中文名 | 左旋那维定 |
英文名 | (-)-Narwedine |
别名 | 那维定 左旋那维定 加兰他敏酮 左旋那维啶 加兰他敏杂质 加兰他敏杂质A 加兰他敏杂质A(EP) 氢溴酸加兰他敏EP杂质A (4AS,8AS)-3-甲氧基-11-甲基-9,10,11,12-四氢-4AH-苯并[2,3]苯并呋喃[4,3-CD]氮杂卓-6(5H)-酮 |
英文别名 | (4aS 8aS)- Narwedine (-)-Narwedine GALANTHAMINONE Galanthaminone Galanthamine, 3-deoxy-3-oxo- GalantaMinone (GalantaMine IMpurity A) GalantaMine interMediate ((-)-Narwedine) (4aS,8aS)-4a,5,9,10,11,12-Hexahydro-3-Methoxy-11-Methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-one 6H-Benzofuro[3a,3,2-ef][2]benzazepin-6-one,4a,5,9,10,11,12-hexahydro-3-Methoxy-11-Methyl-, (4aS,8aS)- (4aS,8aS)-3-Methoxy-11-methyl-4a,5,9,10,11,12-hexahydro-6H-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-one 6H-benzofuro[3a,3,2-ef][2]benzazepin-6-one, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4aS,8aS)- |
CAS | 510-77-0 |
化学式 | C17H19NO3 |
分子量 | 285.34 |
InChI | InChI=1/C17H19NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,14H,7-10H2,1-2H3/t14-,17-/m0/s1 |
密度 | 1.28±0.1 g/cm3(Predicted) |
熔点 | 175-180°C (dec.) |
沸点 | 397.4±42.0 °C(Predicted) |
闪点 | 194.134°C |
蒸汽压 | 0mmHg at 25°C |
溶解度 | 氯仿、DMSO、甲醇 |
折射率 | 1.626 |
酸度系数 | 7.84±0.20(Predicted) |
存储条件 | Sealed in dry,2-8°C |
物化性质 | 白色结晶性粉末,无臭,味苦。熔点258—264℃。溶于水,微溶于乙醇,不溶于丙酮、氯仿、乙醚和苯。与钼酸铵溶液反应后,水浴蒸干,加硫酸显蓝绿色。将加兰他敏加热溶于无水乙醇中,通入溴化氢即得。 抗胆碱酯酶药,氢溴酸加兰他敏与新斯的明相比,作用弱,毒性低。由于提高胆碱受体的感受性,使骨骼肌中受阻抑的神经肌肉传导恢复,改善因神经肌肉传导障碍引起的麻痹状态,从而增强其运动功能。本品可透过血脑屏障,中枢作用较强,早期临床上主要用于治疗小儿麻痹后遗症及重症肌无力等。 |
体外研究 | Galanthaminone reduces the action of AChE and therefore tends to increase the concentration of acetylcholine in the brain. is also an allosteric ligand at nicotinic acetylcholine receptors. It has shown activity in modulating the nicotinic cholinergic receptors on cholinergic neurons to increase acetylcholine release. |
体内研究 | Absorption of Galanthaminone is rapid and complete and shows linear pharmacokinetics. It is well absorbed with absolute oral bioavailability between 80 and 100%. It has a half-life of seven hours. Peak effect of inhibiting acetylcholinesterase was achieved about one hour after a single oral dose of 8 mg in some healthy volunteers. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.505 ml | 17.523 ml | 35.046 ml |
5 mM | 0.701 ml | 3.505 ml | 7.009 ml |
10 mM | 0.35 ml | 1.752 ml | 3.505 ml |
5 mM | 0.07 ml | 0.35 ml | 0.701 ml |
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