N-methyl-D-aspartate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-methyl-D-aspartate
• 英文别名: NMDA；(2R)-2-(methylamino)butanedioate
• 化学式: C₅H₇NO₄
• 分子量: 145.115
• InChiKey: HOKKHZGPKSLGJE-GSVOUGTGSA-L

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  92.3
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  替诺环定 、 N-methyl-D-aspartate 、 、 生成 苯环利定
  参考文献：
  名称：

  Drug system

  摘要：

  本发明涉及一种用于治疗和缓解癫痫症状，作为抗惊厥剂，并用于预防或缓解因中风而导致的脑损伤的药物系统。该药物系统包括作为活性成分的化合物，例如MK-801、苯环利定或苯并环己基哌啶（TCP），以这样的方式给予，使其遇到并结合到N-甲基-D-天门冬氨酸（NMDA）受体通道。在谷氨酸或甘氨酸或类似作用的氨基酸的存在下，该药物可以有效地被谷氨酸拮抗剂（例如AP-5）锁定在受体通道中。

  公开号：

  US04994446A1
• 作为产物：
  描述：

  D-aspartate 、 S-腺苷-L-蛋氨酸 在 D-aspartate N-methyltransferase from the pancreas of mouse 作用下， 以 aq. buffer 为溶剂， 反应 0.33h， 以100%的产率得到N-methyl-D-aspartate
  参考文献：
  名称：

  d-Aspartate N-methyltransferase catalyzes biosynthesis of N-methyl-d-aspartate (NMDA), a well-known selective agonist of the NMDA receptor, in mice

  摘要：

  N-Methyl-D-aspartate (NMDA), which is a selective agonist for the NMDA receptor, has recently been shown to be present in various biological tissues. In mammals, the activity of D-aspartate N-methyltransferase (DDNMT), which produces NMDA from D-aspartate, has been detected only in homogenates prepared from rat tissues. Moreover, the enzymatic properties of DDNMT have been poorly studied and its molecular entity has not yet been identified. In this report, we show for the first time that the activity of DDNMT is present in mouse tissues and succeed in obtaining a partially purified enzyme preparation from a mouse tissue homogenate with a purification fold of 1900 or more, and have characterized the enzymatic activity of this preparation. The results indicate that DDNMT, which is highly specific for D-aspartate and is S-adenosyl-L-methionine-dependent, is a novel enzyme that clearly differs from the known methylamine-glutamate N-methyltransferase (EC 2.1.1.21) and glycine N-methyltransferase (EC 2.1.1.20).

  DOI：

  10.1016/j.bbapap.2020.140527

文献信息

• o-Phosphono(alkyl)-N-sulfonyl-phenyl-alanine derivatives useful as
  申请人：G. D. Searle & Co.

  公开号：US05177240A1

  公开（公告）日：1993-01-05

  A class of phosphono-hydroisoquinoline compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of Formula I: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, wherein each of Z.sup.1 and Z.sup.2 is hydroxyl, wherein W is a single bond connecting the phosphorus atom with the aromatic ring and wherein the A ring is aromatic. Also disclosed are two classes of intermediate compounds having a fully unsaturated A ring, which intermediate compounds are useful in methods to make product compounds of Formula I.

  本文描述了一类磷酸羟基异喹啉化合物，用于治疗与缺氧或缺血相关的神经毒性损伤，通常是中风、心脏骤停或围产期窒息后的损伤。治疗包括单独或在组合物中给予磷酸羟基异喹啉化合物，其有效量作为拮抗剂抑制主要神经元兴奋性氨基酸受体位点的兴奋毒性作用。最感兴趣的化合物是公式I的化合物：##STR1## 其中R1至R4中的每一个都是氢基，Z1和Z2中的每一个都是羟基，W是将磷原子与芳香环连接的单键，A环是芳香的。此外，还披露了两类中间化合物，具有完全不饱和的A环，这些中间化合物在制备公式I的产物化合物的方法中很有用。