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- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
Galantamine
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
357-70-0
- 规格:
10 mM * 1 mL/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥605.0 |
|---|---|---|---|
| 规格: | 50 mg | 产品价格: | ¥550.0 |
| 规格: | 100 mg | 产品价格: | ¥850.0 |
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Galanthamine
CAS No. : 357-70-0
MCE 国际站:Galanthamine
产品活性:Galanthamine 是一种有效的乙酰胆碱酯酶 (AChE) 抑制剂,IC50 为 500 nM。
研究领域:Neuronal Signaling | Apoptosis
In Vitro: Galanthamine inhibits AChE and BChE with IC50 of 0.5 and 8.5 μM. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes.
In Vivo: Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine.
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文献和实验溴吡斯的明(phyridostigmine bromide)口服,60mg/次,3次/日,极量,120mg/次,360mg/日。 氢溴酸加兰他敏(galanthamine hydrobromide)肌内注射,2.5~10mg/次,1次/日。 碘解磷定(pyraloxime methoiodide)0.5~1g/次,缓慢静脉注射。 氯磷定(pyraloxime methylchloride)0.25~0.75g/次,肌内注射。0.5~0.75g/次,加于等渗盐水500
注射,0.25~0.5mg/次,极量,1mg/次。 溴吡斯的明(phyridostigmine bromide)口服,60mg/次,3次/日,极量,120mg/次,360mg/日。 氢溴酸加兰他敏(galanthamine hydrobromide)肌内注射,2.5~10mg/次,1次/日。 碘解磷定(pyraloxime methoiodide)0.5~1g/次,缓慢静脉注射。 氯磷定(pyraloxime methylchloride)0.25~0.75g/次,肌内
局部用于治疗青光眼,能缩小瞳孔,降低眼内压,收缩睫状肌而引起调节痉挛等。常用0.005%溶液滴眼,作用较毛果芸香碱强而持久,但刺激性较大。又由于收缩睫状肌的作用较强,可引起头痛。滴眼后5分钟即出现缩瞳,眼内压下降作用可维持1~2天,调节痉挛现象消失较快。滴眼时应压迫内眦,避免药液流入鼻腔后吸收,引起中毒。 加兰他敏(galanthamine)也是可逆性抗胆碱酯酶药,体外抗胆碱酯酶效价约为毒扁豆碱的1/10。可用于重症肌无力,但疗效较差,也用于脊髓前角灰白质炎(小儿麻痹症)后遗症的治疗。
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