Galantamine Hydrobromide powder is the hydrobromide salt form of galantamine, a tertiary alkaloid with anticholinesterase and neurocognitive-enhancing activities. It is an alkaloid acetylcholinesterase inhibitor. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). This agent may improve neurocognitive function in mild and moderate Alzheimer’ s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse.
|Name||Galantamine Hydrobromide powder|
|Chemical name||(4aS,6R,8aS)-4a,5,9,10,11,12-Hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef]benzazepin-6-ol hydrobromide |
|Synonyms||Galanthamine Hydrobromide; Galantamine HBr; Nivalin; Razadyne; Reminyl; Nivaline; Razadyne. |
|Molecular Weight||368.271 g/mol|
|Melting Point||126.5 °C (259.7 °F)|
|Appearance||White to Off-white powder|
|Half Life||7 hours|
|Solubility||Soluble in DMSO, not in water|
|Storage Condition||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Application||Galantamine (brand names Razadyne, Reminyl, and others) is used for the treatment of cognitive decline in mild to moderate Alzheimer’s disease and various other memory impairments.|
Galantamine hydrobromide powder is a tertiary alkaloid obtained synthetically or naturally from the bulbs and flowers of Narcissus and several other genera of the Amaryllidaceae family with anticholinesterase and neurocognitive-enhancing activities. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). In addition, galantamine is a ligand for nicotinic acetylcholine receptors, which may increase the presynaptic release of Ach and activate postsynaptic receptors. This agent may improve neurocognitive function in mild and moderate Alzheimer’ s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse.
Galantamine Hydrobromide powder is able to get from the bulb of leucojum aestivum, the content is around 0.1% to 2% on dry basis. While Galantamine Hydrobromide has higher content up to 7.4% in phaedranassa negistrophylla, another name of Lycoris radiata plant. However, these plants are from key precious resources and protected by the government. There are 20 lycoris species in the world, and 16 species in China, locating along the middle and lower reaches of the Yangtze River. The raw plants nowadays are cultivated and bulk quantities are available. Lycoris radiata is the most popular natural source for the extraction of Galantamine Hydrobromide.
So how exactly does galantamine hydrobromide work? Although the act of cognitive impairment in Alzheimer’s (AD) isn’t fully understood, it’s been reported that acetylcholine-creating nerves degenerate within the brains of patients with Alzheimer’s.
The degree of this cholinergic loss continues to be correlated with amount of cognitive impairment and density of amyloid plaques (a neuropathological hallmark of Alzheimer’s).
Galantamine hydrobromide binds electrostatically towards the enzyme active site of cholinesterase. Binding is reversible, as a result it functions as a competitive reversible inhibitor of cholinesterase and extends the hydrolysis of endogenous acetylcholine, therefore growing its accumulation and extending and potentiating its effects, that are expressed in intensified and prolonged mediation at the amount of cholinergic postsynaptic membrane.
Galantamine hydrobromide has been discovered to exert direct impact on some CNS structures with cholinergic nerves. Additionally, it functions in CNS by reflex path, potentiating afferent impulses from some peripheral reflexogenic areas.
Galantamine is produced from natural resources and a patented total synthesis process. Many other synthetic methods exist but have not been implemented on an industrial scale.