Geissoschizine methyl ether

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Chemical Structure| 60314-89-8 同义名 : 缝籽木嗪甲醚
CAS号 : 60314-89-8
货号 : A349870
分子式 : C22H26N2O3
纯度 : 99%
分子量 : 366.45
MDL号 : MFCD30725476
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(286.53 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 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 agonist[1]. 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 cortex[2]. 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-competitive[3]. 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 seizures[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.64mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL
参考文献

[1]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

[2]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

[3]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

[4]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