[11C]methylamine | 6044-76-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: [11C]methylamine
• 英文别名: [(11)C]methyl iodide；(111C)methanamine
• CAS: 6044-76-4
• 化学式: CH₅N
• 分子量: 30.0464
• InChiKey: BAVYZALUXZFZLV-BJUDXGSMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  2
• 可旋转键数：
  0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  [11C]methylamine 、 (2S)-2-[(2-chlorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno-[2,3-c]pyran-7,4'-piperidine]-1'-yl)propanamide 在 potassium hydroxide 作用下， 以 二甲基亚砜 为溶剂， 反应 0.08h， 生成 (2S)-2-[(2-chlorophenyl)methyl]-3-(2-fluorospiro[4,5-dihydrothieno-[2,3-c]pyran-7,4'-piperidine]-1'-yl)-N-[(11)C-methyl]propanamide
  参考文献：
  名称：

  Synthesis and Evaluation of Radioligands for Imaging Brain Nociceptin/Orphanin FQ Peptide (NOP) Receptors with Positron Emission Tomography

  摘要：

  Positron emission tomography (PET) coupled to an effective radioligand could provide an important tool for understanding possible links between neuropsychiatric disorders and brain NOP (nociceptin/orphanin FQ peptide) receptors. We sought to develop such a PET radioligand. High-affinity NOP ligands were synthesized based on a 3-(2'-fluoro-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran]-1-yl)-2(2-halobenzyl)-N-alkylpropanamide scaffold and from experimental screens in rats, with ex vivo LC-MS/MS measures, three ligands were identified for labeling with carbon-11 and evaluation with PET in monkey. Each ligand was labeled by C-11-methylation of an N-desmethyl precursor and studied in monkey under baseline and NOP receptor-preblock conditions. The three radioligands, [C-11] (S) 10a-c, gave similar results. Baseline scans showed high entry of radioactivity into the brain to give a distribution reflecting that expected for NOP receptors. Preblock experiments showed high early peak levels of brain radioactivity, which rapidly declined to a Much lower level than seen in baseline scans, thereby indicating a high level of receptor-specific binding in baseline experiments. Overall, [C-11](S)-10c showed the most favorable receptor-specific signal and kinetics and is now selected for evaluation in human subjects.

  DOI：

  10.1021/jm101487v
• 作为产物：
  描述：

  [11C]methyl iodide 在 氨 作用下， 生成 [11C]methylamine
  参考文献：
  名称：

  Gilissen; Bormans; De Groot, Journal of labelled compounds and radiopharmaceuticals, 1999, vol. 42, # SUPPL. 1, p. S443-S444

  摘要：

  DOI：

文献信息

• Synthesis and Preliminary Evaluation of [ ¹¹ C]GNE‐1023 as a Potent PET Probe for Imaging Leucine‐Rich Repeat Kinase 2 (LRRK2) in Parkinson's Disease
  作者：Zhen Chen、Tuo Shao、Wei Gao、Hualong Fu、Thomas Lee Collier、Jian Rong、Xiaoyun Deng、Qingzhen Yu、Xiaofei Zhang、April T. Davenport、James B. Daunais、Hsiao‐Ying Wey、Yihan Shao、Lee Josephson、Wen‐Wei Qiu、Steven Liang

  DOI：10.1002/cmdc.201900321

  日期：2019.9.4

  mainly conferred by LRRK2 mutations that bring about increased kinase activity. As a consequence, selective inhibition of LRRK2 may help to recover the normal functions of LRRK2, thereby serving as a promising alternative therapeutic target for PD treatment. The mapping of LRRK2 by positron emission tomography (PET) studies allows a thorough understanding of PD and other LRRK2-related disorders; it also

  富含亮氨酸的重复激酶2（LRRK2）是参与帕金森氏病（PD）发病机理的一种大蛋白。已经证实PD主要由带来激酶活性增加的LRRK2突变赋予。结果，选择性抑制LRRK2可能有助于恢复LRRK2的正常功能，从而成为有前途的PD治疗替代治疗靶点。通过正电子发射断层扫描（PET）研究对LRRK2进行定位，可以全面了解PD和其他与LRRK2相关的疾病。它还有助于验证和翻译新型LRRK2抑制剂。但是，在原始文献中尚未报道LRRK2 PET探针。本文中，我们提出了[11 C] GNE-1023的简便合成和初步评估，它是用于PD中LRRK2成像的新型强效PET探针。[11 C] GNE-1023的合成具有良好的放射化学收率（10％未经衰变校正的RCY），优异的放射化学纯度（> 99％）和高的摩尔活度（> 37 GBqμmol-1）。[11 C] GNE-1023对LRRK2的出色的体外结合特异性已通过放射自
• Jacobson, G. B.; Gustavsson, S. A.; Markides, K. E., Journal of labelled compounds and radiopharmaceuticals, 1997, vol. 40, p. 793 - 795
  作者：Jacobson, G. B.、Gustavsson, S. A.、Markides, K. E.、Langstroem, B.

  DOI：——

  日期：——
• CROUZEL, C., SYNTH. AND APPL. ISOTOPICALLY LABELLED COMPOUNDS, 1988: PROC. 3RD INT. SY+
  作者：CROUZEL, C.

  DOI：——

  日期：——
• AMANO RYOHEI; CROUZEL CHR., APPL. RADIAT. AND ISOTOP., 37,(1986) N 6, 541-543
  作者：AMANO RYOHEI、 CROUZEL CHR.

  DOI：——

  日期：——