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Bulleyaconitine A

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Chemical Structure| 107668-79-1 同义名 : Bulleyaconi cine A
CAS号 : 107668-79-1
货号 : A646674
分子式 : C35H49NO9
纯度 : 98%
分子量 : 627.765
MDL号 : MFCD01714791
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 20 mg/mL(31.86 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

动物实验配方:
生物活性
描述 Bulleyaconitine A (BLA) is a diterpenoid alkaloid isolated from Aconitum bulleyanum plants. Bulleyaconitine A preferably blocks tetrodotoxin-sensitive voltage-gated sodium channels in dorsal root ganglion neurons by inhibition of protein kinase C, and the effect is around 600 times more potent in neuropathic animals than in naïve ones. Bulleyaconitine A at 5 nM inhibits the hypersensitivity of dorsal root ganglion neurons in neuropathic rats but has no effect on excitability of dorsal root ganglion neurons in sham group[3]. Bulleyaconitine A was more potent for blocking Nav1.3 and Nav1.7 than Nav1.8 in cell lines. The half maximal inhibitory concentration (IC50) values for resting Nav1.3, Nav1.7, and Nav1.8 were 995.6 ± 139.1 nM, 125.7 ± 18.6 nM, and 151.2 ± 15.4 μM, respectively, which were much higher than those for inactivated Nav1.3 (20.3 ± 3.4 pM), Nav1.7 (132.9 ± 25.5 pM), and Nav1.8 (18.0 ± 2.5 μM)[4]. BLA was effective in inhibiting histamine-dependent and histamine-independent itches[5]. It is also activates PKC-δ/NF-κB to reduce airway inflammation in allergic asthma mice[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.96mL

1.59mL

0.80mL

15.93mL

3.19mL

1.59mL

参考文献

[1]Wang CF, Gerner P, et al. Use of bulleyaconitine A as an adjuvant for prolonged cutaneous analgesia in the rat. Anesth Analg. 2008 Oct;107(4):1397-405.

[2]Wang CF, Gerner P, et al. Bulleyaconitine A isolated from aconitum plant displays long-acting local anesthetic properties in vitro and in vivo. Anesthesiology. 2007 Jul;107(1):82-90.

[3]Xie MX, Zhu HQ, Pang RP, Wen BT, Liu XG. Mechanisms for therapeutic effect of bulleyaconitine A on chronic pain. Mol Pain. 2018 Jan-Dec;14:1744806918797243

[4]Xie MX, Yang J, Pang RP, Zeng WA, Ouyang HD, Liu YQ, Liu XG. Bulleyaconitine A attenuates hyperexcitability of dorsal root ganglion neurons induced by spared nerve injury: The role of preferably blocking Nav1.7 and Nav1.3 channels. Mol Pain. 2018 Jan-Dec;14:1744806918778491

[5]Huang Z, Zhou X, Zhang J, Mai CL, Mai JZ, Liu C, Zhang H, Liu XG. Bulleyaconitine A Inhibits Itch and Itch Sensitization Induced by Histamine and Chloroquine. Neuroscience. 2020 Mar 1;429:68-77

[6]Zhan X, Zhang W, Sun T, Feng Y, Xi Y, Jiang Y, Tang X. Bulleyaconitine A Effectively Relieves Allergic Lung Inflammation in a Murine Asthmatic Model. Med Sci Monit. 2019 Mar 4;25:1656-1662