CAS: 88069-67-4; Pilsicainide

该化合物是一种化学化合物,被归类为抗心律剂,主要用于治疗某些类型的心律不全,属于钠管阻塞器,在心脏行动潜力的脱冰阶段抑制钠离子流入,从而稳定心膜和降低...

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CAS号20463-30-3 2,3,5,6-tetrahy... | CAS号94794-30-6 7Α-双稠吡咯啶-乙酸 | CAS号88069-56-1 四氢-1H-吡咯嗪-7a(5h... | CAS号87-62-7 2,6-二甲基苯胺 | CAS号100445-98-5 (Tetrahydro-pyr...

合成工艺路线路线简述

    📜δ4(8)-Dehydropyrrolizidinium Perchlorate置于sodium Hydride体系中,用 乙醇 作为反应溶剂,化学反应 12.0H,反应生成 吡西卡尼
    参考文献:新型抗心律失常药.n-芳基-8-吡咯烷基核烷酰胺.
    标题:新型抗心律失常药.n-芳基-8-吡咯烷基核烷酰胺.
    摘要:描述了n-芳基-8-吡咯烷核苷烷酰胺的合成和抗心律失常活性.评价目标化合物在小鼠中预防氯仿诱导的原纤维形成的能力.发现它们中的许多具有与利多卡因相当的抗纤颤活性.有几个比利多卡因更有效.发现n-(2,6-二甲基苯基)-8-吡咯嗪核苷乙酰胺比利多卡因更有效且毒性较低(ld50),口服犬心律失常的狗也表现出长效作用.
    DOI:10.1021/jm00383A005

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    主要参考文献


    1: Plosker GL. Pilsicainide. Drugs. 2010 Mar 5;70(4):455-67. doi: 10.2165/11204960-000000000-00000. 39(4):357-359. doi: 10.1097/PAF.0000000000000422. 66(16):2067-73. doi: 10.2165/00003495-200666160-00003. 59(17):2191-2195. doi: 10.2169/internalmedicine.4676-20. Epub 2020 May 26.
    5: Hasebe H, Yokoya T, Murakoshi N, Kurebayashi N. Pilsicainide Administration Unmasks a Phenotype of Brugada Syndrome in a Patient with Overlap Syndrome due to the E1784K SCN5A Mutation. Intern Med. 2020 Jan 1;59(1):83-87. doi: 10.2169/internalmedicine.3430-19. Epub 2019 Sep 3.
    6: Onohara T, Hisatome I, Kurata Y, Li P, Notsu T, Morikawa K, Otani N, Yoshida A, Iitsuka K, Kato M, Miake J, Ninomiya H, Higaki K, Shirayoshi Y, Nishihara T, Itoh T, Nakamura Y, Nishimura M. Molecular mechanisms underlying the pilsicainide-induced stabilization of hERG proteins in transfected mammalian cells. J Arrhythm. 2017 Jun;33(3):226-233. doi: 10.1016/j.joa.2016.09.003. Epub 2016 Oct 19.

    合成参考文献


    摘要:Conway DS, Lip GY. New antiarrhythmic agents for atrial fibrillation. Curr Opin Investig Drugs. 2001 Jan;2(1):87–92.
    参考文献:10.1016/j.jacc.2007.10.059
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    参考文献:10.1007/s00424-020-02445-7
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    参考文献:10.1016/s0022-0736(99)90003-1
    摘要:Namba T, Ashihara T, Nakazawa K, Ohe T. Effect of pilsicainide, a pure sodium channel blocker, on spiral waves during atrial fibrillation: theoretical analysis by numerical simulation. J Electrocardiol. 1999 Oct;32(4):321–34. doi: 10.1016/s0022-0736(99)90003-1.
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