...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Synthesis and initial in vitro characterization of a new P2X7R radioligand [F-18]IUR-1602
【24h】

Synthesis and initial in vitro characterization of a new P2X7R radioligand [F-18]IUR-1602

机译：新P2X7R放射性配体的合成和初始体外表征[F-18] IUR-1602

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The overexpression of P2X7R is associated with neuroinflammation and plays an important role in various neurodegenerative diseases. The [F-18]fluoropropyl derivative of GSK1482160, [F-18]IUR-1602, has been first prepared and examined as a new potential P2X7R radioligand. The reference standard IUR-1602 was synthesized from tert-butyl (S)-5-oxopyrrolidine-2-carboxylate, fluoropropylbromide, and 2-chloro-3-(trifluoromethyl)benzylamine with overall chemical yield 13% in three steps. The target tracer [F-18]IUR-1602 was synthesized from desmethyl-GSK1482160 with 3-[F-18]fluoropropyl tosylate, prepared from propane-1,3-diyl bis(4-methylbenzenesulfonate) and K[F-18]F/Kryptofix2.2.2, in two steps and isolated by HPLC combined with SPE in 2-7% decay corrected radiochemical yield. The radiochemical purity was 99%, and the molar activity at end of bombardment (EOB) was 74-370 GBq/mu mol. The potency of IUR-1602 in comparison with GSK1482160 was determined by a radioligand competitive binding assay using [C-11]GSK1482160, and the binding affinity K-i values for IUR-1602 and GSK1482160 are 23.6 and 3.07 nM, respectively. The initial in vitro evaluation results, 8-fold less potency of [F-18]IUR-1602 compared to [C-11]GSK1482160, prevent further in vivo evaluation of [F-18]IUR-1602 in animals and human.
机译：P2X7R的过表达与神经炎症有关，在各种神经变性疾病中起重要作用。首先制备GSK1482160，[F-18] IUR-1602的[F-18]氟丙基衍生物，并将其作为新电位P2X7R放射性配体检查。参考标准IUR-1602由叔丁基（S）-5-氧吡咯烷-2-羧酸丁酯，氟丙基溴化物和2-氯-3-（三氟甲基）苄胺合成，具有整体化学产率为13％，三个步骤。用丙烷-1,3-二乙基双（4-甲基苯磺酸盐）和K [F-18]合成，用3-[F-18]氟丙酯甲磺酸盐合成靶示踪剂[F-18] IUR-1602。 F / Kryptofix2.2.2，分两步，HPLC与SPE相结合2-7％衰减校正放射化学产量。放射化学纯度是＆轰炸末端（Eob）结束时的99％，摩尔活性为74-370 gbq / mu mol。与GSK1482160相比，IUR-1602的效力由使用[C-11] GSK1482160的放射性原竞争性结合测定法测定，并且Iur-1602和GSK1482160的结合亲和力K-I值分别为23.6和3.07nm。初始的体外评估结果，[F-18] IUR-1602的效力为8倍，与[C-11] GSK1482160相比，在动物和人中的[F-18] IUR-1602的体内评价进一步。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号