[18F]N-(2-苯并呋喃甲基)-N'-[4-(2-氟乙氧基)苄基]哌嗪的合成及体内评价，一种新型 σ1 受体 PET 成像剂。
Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent.
机构信息
School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia.
出版信息
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6820-3. doi: 10.1016/j.bmcl.2011.09.028. Epub 2011 Sep 13.
N-(2-Benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine (6, σ(1)K(i)=2.6 nM) was radiolabeled with fluorine-18 to provide a potential σ(1) receptor radioligand for use in positron emission tomography (PET). Radiofluorination of the appropriate tosylate precursor furnished [(18)F]6 with a specific activity of 45 GBq/μmol, in an average radiochemical yield of 18% and greater than 98% radiochemical purity. MicroPET imaging in Papio hamadryas baboon brain revealed [(18)F]6 uptake consistent with σ receptor distribution, and specificity for σ receptors was demonstrated in a haloperidol pre-treated animal. [(18)F]6 possesses suitable properties for PET imaging of σ(1) receptors, and further investigation of this σ(1) receptor tracer is warranted.
N-(2-苯并呋喃甲基)-N'-[4-(2-氟乙氧基)苄基]哌嗪（6，σ(1)K(i)=2.6 nM）被放射性标记氟-18，以提供一种潜在的用于正电子发射断层扫描（PET）的 σ(1)受体放射性配体。适当的 tosylate 前体的放射性氟化提供了 [(18)F]6，其比活度为 45 GBq/μmol，平均放射化学产率为 18%以上，放射化学纯度大于 98%。在 Papio hamadryas baboon 大脑中的 MicroPET 成像显示 [(18)F]6 的摄取与 σ 受体分布一致，并在氟哌啶醇预处理的动物中证明了对 σ 受体的特异性。[(18)F]6 具有用于 PET 成像 σ(1)受体的合适特性，进一步研究这种 σ(1)受体示踪剂是有必要的。
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