Galanthamine

製品コードS3866 バッチS386603

印刷

化学情報

Chemical Structure Synonyms Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H21NO3
分子量 287.35 CAS No. 357-70-0
Solubility (25°C)* 体外 DMSO 28 mg/mL (97.44 mM)
Water 14 mg/mL (48.72 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
in vitro Galantamine shows reversible, competitive acetylcholinesterase inhibiting and nicotinic acetylcholinergic receptor modulatory properties[2]. Galantamine reduced the release of reactive oxygen species (up to 50%) and prevented loss in mitochondrial activity. Galantamine treatment resulted in a significant inhibition of H2O2-induced nitrite generation. Galantamine also concentration-dependently inhibited AChE activity (28–88%) in H2O2–SK-N-SH cells after 24 h. This drug, which facilitates cholinergic neurotransmission, is also neuroprotective by lowering oxidative injury[3].
in vivo Generally, oral absorption was rapid, with maximal plasma levels reached within 2 h in all species. Absolute oral bioavailability of a gavage dose was high in rat (77 %) and dog (78 %). In mice and rats, the bioavailability of galantamine administered via the food was lower than of galantamine administered by gavage. Elimination half-life of galantamine was relatively large in rat and dog and smaller in mouse and rabbit. After i.v. administration, galantamine plasma levels declined fairly rapidly in the various animal species tested with an elimination half-life of 1−5 h in the rat and 4−7 h in the dog. The volume of distribution was 4−5 l/kg in rats and dogs. Plasma clearance was highest in male rats, 1.9 l/kg/h, about twice the value of female rats and of dogs. Sex differences in pharmacokinetics of galantamine were shown to exist in rats and mice. Male rats generally had lower plasma values of galantamine and lower exposure rates; in mice, the effect was opposite. In dogs, no sex differences in the pharmacokinetics of galantamine could be detected. In mice and rats, the bioavailability of galantamine administered via the food was lower than of galantamine administered by gavage[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SK-N-SH cells
濃度 0.1-100 μM
反応時間 24 h
実験の流れ Cells are seeded in 96-multiwell dishes at a density of 100,000 cells/ml (100 ml in each well) for cytotoxicity and fluorescence detection or in six-well dishes (1 ml in each well) for measuring NO production and acetylcholinesterase (AChE) activity. Cells are treated with the drugs in serum-free DMEM. Experiments are carried out 24–48 h after cells are seeded. Cells are exposed for 2 h, either to H2O2 (500 μM), or galantamine alone (0.1-100 μM), or to the combination of H2O2 plus galantamine. As no change in AChE activity is seen after 2 h, SK-N-SH cells are also incubated with galantamine for 24 h.
動物実験 動物モデル Male Sprague Dawley rats
投薬量 0, 0.1, 1.0, or 5.0 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

α7-Acetylcholine Receptor Signaling Reduces Neuroinflammation After Subarachnoid Hemorrhage in Mice [ Neurotherapeutics, 2021, 10.1007/s13311-021-01052-3] PubMed: 33970466

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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