|(7R,7aR,14R,14aS)-十四氢-7,14-甲桥二吡啶并[1,2-a:1',2'-e][1,5]二氮杂环辛烷|CsnPharm

CAS No.: 492-08-0

(7R,7aR,14R,14aS)-Dodecahydro-2H,6H-7,14-methanodipyrido[1,2-a:1',2'-e][1,5]diazocine Catalog No. CSN24909

Synonyms: Pachycarpin;Pachycarpine;d-Sparteine

Inhibition of human CYP2D6 expressed in Escherichia coli JM109

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技术信息

生物活性

描述Sparteine is a quinolizidine alkaloid extracted from Lupinus that has numerous pharmacological properties both in humans and animal models. In the central nervous system, sparteine reduces locomotor activity, has light analgesic effects, also has no effects on short-term memory or spatial learning and does not induce changes in behavior or electroencephalographic (EEG) activity. Sparteine decreases amplitude and frequency or blocks the epileptiform activity induced by PTZ (pentylenetetrazole), pilocarpine and kainic acid^[2]. Administration of sparteine, via ICV (intraventricular) or IP (intraperotineal), caused neuronal necrosis in brain structures, mainly related with cholinergic pathways^[3]. (+)-Sparteine (2 mM) reduced the ACh-induced current caused by activation of nicotinic ACh receptors (AChRs) in a voltage-independent manner at membrane potentials of -50 mV to +30 mV, whereas its blocking effect increased at more negative membrane potentials. At higher concentrations, i.e., 5 mM and 10 mM (lower concentrations were not effective), (+)-sparteine reduced the amplitude of the EPSC and the time constant of the EPSC decay. (+)-sparteine produces in ganglionic AChRs a competitive blocking effect and, in addition, an open-channel blockade^[4]. Sparteine exhibited a better anticonvulsant effect at a dose of 30 mg/kg (i.p.) than at the other doses used^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.2666 mL
- 21.3329 mL
- 42.6657 mL
- 5 mM
- 0.8533 mL
- 4.2666 mL
- 8.5331 mL
- 10 mM
- 0.4267 mL
- 2.1333 mL
- 4.2666 mL

技术信息

CAS号

492-08-0

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H26N2

运输

蓝冰

分子量

234.38

别名

Pachycarpin;Pachycarpine;d-Sparteine;(+)-鹰爪豆碱;鹰爪豆碱

溶解度

Water

2.0 mg/mL (8.5 mM) warming

动物实验配方

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(7R,7aR,14R,14aS)-Dodecahydro-2H,6H-7,14-methanodipyrido[1,2-a:1',2'-e][1,5]diazocine Catalog No. CSN24909

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