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Geissoschizine methyl ether

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  • A349870
  • 2026年05月27日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 英文名

      (Z)-Methyl 2-((2S,12bS,E)-3-ethylidene-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizin-2-yl)-3-methoxyacrylate

    • 供应商

      上海安毕达生物科技有限公司

    • CAS号

      60314-89-8

    • 规格

      1mg/5mg/10mg

    规格:1mg产品价格:¥1040.0
    规格:5mg产品价格:¥3200.0
    规格:10mg产品价格:¥4750.0
    Geissoschizine methyl ether是一种强效的5-HTA受体激动剂。

    Geissoschizine methyl ether, a major indole alkaloid found in Uncaria hook, is a major active component of Yokukansan with psychotropic effects. Geissoschizine methyl ether is potent 5-HT1A receptor agonist1. In the brains, GM (Geissoschizine methyl ether) was presumed to bind to 5- HT1A, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors on neuron-like large cells mainly in the frontal cortex2. Geissoschizine methyl ether (1) inhibited 50% of AChE activity at concentrations of 3.7 ± 0.3 µg mL(-1) while the IC(50) value of physostigmine as a standard was 0.013 ± 0.002 µg mL(-1). The mode of AChE inhibition by 1 was reversible and non-competitive3. GM (Geissoschizine methyl ether) potently inhibited the voltage-gated sodium (NaV), calcium (CaV), and delayed rectifier potassium (IK) currents, and the ligand-gated nicotinic acetylcholine (nACh) currents with IC50 values in the range of 1.3-13.3 μmol/L. In the maximal electroshock (MES)-induced mouse seizure model, oral administration of GM (50-100 mg/kg) dose-dependently suppressed generalized tonic-clonic seizures. In 6-Hz-induced mouse seizure model, oral administration of GM (100 mg/kg) reduced treatment-resistant seizures4.

    溶解方案(细胞实验)

    DMSO 中的溶解度 : 100 mg/mL (272.89 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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    图标文献和实验
    该产品被引用文献
    Nishi A, Yamaguchi T, Sekiguchi K, Imamura S, Tabuchi M, Kanno H, Nakai Y, Hashimoto K, Ikarashi Y, Kase Y. Geissoschizine methyl ether, an alkaloid in Uncaria hook, is a potent serotonin ₁A receptor agonist and candidate for amelioration of aggressiveness and sociality by yokukansan. Neuroscience. 2012 Apr 5;207:124-36

    Ikarashi Y, Sekiguchi K, Mizoguchi K. Serotonin Receptor Binding Characteristics of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook. Curr Med Chem. 2018;25(9):1036-1045

    Yang ZD, Duan DZ, Du J, Yang MJ, Li S, Yao XJ. Geissoschizine methyl ether, a corynanthean-type indole alkaloid from Uncaria rhynchophylla as a potential acetylcholinesterase inhibitor. Nat Prod Res. 2012;26(1):22-8

    Xie ZQ, Tian XT, Zheng YM, Zhan L, Chen XQ, Xin XM, Huang CG, Gao ZB. Antiepileptic geissoschizine methyl ether is an inhibitor of multiple neuronal channels. Acta Pharmacol Sin. 2020 May;41(5):629-637

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    Geissoschizine methyl ether
    ¥1040 - 4750