RF9 | 1053615-07-8

• 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: RF9
• 英文别名: 1-adamantanecarbonyl-Arg-Phe-NH2；N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]adamantane-2-carboxamide
• CAS: 1053615-07-8
• 化学式: C₂₆H₃₈N₆O₃
• 分子量: 482.626
• InChiKey: ZLSDDXOZWMSRNZ-BFLAJNRSSA-N

物化性质

• 密度：
  1.44±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  35
• 可旋转键数：
  11
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  166
• 氢给体数：
  5
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-金刚烷甲酸 、 Fmoc-L-苯丙氨酸 、 FMOC-L-精氨酸 在 1-羟基苯并三唑 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 、 N,N-二甲基甲酰胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 RF9
  参考文献：
  名称：

  Pressor and tachycardic responses to intrathecal administration of neuropeptide FF in anesthetized rats

  摘要：

  Neuropeptide FF (NPFF) belongs to a neuropeptide family including two precursors (pro-NPFFA and pro-NPFFB) and two receptors (NPFF1 and NPFF2). NPFF and NPFF receptor mRNAs have been reported to be highly expressed and localized in the rat and human spinal cord. In the present study, the i.t. action of NPFF system on blood pressure and heart rate were examined using NPFF and two related agonists, NPVF and dNPA, which exhibit highest selectivities for NPFF1 and NPFF2 receptors, respectively. In urethane-anesthetized rats, NPFF and related peptides (5-40 nmol, i.t.) produced significant pressor and tachycardic responses at the spinal cord level. These effects were dose-dependent and similar with respect to time-course for the three peptides. Furthermore, i.t, injection of RF9 (20 nmol), a selective NPFF antagonist, significantly antagonized the cardiovascular responses to 20 nmol NPFF and related peptides (i.t.). Moreover, pretreatment of the rats with alpha-adrenoceptor antagonist phentolamine (1 mg/kg, iv.) significantly reduced the pressor effects of NPFF. Nevertheless, pretreatment with muscarinic receptor and adrenoceptor antagonists (i.v.) could block the tachycardic effects induced by NPFF. Collectively, our results suggested that i.t. administration of NPFF and related peptides increased MAP and HR which were possibly mediated by the activation of both NPFF, and NPFF2 receptors in the rat spinal cord. In addition, our results showed that the muscarinic receptor and adrenoceptor participated in the tachycardic response to i.t. NPFF, while a-adrenoceptor played an important role in the regulation of pressor effect of NPFF. (C) 2009 Elsevier Inc. All rights reserved.

  DOI：

  10.1016/j.peptides.2009.11.003

文献信息

• COMPOSITIONS AND METHODS FOR MODULATING SLEEP AND WAKEFULNESS
  申请人：Chow Suk Hen

  公开号：US20150246140A1

  公开（公告）日：2015-09-03

  In some aspects, the invention relates to methods of treating conditions associated with sleep disorders, comprising administering an agent that modulates the activity of a neuropeptide receptor or a neuropeptide receptor ligand. In some aspects, the invention relates to methods of screening agents that modulate the activity of a neuropeptide receptor in an organism, optionally using cells or organisms comprising a genetic modification that affects a neuropeptide signaling pathway. In some aspects, the invention relates to methods of characterizing a condition associated with a sleep disorder comprising sequencing a nucleic acid encoding either a neuropeptide receptor or a neuropeptide receptor ligand and comparing the sequence with a reference sequence.
• [EN] COMPOSITIONS AND METHODS FOR MODULATING SLEEP AND WAKEFULENESS<br/>[FR] COMPOSITIONS ET PROCÉDÉS DESTINÉS À MODULER LE SOMMEIL ET L'ÉTAT DE VEILLE
  申请人：CALIFORNIA INST OF TECHN

  公开号：WO2015120446A1

  公开（公告）日：2015-08-13

  In some aspects, the invention relates to methods of treating conditions associated with sleep disorders, comprising administering an agent that modulates the activity of a neuropeptide receptor or a neuropeptide receptor ligand. In some aspects, the invention relates to methods of screening agents that modulate the activity of a neuropeptide receptor in an organism, optionally using ceils or organisms comprising a genetic modification that affects a neuropeptide signaling pathway. In some aspects, the invention relates to methods of characterizing a condition associated with a sleep disorder comprising sequencing a nucleic acid encoding either a neuropeptide receptor or a neuropeptide receptor ligand and comparing the sequence with a reference sequence.
• Pressor and tachycardic responses to intrathecal administration of neuropeptide FF in anesthetized rats
  作者：Quan Fang、Ning Li、Tian-nan Jiang、Qian Liu、Yu-lin Li、Rui Wang

  DOI：10.1016/j.peptides.2009.11.003

  日期：2010.4

  Neuropeptide FF (NPFF) belongs to a neuropeptide family including two precursors (pro-NPFFA and pro-NPFFB) and two receptors (NPFF1 and NPFF2). NPFF and NPFF receptor mRNAs have been reported to be highly expressed and localized in the rat and human spinal cord. In the present study, the i.t. action of NPFF system on blood pressure and heart rate were examined using NPFF and two related agonists, NPVF and dNPA, which exhibit highest selectivities for NPFF1 and NPFF2 receptors, respectively. In urethane-anesthetized rats, NPFF and related peptides (5-40 nmol, i.t.) produced significant pressor and tachycardic responses at the spinal cord level. These effects were dose-dependent and similar with respect to time-course for the three peptides. Furthermore, i.t, injection of RF9 (20 nmol), a selective NPFF antagonist, significantly antagonized the cardiovascular responses to 20 nmol NPFF and related peptides (i.t.). Moreover, pretreatment of the rats with alpha-adrenoceptor antagonist phentolamine (1 mg/kg, iv.) significantly reduced the pressor effects of NPFF. Nevertheless, pretreatment with muscarinic receptor and adrenoceptor antagonists (i.v.) could block the tachycardic effects induced by NPFF. Collectively, our results suggested that i.t. administration of NPFF and related peptides increased MAP and HR which were possibly mediated by the activation of both NPFF, and NPFF2 receptors in the rat spinal cord. In addition, our results showed that the muscarinic receptor and adrenoceptor participated in the tachycardic response to i.t. NPFF, while a-adrenoceptor played an important role in the regulation of pressor effect of NPFF. (C) 2009 Elsevier Inc. All rights reserved.