CAS: 54527-84-3; 3-(2-(Benzyl(Methyl)Amino)Ethyl) 5-Methyl 2,6-Dimethyl-4-(3-Nitrophenyl)-1,4-Dihydropyridine-3,5-Dicarboxylate Hydrochloride

该化合物是二氢类的钙管阻塞器,主要用于抗血压和抗黄素性能,有选择性地抑制通过血管光滑肌肉细胞膜的钙离子流入,导致周边血管血管变异,减少系统血管抗药性.盐的形态会增加溶解性和生物利用率,使其适合口服和静脉注射.关键优势包括它的迅速行动,脑动脉和冠状动脉的优先放大以及最小的负非热效应,使其在急性高血压紧急情况和慢性高血压管理中特别有用.其可预测的药效动力学和特征化安全剖面图进一步支持其临床用途.

结构式图片

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ECHA物质C&L通报REACH预注册

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CAS号54527-65-0 2-(苄基甲基氨基)乙基乙酰乙酸酯 | CAS号99-61-6 间硝基苯甲醛 | CAS号14205-39-1 3-氨基巴豆酸甲酯 | CAS号39562-17-9 3-硝基苯叉基乙酰乙酸乙酯 | CAS号54527-73-0 2-(N-甲基苄基氨基)乙基 ... | CAS号103785-47-3 methanesulfonyl... | CAS号103-67-3 N-甲基苄胺 | CAS号85677-95-8 2-hydroxyethyl ... | CAS号101-98-4 N-甲基-N-羟乙基苄胺

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    专利信息


    专利号:US-6187756-B1
    优先权日:1996-09-05
    标 题 :Composition and methods for treatment of neurological disorders and neurodegenerative diseases
    发明人:LEE ROBERT K K; WURTMAN RICHARD J
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

    专利号:WO-2007043621-A1
    优先权日:2005-10-13
    标 题:Total synthesis of pladienolide b and pladienolide d

    专利号:US-2013030282-A1
    优先权日:2011-07-18
    标题:Synthesis and characterization of near ir fluorescent magnetic and non-magnetic albumin nanoparticles for biomedical applications
    发明人:MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL
    权利人:UNIV BAR ILAN; MARGEL SHLOMO; COHEN SARIT; SALKMON ENAV COREM; PELLACH MICHAL
    摘要:The present invention discloses Near Infrared (NIR) fluorescent albumin nanoparticles having a structure selected from a core structure or a core-shell structure. Also disclosed are a process of preparing these NIR fluorescent albumin nanoparticles, and a method of in vivo detection of pathologies, in particular cancer pathology, by using administering these NIR fluorescent albumin nanoparticles to a patient.

    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 %.

    专利号:US-6884842-B2
    优先权日:1997-10-14
    标题:Molecular compounds having complementary surfaces to targets
    发明人:SOANE DAVID S; BARRY STEPHEN E; GOODWIN ANDREW; OFFORD DAVID A; PERROTT MICHAEL G
    权利人:ALNIS BIOSCIENCES INC
    摘要:Synthetic polymer complements (SPCs) are provided, as well as methods for their synthesis and use. The SPCs may have surfaces that include functional groups that are complementary to surface sites of targets such as nanostructures or macromolecular targets, and may be capable of specifically interacting with such targets. The positions of the functional groups in one embodiment are stabilized by a polymer network. The SPCs are formed by contacting the target with a set of monomers which self-assemble on the target, and then are polymerized into a network to form the synthetic polymer complement. At least a portion of the surface of the resulting SPC thus may include an imprint of the target. The complex of the SPC and the target may be the desired product. Alternatively, the target is released, for example, by controllably expanding and contracting the crosslinked network. The SPC is isolated and used in many applications.
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    主要参考文献


    1: McKeever RG, Hamilton RJ. Calcium Channel Blockers. 2018 Feb 21. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2018 Jan-. Available from http://www.ncbi.nlm.nih.gov/books/NBK482473/ doi: 10.1016/j.etap.2018.02.005. [Epub ahead of print] doi: 10.1186/s40981-017-0094-5. Epub 2017 May 8.
    4: Zhang P, Weeranoppanant N, Thomas DA, Tahara K, Stelzer T, Russell MG, O'Mahony M, Myerson AS, Lin H, Kelly LP, Jensen KF, Jamison TF, Dai C, Cui Y, Briggs N, Beingessner RL, Adamo A. Advanced Continuous Flow Platform for On-Demand Pharmaceutical Manufacturing. Chemistry. 2018 Feb 21;24(11):2776-2784. doi: 10.1002/chem.201706004. Epub 2018 Jan 31. doi: 10.1016/j.clinthera.2017.12.007. Epub 2017 Dec 28. doi: 10.3892/mmr.2017.8233. Epub 2017 Dec 8.
    8: Soomherun N, Kreua-Ongarjnukool N, Chumnanvej S, Thumsing S. Encapsulation of Nicardipine Hydrochloride and Release from Biodegradable Poly(D,L-lactic-co-glycolic acid) Microparticles by Double Emulsion Process: Effect of Emulsion Stability and Different Parameters on Drug Entrapment. Int J Biomater. 2017;2017:1743765. doi: 10.1155/2017/1743765. Epub 2017 Nov 8.

    合成参考文献


    摘要:United States Patent Document., #4565823
    摘要:Arzneimittel-Forschung. Drug Research., 26(2172), 1976 []
    参考文献:10.1007/bf03190011
    摘要:Mrhar A, Bogataj M, Grabnar I, Karba R. Formulation of controlled release microspheres containing nicardipine: the role of pharmacokinetic modeling and computer simulation. European Journal of Drug Metabolism and Pharmacokinetics. 1999 Mar;24(1):55–61. doi: 10.1007/bf03190011.
    参考文献:10.1007/s12028-014-9973-z
    摘要:Tagami T, Kuwamoto K, Watanabe A, Unemoto K, Yokobori S, Matsumoto G, Igarashi Y, Yokota H; SAH PiCCO Study Group. Effect of triple-h prophylaxis on global end-diastolic volume and clinical outcomes in patients with aneurysmal subarachnoid hemorrhage. Neurocrit Care. 2014 Dec;21(3):462–9. doi: 10.1007/s12028-014-9973-z.
    参考文献:10.1186/s13256-021-02983-3
    摘要:Yoshimoto M, Takeda N, Yoshimoto T, Matsumoto S. Hypertensive cerebral hemorrhage with undetectable plasma vascular endothelial growth factor levels in a patient receiving intravitreal injection of aflibercept for bilateral diabetic macular edema: a case report. Journal of Medical Case Reports. 2021 Jul 27;15(1):403. doi: 10.1186/s13256-021-02983-3.
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