CAS: 119257-34-0; N-Propyl-N-(Pyridin-4-yl)-1H-Indol-1-Amine

该化合物是一种属于管道衍生物类别的化学化合物,主要因其潜在的药理特性而得到承认,特别是选择性的血清素和新肾上腺素再摄入抑制剂(SNRI),该化合物因其对认知功能和情绪调控的影响而受到调查,从而在治疗抑郁和焦虑等条件下引起了兴趣.Besipirdine展示了各种...

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    N-(吡啶-4-基)-1H-吲哚-1-胺 P 86-7480 119257-33-9

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      📜1H-吲哚-1-胺置于sodium Hydride体系中,用 异丙醇 用作溶剂,化学反应 4.0H,反应生成贝西吡啶
      参考文献:Synthesis And Structure−activity Relationships Of N-Propyl-N-(4-Pyridinyl)-1H-Indol-1-Amine (Besipirdine) And Related Analogs As Potential Therapeutic Agents For Alzheimer'S Disease
      标题:Synthesis And Structure−activity Relationships Of N-Propyl-N-(4-Pyridinyl)-1H-Indol-1-Amine (Besipirdine) And Related Analogs As Potential Therapeutic Agents For Alzheimer'S Disease
      摘要:A Series Of Novel N-(4-Pyridinyl)-1H-Indol-1-Amines And Other Heteroaryl Analogs Was Synthesized And Evaluated In Tests To Determine Potential Utility For The Treatment Of Alzheimer'S Disease. From These Compounds,N-Propyl-N-(4-Pyridinyl)-1H-Indol-1-Amine (Besipirdine,4C) Was Selected For Clinical Development Based On In-Depth Biological Evaluation. In Addition To Cholinomimetic Properties Based Initially On In Vitro Inhibition Of [h-3]Quinuclidinyl Benzilate Binding,In. Vivo Reversal Of Scopolamine-Induced Behavioral Deficits,And Subsequently On Other Results,4C Also Displayed Enhancement Of Adrenergic Mechanisms As Evidenced In Vitro By Inhibition Of [h-3]Clonidine Binding And Synaptosomal Biogenic Amine Uptake,And In Vivo By Reversal Of Tetrabenazine-Induced Ptosis. The Synthesis,Structure-Activity Relationships For This Series,And The Biological Profile Of 4C Are Reported.
      Doi:10.1021/jm9506433

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      专利信息


      专利号:US-6512125-B1
      优先权日:1994-05-13
      标 题 :Preparation of 1H-indol-1-amines
      发明人:LEE THOMAS B; GOEHRING KEITH E
      权利人:AVENTIS PHARMA INC
      摘要:The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.

      专利号:US-2014315720-A1
      优先权日:2012-10-24
      标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
      发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
      权利人:CELANESE ACETATE LLC
      摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

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      主要参考文献


      1: Pérez-Martínez FC, Vela-Navarrete R, Virseda J, Ocaña AV, Lluel P, Rekik M, Bienaymé H, Ferté J, Attali P, Palea S. Halothane-anesthetized rabbit: a new experimental model to test the effects of besipirdine and duloxetine on lower urinary tract function. Urol Int. 2011;86(2):210-9. doi: 10.1159/000321226.
      5: Huff FJ. Preliminary evaluation of besipirdine for the treatment of Alzheimer's disease. Besipirdine Study Group. Ann N Y Acad Sci. 1996 Jan 17;777:410-4. Erratum in: Drug Metab Dispos 1997 Aug;25(8):1016.

      合成参考文献


      参考文献:10.1016/0361-9230(96)00163-3|10.1016/s0361-9230(96)00163-3
      摘要:Woods-Kettleberger AT, Smith CP, Corbett R, Szewczak MR, Roehr JE, Bores GM, Klein JT, Kongsamut S. Besipirdine (HP 749) reduces schedule-induced polydipsia in rats. Brain Research Bulletin. 1996;41(2):125–30. doi: 10.1016/0361-9230(96)00163-3.
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