CAS: 32795-44-1; N-Acetylprocainamide

该化合物是一种化学化合物,主要用于治疗心律不全,主要用于治疗心律不全,是一种抗心律的化学剂,是丙烯酸的衍生物,其特点是乙酰基组能够加强其药理特性,其特点是能够堵塞钠管,稳定心细胞膜,有助于恢复正常的心脏节奏.N-Acetylprocainamide通常在临床环境中施用,以其中度功效和副作用为名,其中可能包括胃肠紊乱和对血细胞数的潜在影响.该化合物在水中溶解,呈现出中度分子重量,适于静脉管管理,其化学结构包括芳香环,氨化功能组和液态链,有助于其生物活动.与许多药物一样,对剂量和病人反应的仔细监测对于在尽量减少不利影响的同时优化治疗结果至关重要.

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CAS号201230-82-2 carbon monoxide | CAS号103-88-8 4'-溴乙酰苯胺 | CAS号100-36-7 N,N-二乙基乙二胺 | CAS号122-85-0 对乙酰氨基苯甲醛 | CAS号614-39-1 盐酸普鲁卡因胺 | CAS号75-36-5 乙酰氯

合成工艺路线路线简述

    📜N,N-二乙基乙二胺置于叔丁基过氧化氢,N-氯代丁二酰亚胺,Copper(Ll) Sulfate Pentahydrate体系中,化学反应 3.0H,反应生成 N-乙酰普鲁卡因胺
    参考文献:Copper-Catalyzed One-Pot Oxidative Amidation Of Alcohol To Amide Via C-h Activation
    标题:Copper-Catalyzed One-Pot Oxidative Amidation Of Alcohol To Amide Via C-h Activation
    摘要:铜催化的一锅法氧化酰胺化反应,使用从多种类型的一级和二级胺现场制备的n-氯胺与脂肪族和芳香族醇反应,在温和条件下形成酰胺.
    DOI:10.1039/c6Ra20732D

    海关参考信息

    专利信息


    专利号:US-4795828-A
    优先权日:1983-01-03
    标题 :Functionalized intermediate for the synthesis of alpha-functionalized derivatives and labeled conjugates of procaimamide and NAPA
    发明人:BUCKLER ROBERT T; WARD FREDERICK E
    权利人:MILES INC
    摘要:Procainamide and N-acetylprocainamide (NAPA) immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining the respective drugs. The immunogens comprise the drugs coupled at the alpha -position of the amide side chain to an immunogenic carrier material. The labeled conjugates and synthetic intermediates similarly are alpha -position derivatives of the drugs or precursors thereof. The antibodies and labeled conjugates are particularly useful in homogeneous nonradioisotopic immunoassays for measuring the respective drugs in biological fluids such as serum.

    专利号:US-5525474-A
    优先权日:1994-01-31
    标 题 :Piperidine analogs and conjugates of procainamide and NAPA
    发明人:SIGLER GERALD F; WALTER CHARLES F; GLANCY TODD; HUBER ERASMUS; KLEIN FRANK E
    权利人:BOEHRINGER MANNHEIM CORP
    摘要:Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: wherein: X=hydrogen or acetyl; n=1 to p where p=MW of Z/1000; Z=a poly(amino acid) or polysaccharide; and R3=a bond or aving 2 to 10 carbon atoms. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.

    专利号:US-5439798-A
    优先权日:1993-12-17
    标 题:Maleimide adduct conjugates of procainamide and NAPA
    发明人:SIGLER GERALD F; WALTER CHARLES F; DURANT CHARLES E; GLANCY TODD; KLEIN FRANK E; DORN ALLAN R
    权利人:BOEHRINGER MANNHEIM CORP
    摘要:Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: +TR wherein: X=hydrogen or acetyl; R1=an alkyl group having 1 to 3 carbon atoms; m=an integer from 2 to 10; R2=an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms; Z=a poly(amino acid); and n=1 to p where p=MW of Z/1000. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.

    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:US-6469055-B2
    优先权日:1996-09-05
    标题 :Compositions 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 , or forskolin is inhibited by immunosuppressants, immunophilin ligands, 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:US-5362625-A
    优先权日:1991-05-15
    标 题:Methods and compositions for enzyme complementation assays using the omega region of β-galactosidase
    发明人:KREVOLIN MARK; KATES DAVID
    权利人:MICROGENICS CORP
    摘要:The use of omega-acceptor and omega-donor polypeptides (comprising about two-thirds and one-third of the beta -galactosidase molecule amino and carboxyl termini, respectively), prepared by recombinant DNA techniques, DNA synthesis, or chemical polypeptide synthesis techniques, which are capable of interacting to form an active enzyme complex having catalytic activity characteristic of beta -galactosidase, is described along with improved methods and novel compositions for enzyme complementation assays for qualitative and quantitative determination of a suspected analyte in a sample.

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    主要参考文献


    1: Harron DW, Brogden RN. Acecainide (N-acetylprocainamide). A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in cardiac arrhythmias. Drugs. 1990 May;39(5):720-40. Review. Epub 2012 Aug 30. Review. Chinese. German.

    合成参考文献


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    参考文献:10.2165/00003495-200868050-00004
    摘要:Dopp AL, Miller JM, Tisdale JE. Effect of drugs on defibrillation capacity. Drugs. 2008;68(5):607–30. doi: 10.2165/00003495-200868050-00004.
    参考文献:10.2165/00003088-199223020-00003
    摘要:Sue YJ, Shannon M. Pharmacokinetics of drugs in overdose. Clin Pharmacokinet. 1992 Aug;23(2):93–105. doi: 10.2165/00003088-199223020-00003.
    参考文献:10.2165/00003495-199346060-00004
    摘要:Wormsley KG. Safety profile of ranitidine. A review. Drugs. 1993 Dec;46(6):976–85. doi: 10.2165/00003495-199346060-00004.
    参考文献:10.2165/00003495-199447010-00004
    摘要:Napolitano C, Priori SG, Schwartz PJ. Torsade de pointes. Mechanisms and management. Drugs. 1994 Jan;47(1):51–65. doi: 10.2165/00003495-199447010-00004.
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