(E)-N-(benzyl)cinnamamidine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (E)-N-(benzyl)cinnamamidine
• 英文别名: (E)-N-Benzyl-3-phenyl-acrylamidine；(E)-N'-benzyl-3-phenylprop-2-enimidamide
• 化学式: C₁₆H₁₆N₂
• 分子量: 236.316
• InChiKey: HEXBAJSBFNYKJO-VAWYXSNFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  38.4
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• Amidine derivatives as selective antagonists of ndma receptors
  申请人：——

  公开号：US20030119871A1

  公开（公告）日：2003-06-26

  A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, in particular neuropathic pain and headache, specifically migraine, whils displaying fewer ataxic and related side-effects associated with other classes of NMDA receptor antagonists.

  一类styryl amidine衍生物，它们是hum NMDA受体的拮抗剂，对含有NR2B亚基的受体具有选择性，在治疗和/或预防神经系统和神经退行性疾病方面具有活性，特别是神经病性疼痛和头痛，特别是偏头痛，同时显示出更少的共济失调和其他NMDA受体拮抗剂相关的副作用。
• Conjugates of glutamate and NMDA receptor channel blockers without excito-toxic effects
  申请人：Tschollar,, Werner

  公开号：EP1903028A1

  公开（公告）日：2008-03-26

  Methods for delivering therapeutic amounts of glutamate to the CNS while simultaneously protecting against its excito-toxic effects are provided. By administering a blood-brain barrier-permeable Conjugate Compound, which comprises glutamate linked to an N-methyl-D-aspartate receptor antagonist, glutamate is released within the CNS for beneficial effect without causing excito-toxicity. Examples of such Conjugate Compounds are provided and their cognition-enhancing effect without engendering excito-toxicity in both normal and cognition-impaired animals is demonstrated.

  本研究提供了向中枢神经系统输送治疗量谷氨酸的方法，同时防止其兴奋毒性效应。通过施用可透过血脑屏障的共轭化合物（其中包括与 N-甲基-D-天冬氨酸受体拮抗剂相连的谷氨酸），谷氨酸可在中枢神经系统内释放，从而产生有益效果，同时不会导致兴奋毒性。本文提供了此类共轭化合物的实例，并证明了它们在正常动物和认知障碍动物中的认知增强效果，而不会产生兴奋毒性。
• AMIDINE DERIVATIVES AS SELECTIVE ANTAGONISTS OF NMDA RECEPTORS
  申请人：MERCK SHARP & DOHME LTD.

  公开号：EP1296940A1

  公开（公告）日：2003-04-02
• Prevention and treatment of cognitive impairment using (R)-(-)-5-methyl-1-nicotynoyl-2-pyrazoline (MNP) and analogs
  申请人：Gallagher Michela

  公开号：US20060014801A1

  公开（公告）日：2006-01-19

  The invention provides methods for improving cognitive function in a subject by administering (R)-(−)-5-methyl-1-nicotinoyl-2-pyrazoline (MNP) or an analog to a subject in need of such treatment. The invention is useful for treatment of cognitive impairment such as mild cognitive impairment (MCI) as well as other conditions.
• Subunit Selective NMDA Receptor Antagonists For The Treatment Of Neurological Conditions
  申请人：Traynelis Stephen F.

  公开号：US20110319416A1

  公开（公告）日：2011-12-29

  Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.