2-chloro-10-(3-morpholino-propyl)-phenothiazine | 95276-81-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: 2-chloro-10-(3-morpholino-propyl)-phenothiazine
• 英文别名: 2-Chlor-10-(3-morpholino-propyl)-phenothiazin；4-[3-(2-Chlorophenothiazin-10-yl)propyl]morpholine
• CAS: 95276-81-6
• 化学式: C₁₉H₂₁ClN₂OS
• 分子量: 360.908
• InChiKey: VAOAZCXRDRRBKE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  41
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氯吩噻嗪 在 苄基三甲基氢氧化铵 、 镍 、 苯 作用下， 49.0~61.0 ℃ 、5.49 MPa 条件下， 生成 2-chloro-10-(3-morpholino-propyl)-phenothiazine
  参考文献：
  名称：

  Fujii, Yakugaku Zasshi/Journal of the Pharmaceutical Society of Japan, 1956, vol. 76, p. 644,647, 648

  摘要：

  DOI：

文献信息

• Phenothiazine antipsychotics exhibit dual properties in pseudo-allergic reactions: Activating MRGPRX2 and inhibiting the H1 receptor
  作者：Yajing Hou、Delu Che、Di Wei、Cheng Wang、Yitong Xie、Kaining Zhang、Jiao Cao、Jia Fu、Nan Zhou、Huaizhen He

  DOI：10.1016/j.molimm.2019.04.008

  日期：2019.7

  confirmed a potential antagonist effect of these drugs on the H1R. The molecular docking and activity experiments indicated that the N-methyl substitution on the side chain of these drugs played a significant role in activating MRGPRX2, while the phenothiazine tricyclic ring was associated with the inhibiting effect on the H1R. Therefore, due to their dual properties of increasing histamine levels without

  吩噻嗪是一类具有相同三环结构的抗精神病药，已广泛用于临床。然而，定期报告了这些药物的不良反应，在某些情况下还指出了皮肤过敏反应。然而，尚未描述这些药物引起的过敏反应的潜在机制。在本研究中，我们发现吩噻嗪类抗精神病药通过体外与Mas相关的G蛋白偶联受体成员X2（MRGPRX2）增强钙动员并激活肥大细胞释放β-己糖胺酶，组胺和肿瘤坏死因子-α 。此外，它们还通过以下途径诱导血清中的组胺释放C57BL / 6小鼠中的Mrgprb2，无埃文斯蓝色外渗或足爪肿胀。进一步的实验表明，这些药物与组胺H 1受体（H1R）具有良好的相互作用，并显示出对H 1 R-HEK293细胞的抗钙动员作用，这证实了这些药物对H 1 R的潜在拮抗作用。对接和活性实验表明，这些药物侧链上的N-甲基取代在激活MRGPRX2中起着重要作用，而吩噻嗪三环与H 1的抑制作用有关。R.因此，由于其具有增加组胺水平的双重特性，而没有明
• SMALL MOLECULE COMPOUNDS FOR STEM CELL DIFFERENTIATION
  申请人：Mercola Mark

  公开号：US20100159596A1

  公开（公告）日：2010-06-24

  Methods and small molecule compounds for stem cell differentiation are provided. One example of a class of compounds that may be used is represented by the compound having the structure IA or IB in the form of free base or a pharmaceutically acceptable salt, hydrate, solvate or N-oxide thereof: R 1 is independently hydrogen or (C 1 -C 6 )alkyl; R 2 is independently hydrogen, (C 1 -C 6 )alkyl, aryl, or heteroaryl; R 2′ is independently hydrogen, (C 1 -C 6 )alkyl, CF 3 or C 2 F 5 ; R 3 is independently (C 1 -C 6 )alkyl, aryl, 2-tetrahydrofurylmethyl, an aliphatic tertiary amine, or 4-methoxybenzyl; or R 2 and R 3 may be joined together to form a 5 or 6 member ring lactone; R 4 is independently hydrogen, (C 1 -C 6 )alkyl, a 2- or 4-R 5 -substituted aromatic ring selected from a 4-R 5 -phenyl or a 2-R 5 -5-pyridyl, aryl, heteroaryl, aliphatic tertiary amine or halogen; and R 5 , R 5′ , R 6 , R 6′ , R 7 , R 7′ , are each independently hydrogen, (C 1 -C 6 )alkyl, aryl, optionally substituted phenyl, heteroaryl, a heterocyclic ring, an aliphatic tertiary amine, or halogen.

  提供干细胞分化的方法和小分子化合物。可以使用的一类化合物的一个示例由结构IA或IB表示，以自由碱基或其药学上可接受的盐，水合物，溶剂或N-氧化物的形式存在：R1独立地是氢或（C1-C6）烷基; R2独立地是氢，（C1-C6）烷基，芳基或杂环芳基; R2'独立地是氢，（C1-C6）烷基，CF3或C2F5; R3独立地是（C1-C6）烷基，芳基，2-四氢呋喃甲基，脂肪族三级胺或4-甲氧基苄基; 或者R2和R3可以结合形成5或6元环内酯; R4独立地是氢，（C1-C6）烷基，2-或4-R5-取代的芳环，选自4-R5-苯基或2-R5-5-吡啶基，芳基，杂环芳基，脂肪族三级胺或卤素; R5，R5'，R6，R6'，R7，R7'独立地是氢，（C1-C6）烷基，芳基，可选取代的苯基，杂环芳基，杂环环，脂肪族三级胺或卤素。
• Calmodulin inhibitors, Chk2 inhibitors and RSK inhibitors for the treatment of ribosomal disorders and ribosomapathies
  申请人：THE CHILDREN'S MEDICAL CENTER CORPORATION

  公开号：US10980808B2

  公开（公告）日：2021-04-20

  The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.

  本发明涉及治疗核糖体紊乱和核糖体病（如钻石黑凡贫血症（DBA））的方法、组合物和试剂盒。在一些实施方案中，本发明涉及使用新型化合物，即 RSK（p90S6K）的抑制剂；p70S6K 的抑制剂；和 rps6 的抑制剂，来治疗核糖体紊乱和核糖体病。在某些实施方案中，本发明涉及使用特异性 Chk2 抑制剂和特异性吩噻嗪衍生物治疗核糖体紊乱和核糖体病，如 DBA。
• CALMODULIN INHIBITORS, CHK2 INHIBITORS AND RSK INHIBITORS FOR THE TREATMENT OF RIBOSOMAL DISORDERS AND RIBOSOMAPATHIES
  申请人：THE CHILDREN'S MEDICAL CENTER CORPORATION

  公开号：US20190314374A1

  公开（公告）日：2019-10-17

  The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.
• US9012217B2
  申请人：——

  公开号：US9012217B2

  公开（公告）日：2015-04-21