[carbonyl-11C]WAY-100635 | 162760-97-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: [carbonyl-11C]WAY-100635
• 英文别名: [carbonyl-(11C)]cyclohexanecarboxylic acid {2-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethyl}-pyridin-2-yl-amide；[carbonyl-C-11]-{2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl}-N-(2-pyridinyl)cyclohexanecarboxamide；[carbonyl-(11)C]-WAY-100635；(Carbonyl-(11)C)Way 100635；N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide
• CAS: 162760-97-6
• 化学式: C₂₅H₃₄N₄O₂
• 分子量: 421.56
• InChiKey: SBPRIAGPYFYCRT-FNNGWQQSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  48.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1-(2-methoxyphenyl)-4-(2-(2-pyridylamino)ethyl)piperazine 、 [carbonyl-11C]cyclohexanecarbonyl chloride 在 TEA 作用下， 反应 0.1h， 生成 [carbonyl-11C]WAY-100635
  参考文献：
  名称：

  Truong, P.; Krasikova, R.N.; Halldin, C., Journal of labelled compounds and radiopharmaceuticals, 2003, vol. 46, p. S244 - S244

  摘要：

  DOI：

文献信息

• Method for the use of [11C] carbon monoxide in labeling synthesis of 11C-labelled amides using metal amides and photo-induced free radical carbonylation
  申请人：Itsenko Oleksiy

  公开号：US20060133998A1

  公开（公告）日：2006-06-22

  Methods and reagents for photo-initiated carbonylation with carbon-isotope labeled carbon monoxide using weakly nucleophilic amines and alkyl/aryl iodides are provided. The resultant carbon-isotope labeled amides are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.

  提供了使用弱亲核胺和烷基/芳基碘进行碳同位素标记一氧化碳的光引发羰基化的方法和试剂。所得的碳同位素标记酰胺可用作放射性药物，特别适用于正电子发射断层扫描（PET）中。同时还提供了用于PET研究的相关试剂盒。
• [EN] RADIOLABELED COMPOUNDS AND METHODS THEREOF<br/>[FR] COMPOSÉS RADIOMARQUÉS ET LEURS PROCÉDÉS
  申请人：GE HEALTHCARE LTD

  公开号：WO2011150183A1

  公开（公告）日：2011-12-01

  The present invention relates to radiodiagnostic compounds, methods of making those compounds, and methods of use thereof as imaging agents for preferably a HA serotonin 5-HT1A receptor for use in PET or SPECT, preferably PET. Compositions comprising an imaging-effective amount of radiolabeled compounds are also disclosed. The present invention also relates to non-radiolabeled compounds, methods of making those compounds, and methods of use thereof to treat various neurological and/or psychiatric disorders.

  本发明涉及放射诊断化合物，制备这些化合物的方法，以及将其用作HA血清素5-HT1A受体的成像剂，用于PET或SPECT，更好地使用PET的方法。还披露了包含放射标记化合物的成像有效量的组合物。本发明还涉及非放射标记化合物，制备这些化合物的方法，以及将其用于治疗各种神经学和/或精神疾病的方法。
• EFFICIENT SYNTHETIC METHOD OF 18F-MEFWAY PRECURSOR
  申请人：RYU Young Hoon

  公开号：US20120136152A1

  公开（公告）日：2012-05-31

  The present invention relates a novel method for preparing an 18 F-mefway precursor. The present invention provides an efficient synthetic method of an 18 F-mefway precursor, which comprises an improved the acid chloride coupling reaction and proper reduction condition to suppress breakdown of amide bond and can obtain the precursor in high yield.

  本发明涉及一种制备18F-mefway前体的新方法。本发明提供了一种高效的合成方法，包括改进的酸氯化物偶联反应和适当的还原条件，以抑制酰胺键的降解，并可以高产率地获得前体。
• COMPOSITIONS AND METHODS RELATED TO SEROTONIN 5-HT1A RECEPTORS
  申请人：Mukherjee Jogeshwar

  公开号：US20070196271A1

  公开（公告）日：2007-08-23

  Contemplated substituted arylpiperazinyl compounds, and most preferably 18 F-Mefway, exhibit desirable in vitro and in vivo binding characteristics to the 5-HT1A receptor. Among other advantageous parameters, contemplated compounds retain high binding affinity, display optimal lipophilicity, and are radiolabeled efficiently with 18 F-fluorine in a single step. Still further, contemplated compounds exhibit high target to non-target ratios in receptor-rich regions both in vitro and in vivo, and selected compounds can be effectively and sensitively displaced by serotonin, thus providing a quantitative tool for measuring 5-HT1A receptors and serotonin concentration changes in the living brain.

  考虑替代芳基哌嗪类化合物，最好是18F-Mefway，展示出理想的体外和体内与5-HT1A受体结合特性。在其他有利参数中，考虑的化合物保留高结合亲和力，显示出最佳的亲脂性，并且能够通过单步骤高效地用18F-氟标记。此外，考虑的化合物在体外和体内的受体丰富区域展现出高的靶向与非靶向比例，而且选定的化合物可以被5-羟色胺有效敏感地置换，从而提供了一种用于测量活体大脑中5-HT1A受体和5-羟色胺浓度变化的定量工具。
• SEROTONERGIC AGENTS FOR TREATING SEXUAL DYSFUNCTION
  申请人：SUKOFF RIZZO J. Stacey

  公开号：US20080070925A1

  公开（公告）日：2008-03-20

  Methods and compositions are provided for treating sexual dysfunction, e.g., sexual dysfunction associated with drug treatment, using 5-HT 1A receptor antagonists.

  提供了用于治疗性功能障碍（例如与药物治疗有关的性功能障碍）的方法和组合物，使用5-HT1A受体拮抗剂。