. did. According to the present invention, the synthesis of 18F-labeled radioactive tracer for new cranial nerve inflammation target PET and the diagnosis of cranial nerve inflammatory diseases, 18F having a longer half-life than [11C] PBR28 has minimal structural changes. It is expected to be a radiotracer for cranial nerve inflammation target PET, which can be excellently labeled and can be used effectively after its excellent selective and specific imaging and pharmacokinetic advantages have been verified. [Selection] Figure 2本発明は、[１８Ｆ]フルオロメチル基が導入された脳神経炎症標的陽子放出断層撮影放射性追跡子、その合成及びそれを用いた生物学的結果の評価方法に関する。本発明は、ＰＢＲ２８－ＯＨに補欠グループであるジヨードメタンに１８Ｆを標識した[１８Ｆ]フルオロヨードメタンを２段階で導入したり、トリアゾリウムトリフラート前駆体を用いて１８Ｆを１段階、高収率で置換してフルオロメチル基が導入された１８Ｆ標識放射性追跡子を得た。既知の［１１Ｃ］ＰＢＲ２８と体外結合親和性、脂肪親和性、及び脳神経炎症モデルでの薬物動態学の比較評価の結果、１８Ｆ標識放射性追跡子が［１１Ｃ］ＰＢＲ２８と類似した結合親和性、脂肪親和性を持つことを確認した。更に、脳
