Molecular Formula | C17H19NO3 |
Molar Mass | 285.34 |
Density | 1.28±0.1 g/cm3(Predicted) |
Melting Point | 175-180°C (dec.) |
Boling Point | 397.4±42.0 °C(Predicted) |
Flash Point | 194.134°C |
Solubility | Chloroform, DMSO, Methanol |
Vapor Presure | 0mmHg at 25°C |
pKa | 7.84±0.20(Predicted) |
Storage Condition | Sealed in dry,2-8°C |
Refractive Index | 1.626 |
Physical and Chemical Properties | White crystalline powder, odorless, bitter taste. Melting point 258-264 °c. Soluble in water, ethanol-soluble, insoluble in acetone, chloroform, ether and benzene. After reaction with ammonium molybdate solution, water bath evaporation, plus sulfuric acid blue-green. Galantamine was dissolved in anhydrous ethanol by heating, and hydrogen bromide was added. Anti-cholinesterase drugs, Galanthamine Hydrobromide, compared with neostigmine, weak effect, low toxicity. Since the sensitivity of the choline receptor is increased, the inhibited neuromuscular conduction in the skeletal muscle is restored, and the paralysis state caused by the neuromuscular conduction disorder is improved, thereby enhancing the motor function. This product can penetrate the blood-brain barrier, central role is strong, early clinical mainly for the treatment of polio sequelae and myasthenia gravis. |
In vitro study | 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. |
In vivo study | 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 |