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（18）F 标记的 S-氟烷基二芳基胍的合成及体外评价：新型高亲和力 NMDA 受体拮抗剂用于 PET 成像。

Synthesis and in vitro evaluation of (18)F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET.

机构信息

GE Healthcare MDx Research, MRC Cyclotron Building, Hammersmith Hospital, London W12 0NN, United Kingdom.

出版信息

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1749-51. doi: 10.1016/j.bmcl.2010.01.052. Epub 2010 Jan 20.

DOI:10.1016/j.bmcl.2010.01.052
PMID:20138515
Abstract

Two S-[(18)F]fluoroalkylated diarylguanidines were synthesized and evaluated in vitro as potential tracers for imaging of N-methyl-d-aspartate receptors (NMDARs) with positron emission tomography (PET). [(18)F]1 and [(18)F]10 were synthesized by [(18)F]fluoroethylation and [(18)F]fluoromethylation of the thiol precursor 6, respectively. [(18)F]1 is a promising candidate NMDAR PET tracer, with low nanomolar affinity for the NMDA PCP-site, high selectivity and moderate lipophilicity.

摘要

两种 S-[(18)F]二芳基胍被合成并在体外进行评估，作为正电子发射断层扫描 (PET) 成像 N-甲基-D-天冬氨酸受体 (NMDAR) 的潜在示踪剂。[(18)F]1 和 [(18)F]10 分别通过 [(18)F]氟乙基化和 [(18)F]氟甲基化硫醇前体 6 合成。[(18)F]1 是一种很有前途的 NMDAR PET 示踪剂，对 NMDA PCP 位点具有低纳摩尔亲和力、高选择性和适度的亲脂性。

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