(2S,4R)-4-methyl glutamic acid dimethyl ester | 441311-24-6

• 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: (2S,4R)-4-methyl glutamic acid dimethyl ester
• 英文别名: dimethyl (2S,4R)-2-amino-4-methylpentanedioate
• CAS: 441311-24-6
• 化学式: C₈H₁₅NO₄
• 分子量: 189.211
• InChiKey: HAYLWMJZMLTECL-RITPCOANSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  78.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Esters of alkycarboxy amino acids as prodrugs of modulators of the kainate receptor
  申请人：Annovis, Inc.

  公开号：US20020115721A1

  公开（公告）日：2002-08-22

  Disclosed are prodrug compounds of a class of alkyl carboxy amino acid analogs of glutamic acid that act as specific regulators of the kainate EAA receptor cation channel. These compounds are useful for treating neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders associated with excessive or insufficient activation of the kainate subtype of the ionotropic EAA receptors; treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainate receptor; alleviating pain and improving and enhancing memory, learning, and associated mental processes.

  本发明涉及一类丙基羧基氨基酸类谷氨酸类似物的前药化合物，它们作为特异性调节kainate EAA受体阳离子通道的调节剂。这些化合物可用于治疗与离子型EAA受体kainate亚型过度或不足激活相关的神经、神经心理、神经精神、神经退行性、神经精神药理学和功能障碍；治疗与kainate受体去活化、亚最佳激活或过度激活相关的认知障碍；缓解疼痛并改善和增强记忆、学习和相关的心理过程。
• Screen for glutamate reuptake inhibitors, stimulators, and modulators
  申请人：——

  公开号：US20020115688A1

  公开（公告）日：2002-08-22

  Disclosed is a method for identifying compounds that bind to or modulate a glutamate transporter. The disclosed method is useful for identifying compounds that can inhibit, stimulate, or modulate the activity of the glutamate transporter and thus affect glutamate reuptake. The method is a screening technique where compounds known to bind to glutamate receptors (for example, glutamate receptor ligands, including many agonists, and antagonists) are bound to a glutamate transporter and compounds are screened to identify those that can alter the binding of the glutamate receptor-binding compounds. Compounds shown to alter the binding of the receptor compounds from glutamate transporters in the disclosed assay can have a variety of effects on glutamate transporter activity including activation or inhibition. These compounds are expected to affect or interfere with glutamate reuptake by the glutamate transporter and thus can be used to modulate, stimulate, or inhibit glutamate reuptake. Such compounds are useful to treat various neurological diseases and conditions involving glutamate transporter and glutamate receptor activation. One of the compounds is (2S,4R)-4-methylglutamate or [ 3 H]-(2S,4R)-4-methylglutamate. For example, excess extracellular glutamate is a cause of excessive activation of glutamate receptors. Stimulating glutamate reuptake by glutamate transporters can ameliorate excessive activation of glutamate receptors by reducing the extracellular glutamate concentration. Prodrug forms of transporter compounds are preferred for use as drugs.

  本文揭示了一种识别结合或调节谷氨酸转运体的化合物的方法。揭示的方法用于识别可以抑制、刺激或调节谷氨酸转运体活性的化合物，从而影响谷氨酸的再摄取。该方法是一种筛选技术，其中已知与谷氨酸受体结合的化合物（例如，谷氨酸受体配体，包括许多激动剂和拮抗剂）与谷氨酸转运体结合，并筛选化合物以识别可以改变谷氨酸受体结合化合物的结合的化合物。在揭示的测定中，被证明可以改变受体化合物从谷氨酸转运体中结合的化合物可以对谷氨酸转运体活性产生各种效应，包括激活或抑制。这些化合物预计会影响或干扰谷氨酸转运体的谷氨酸再摄取，从而可以用于调节、刺激或抑制谷氨酸再摄取。这些化合物对于治疗涉及谷氨酸转运体和谷氨酸受体激活的各种神经疾病和病症非常有用。其中一种化合物是（2S，4R）-4-甲基谷氨酸或[3H] -（2S，4R）-4-甲基谷氨酸。例如，过多的细胞外谷氨酸是谷氨酸受体过度激活的原因。通过刺激谷氨酸转运体的谷氨酸再摄取，可以通过降低细胞外谷氨酸浓度来缓解谷氨酸受体的过度激活。药物使用时，转运体化合物的前药形式更受欢迎。
• Methods for modulation, stimulation, and inhibition of glutamate reuptake
  申请人：Annovis. Inc.

  公开号：US20020188022A1

  公开（公告）日：2002-12-12

  Disclosed is a method for inhibiting, stimulating, modulating, or regulating glutamate reuptake. The method makes use of compounds that are ligands of glutamate receptors, including many agonists, or antagonists of glutamate receptors. It has been discovered that such compounds can bind to or modulate glutamate transporters and affect extracellular glutamate levels by affecting transporter activity. The disclosed compounds can have a variety of effects on glutamate transporter activity including activation or inhibition. Such compounds are useful to treat various neurological diseases and conditions involving glutamate transporter and glutamate receptor activation. For example, excess extracellular glutamate is a cause of excessive activation of glutamate receptors. Stimulating glutamate reuptake by glutamate transporters can ameliorate excessive activation of glutamate receptors by reducing the extracellular glutamate concentration. Prodrug forms of transporter compounds can be used as drugs.

  本发明公开了一种抑制、刺激、调节或调节谷氨酸再摄取的方法。该方法利用作为谷氨酸受体配体的化合物，包括谷氨酸受体的许多激动剂或拮抗剂。研究发现，这些化合物可以与谷氨酸转运体结合或调节谷氨酸转运体，并通过影响转运体的活性来影响细胞外谷氨酸的水平。所公开的化合物可对谷氨酸转运体的活性产生多种影响，包括激活或抑制。此类化合物可用于治疗涉及谷氨酸转运体和谷氨酸受体激活的各种神经系统疾病和病症。例如，细胞外谷氨酸过多是谷氨酸受体过度激活的一个原因。通过谷氨酸转运体刺激谷氨酸的再摄取，可以降低细胞外谷氨酸的浓度，从而改善谷氨酸受体的过度激活。转运体化合物的原药形式可用作药物。
• SCREEN FOR GLUTAMATE REUPTAKE INHIBITORS, STIMULATORS, AND MODULATORS
  申请人：Annovis, Inc.

  公开号：EP1314041A2

  公开（公告）日：2003-05-28
• METHOD FOR MODULATION, STIMULATION, AND INHIBITION OF GLUTAMATE REUPTAKE
  申请人：Annovis, Inc.

  公开号：EP1365758A2

  公开（公告）日：2003-12-03