Strychnine hydrochloride
(Synonyms: 盐酸士的宁) 目录号 : GD21200Strychnine hydrochloride是Strychnine与一摩尔当量的HCl化合而得的盐酸盐,Strychnine具有杀鸟剂、胆碱能拮抗剂、甘氨酸受体拮抗剂、杀鼠剂和神经递质剂的作用。
Cas No.:1421-86-9
Sample solution is provided at 25 µL, 10mM.
Strychnine hydrochloride is a hydrochloride obtained by combining Strychnine with one molar equivalent of HCl. Strychnine has the effects of an aviicide, cholinergic antagonist, glycine receptor antagonist, rodenticide and neurotransmitter[1, 2, 3]. Strychnine is a toxic alkaloid extract extracted from the dried mature seeds of Strychnos nux-vomica L.[4]. Strychnine can selectively excite the spinal cord and enhance the tension of skeletal muscles. It is clinically used to treat mild paresis or amblyopia[5].
In vivo, Strychnine hydrochloride (0.1, 0.3, 0.9mg/kg) was orally treated with Wistar rats for 7 days. The high-dose group significantly reduced the activities of the three subfamilies of cytochrome P450 (CYP) CYP3A, CYP1A2 and CYP2C, and significantly increased the activity of CYP2E1[6].
References:
[1] Mohsen A M Y. Structure Activity Relationships of Monomeric and Dimeric Strychnine Analogs as Ligands Targeting Glycine Receptors[M]. Bayerische Julius-Maximilians-Universitaet Wuerzburg (Germany), 2016.
[2] Marrs T C, Maynard R L. Neurotranmission systems as targets for toxicants: A review[J]. Cell Biology and Toxicology, 2013, 29: 381-396.
[3] Patocka J. Strychnine[M]//Handbook of toxicology of chemical warfare agents. Academic Press, 2020: 239-247.
[4] Behera M C, Mohanty T L, Paramanik B K. Silvics, phytochemistry and ethnopharmacy of endangered poison nut tree (Strychnos nux-vomica L.): A review[J]. Journal of Pharmacognosy and Phytochemistry, 2017, 6(5): 1207-1216.
[5] Huang N, Wang Y, Zhan G, et al. Contribution of skeletal muscular glycine to rapid antidepressant effects of ketamine in an inflammation-induced mouse model of depression[J]. Psychopharmacology, 2019, 236: 3513-3523.
[6] Gao Q, Wang J, Han F, et al. Effect of strychnine hydrochloride on liver cytochrome P450 mRNA expression and monooxygenase activities in rat[J]. Acta Pharmaceutica Sinica B, 2011, 1(2): 121-128.
Strychnine hydrochloride是Strychnine与一摩尔当量的HCl化合而得的盐酸盐,Strychnine具有杀鸟剂、胆碱能拮抗剂、甘氨酸受体拮抗剂、杀鼠剂和神经递质剂的作用[1, 2, 3]。Strychnine是一种有毒的生物碱提取物,提取自马钱子(Strychnos nux-vomica L.)的干燥成熟种子[4]。Strychnine能够选择性兴奋脊髓,增强骨骼肌的紧张度,临床用于轻瘫或弱视的治疗[5]。
在体内,Strychnine hydrochloride(0.1, 0.3, 0.9mg/kg)通过口服处理Wistar大鼠7天,高剂量组显著降低了细胞色素P450(CYP)的三个亚家族CYP3A、CYP1A2和CYP2C的活性,显著增加了CYP2E1的活性[6]。
Animal experiment [1]: | |
Animal models | Male Wistar rats |
Preparation Method | A total of 18 rats were randomly divided into 6 groups (n=3/group) and given an oral dose of A: saline containing 0.5% CMC; B: Strychnine hydrochloride 0.1mg/kg/day; C: Strychnine hydrochloride 0.3mg/kg/day; D: Strychnine hydrochloride 0.9mg/kg/day; E: Strychnine hydrochloride 0.9mg/kg/day plus Glycyrrhetic acid 25mg/kg/day; and F: Strychnine hydrochloride 0.9mg/kg/day plus Liquiritin 20mg/kg/day once a day for 7 consecutive days. Animals were sacrificed 1h after the last dose and livers were immediately removed and sliced into two parts. One part was weighed, washed in cold homogenization buffer (0.25mol/L sucrose, 0.01mol/L tris–HCl, 1mmol/L EDTA, pH 7.4) and used to prepare rat liver microsomes (RLM)17. The other was stored in liquid nitrogen until used for mRNA extraction. |
Dosage form | 0.1, 0.3, 0.9mg/kg/day for 7 days; p.o. |
Applications | Compared to control, the mRNA expressions of CYP3A1, 1A2 and 2E1 were higher in rats receiving the highest dose of Strychnine hydrochloride. CYP2E1 activity was higher and CYP2C, CYP3A and CYP1A2 activities were lower in rats receiving the highest dose of Strychnine hydrochloride. |
References: |
Cas No. | 1421-86-9 | SDF | |
别名 | 盐酸士的宁 | ||
分子式 | C21H23ClN2O2 | 分子量 | 370.87 |
溶解度 | 储存条件 | Store at -20°C, argon filling | |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.6964 mL | 13.4818 mL | 26.9636 mL |
5 mM | 0.5393 mL | 2.6964 mL | 5.3927 mL |
10 mM | 0.2696 mL | 1.3482 mL | 2.6964 mL |
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