Gelsemine

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Chemical Structure| 509-15-9 同义名 : 钩吻素甲
CAS号 : 509-15-9
货号 : A660802
分子式 : C20H22N2O2
纯度 : 99%
分子量 : 322.401
MDL号 : MFCD00082347
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(325.68 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

H2O: 5 mg/mL(15.51 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方:
生物活性
描述 Gelsemine is one of the principal alkaloids produced by the Gelsemium genus of plants belonging to the Loganiaceae family. Gelsemine exerts anxiolytic and analgesic effects on behavioural models[3]. Gelsemine from Gelsemium elegans Benth is a potential anesthetic and analgesic agent with no physical dependence and opiate addiction[4]. Rats were intraperitoneally injected (500μl/daily/7days) with gelsemine (10(-6), 10(-10) or 10(-14)M) or control solution. Gelsemine or diazepam treatment did not affect the number of closed arm entries and rears illustrating the rat general activity. In contrast, gelsemine (10(-6) to 10(-10)M) or DZP increased dose-dependently the number of entries and the percent of time spent in the open arms indicating that gelsemine is an anxiolytic[5]. A single intrathecal injection of gelsemine produced potent and specific antinociception in formalin-induced tonic pain, bone cancer-induced mechanical allodynia, and spinal nerve ligation-induced painful neuropathy. The antinociception was dose-dependent, with maximal inhibition of 50% to 60% and ED50 values of 0.5 to 0.6 μg. Multiple daily intrathecal injections of gelsemine for 7 days induced no tolerance to antinociception in the rat model of bone cancer pain[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.02mL

6.20mL

3.10mL

参考文献

[1]Wu T, Chen G, et al. Anti-hyperlipidemic and anti-oxidative effects of gelsemine in high-fat-diet-fed rabbits. Cell Biochem Biophys. 2015 Jan;71(1):337-44.

[2]Zhao QC, Hua W, et al. Antitumor activity of two gelsemine metabolites in rat liver microsomes. J Asian Nat Prod Res. 2010 Sep;12(9):731-9.

[3]Lara CO, Murath P, Muñoz B, Marileo AM, Martín LS, San Martín VP, Burgos CF, Mariqueo TA, Aguayo LG, Fuentealba J, Godoy P, Guzman L, Yévenes GE. Functional modulation of glycine receptors by the alkaloid gelsemine. Br J Pharmacol. 2016 Jul;173(14):2263-77

[4]Zhang S, Hu S, Yang X, Shen J, Zheng X, Huang K, Xiang Z. Development of a liquid chromatography with mass spectrometry method for the determination of gelsemine in rat plasma and tissue: Application to a pharmacokinetic and tissue distribution study. J Sep Sci. 2015 Mar;38(6):936-42

[5]Meyer L, Boujedaini N, Patte-Mensah C, Mensah-Nyagan AG. Pharmacological effect of gelsemine on anxiety-like behavior in rat. Behav Brain Res. 2013 Sep 15;253:90-4

[6]Zhang JY, Gong N, Huang JL, Guo LC, Wang YX. Gelsemine, a principal alkaloid from Gelsemium sempervirens Ait., exhibits potent and specific antinociception in chronic pain by acting at spinal α3 glycine receptors. Pain. 2013 Nov;154(11):2452-62