CAS: 35920-39-9; (2S,3S,4R,5R)-5-(6-Amino-9H-Purin-9-yl)-N-Ethyl-3,4-Dihydroxytetrahydrofuran-2-Carboxamide

该化合物是一种强能的腺受体激动剂,对所有腺受体亚型(A1, A2A, A2B, A3)具有高度亲近性. 它广泛用于药物学研究,以研究由于其非选择性活化特征而导致的腺受体信号路径. NECA表现出强大的血管和抗炎效应,因此对调查心血管和免疫系统调节很有价值.它的稳定性和生物利用率提高了其在体外和活性研究中的效用.作为一种研究工具,NECA协助揭示了腺受体的生理作用,促进了针对诸如化学,炎症和...

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号39491-53-7 5'-乙基羧酰胺基-2',3'... | CAS号19234-66-3 2′,3′-异亚丙基腺苷-5′-羧酸 | CAS号75-04-7 乙胺 | CAS号35803-57-7 ethyl adenosine... | CAS号362-75-4 2',3'-异丙叉腺苷 | CAS号3415-09-6 腺苷酸-5-羧酸 | CAS号41110-82-1 adenosine-5'-ca... | CAS号72209-27-9 (2S,3S,4R,5R)-N...

合成工艺路线路线简述

    📜2',3'-Isopropylideneadenosine-5'-Carboxylic Acid置于盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 4.0H,反应生成 5-N-乙基酰胺基腺苷
    参考文献:核苷和核苷酸.200. 5'-N-乙基羧酰胺基腺苷衍生物的再研究:P(3)嘌呤受体样蛋白的结构-活性关系.
    标题:核苷和核苷酸.200. 5'-N-乙基羧酰胺基腺苷衍生物的再研究:P(3)嘌呤受体样蛋白的结构-活性关系.
    摘要:Atp在兔胸主动脉中的非p(1)和非p(2)肌肉松弛作用最近归因于推定的p(3)嘌呤受体,该受体被腺苷或atp激活.由于此假定的p(3)嘌呤受体和新的[(3)h]-5'-N-乙基羧酰胺基腺苷(neca)结合蛋白从大鼠脑膜的生理作用,称为p(3)嘌呤受体样蛋白(p (3)lp),由于其配体特异性尚未完全阐明,我们需要特定的配体以获得有关受体的进一步信息.我们检查了各种5'-N-取代的羧酰胺基腺苷衍生物对p(3)lp的结构-活性关系(sar),并发现了5'-N-取代的羧酰胺基附近的疏水结合区.从直链烷基n-取代的衍生物,Nn-戊基衍生物10被发现是最有效的配体,其k(i)值为12 Nm.在一系列n-环烷基衍生物中,N-环己基衍生物27是最强的配体,其k(i)值为18 Nm.另一方面,具有支链烷基侧链和庞大的环烷基的n-取代基对p(3)lp没有任何有效的亲和力.因此,疏水口袋容纳大约10个碳原
    DOI:10.1021/jm000150K

    海关参考信息

    专利信息


    专利号:US-9018371-B2
    优先权日:2007-03-07
    标 题 :Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient
    发明人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH
    权利人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH; FM THERAPEUTICS CO LTD; US OF AMERICA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES THE OFFICE OF TECHNO
    摘要:Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A 3 adenosine receptors and act as A 3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.

    专利号:US-2024368164-A1
    优先权日:2021-04-28
    标 题 :Purine nucleosides, their intermediates, and methods of preparation thereof
    发明人:RAVI RAMA SURESH; JACOBSON KENNETH A; POE RUSSELL BIRCH
    权利人:ASTROCYLE PHARMACEUTICALS INC; US HEALTH
    摘要:The present invention provides purine nucleoside analog compounds and methods of use thereof for treatment of certain injuries, disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries. The present invention further provides methods of synthesizing such compounds, and intermediates useful in the synthesis of such compounds.

    专利号:US-2023286975-A1
    优先权日:2020-07-07
    标题:Improved method for the production of lysergic acid diethylamide (lsd) and novel derivatives thereof
    发明人:GRILL MATTHIAS
    权利人:COMPASS PATHFINDER LTD
    摘要:The present invention provides an improved method for the production of lysergic acid diethylamide (LSD) for GMP purposes. Furthermore, the present invention provides novel LSD derivatives of formula I as well as their synthesis and purification. Due to the affinity of the presented substances for the 5-HT 2A receptor, the invention may find application in numerous forms of therapy, such as against depression or drug addiction.

    专利号:US-2007105821-A1
    优先权日:2005-02-25
    标 题 :Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines

    专利号:WO-9636631-A1
    优先权日:1995-05-19
    标题:Multiply-substituted fullerenes and methods for their preparation and characterization
    发明人:MURPHY RANDALL B; WILSON STEPHEN R; LU QUING
    权利人:SPHERE BIOSYSTEMS INC
    摘要:The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the Cn fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.

    专利号:US-2023271983-A1
    优先权日:2020-07-29
    标题 :Functionalized isonitriles and products, preparation and uses thereof
    发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
    权利人:UNIV SANTIAGO COMPOSTELA
    摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    参考标题:Ring Opening Reactions: Synthesis Of Aicar Analogs As Potential Antimetabolite Agents
    作者:S. Costanzi,C. Lambertucci,F. R. Portino,R. Volpini,S. Vittori,G. Cristalli |发布日期:2005.4.1
    摘要:Adenosine, We Planned The Synthesis Of The Corresponding Derivatives Of The 5′-N-Ethylcarboxamidoadenosine (Neca). For This Purpose, We Designed The Synthesis Of 2-Mercapto-Neca To Be Pursued By Means Of An "Opening-Closure" Method. We Obtained The Open Aicar Analog; However, Ring Closure Efforts Failed To Give The Desired Compound. The Newly Synthesized Aicar Derivative Could Potentially Be Endowed With Antiviral

    合成参考文献


    摘要:Journal of Medicinal Chemistry., 23(313), 1980
    参考文献:10.1021/jm960376g
    摘要:Vittori S, Camaioni E, Di Francesco E, Volpini R, Monopoli A, Dionisotti S, Ongini E, Cristalli G. 2-Alkenyl and 2-Alkyl Derivatives of Adenosine and Adenosine-5‘-N-Ethyluronamide: Different Affinity and Selectivity of E- and Z-Diastereomers at A2A Adenosine Receptors. J. Med. Chem. 1996 Jan 01;39(21):4211–7. doi: 10.1021/jm960376g.
    参考文献:10.1021/jm001114o
    摘要:van Tilburg EW, van der Klein PAM, von Frijtag Drabbe Künzel J, de Groote M, Stannek C, Lorenzen A, IJzerman AP. 5‘-O-Alkyl Ethers of N,2-Substituted Adenosine Derivatives: Partial Agonists for the Adenosine A1 and A3 Receptors. J. Med. Chem. 2001 Jul 26;44(18):2966–75. doi: 10.1021/jm001114o.
    参考文献:10.1038/sj.bjp.0704245
    摘要:Esquisatto LCM, Costa SKP, Camargo EA, Ribela MTCP, Brain SD, Nucci GD, Antunes E. The plasma protein extravasation induced by adenosine and its analogues in the rat dorsal skin: evidence for the involvement of capsaicin sensitive primary afferent neurones and mast cells. British J Pharmacology. 2001 Sep;134(1):108–15. doi: 10.1038/sj.bjp.0704245.
    参考文献:10.1038/nature10136
    摘要:Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG. Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature. 2011 May 18;474(7352):521–5.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知