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药品详细

Phosphatidylserine(磷脂酰丝氨酸)

化学结构式图
中文名
磷脂酰丝氨酸
英文名
Phosphatidylserine
分子式
C13H24NO10P
化学名
(2S)-2-amino-3-({[(2R)-2-(butanoyloxy)-3-(propanoyloxy)propoxy](hydroxy)phosphoryl}oxy)propanoic acid
分子量
Average: 385.3041
Monoisotopic: 385.113782505
CAS号
8002-43-5
ATC分类
药物类型
small molecule
阶段
approved, nutraceutical
商品名
同义名
基本介绍

Phosphatidylserine (PS) is a phospholipid nutrient found in fish, green leafy vegetables, soybeans and rice, and is essential for the normal functioning of neuronal cell membranes and activates Protein kinase C (PKC) which has been shown to be involved in memory function. In apoptosis, phosphatidylserine is transferred to the outer leaflet of the plasma membrane. This is part of the process by which the cell is targeted for phagocytosis. PS has been shown to slow cognitive decline in animal models. PS has been investigated in a small number of double-blind placebo trials and has been shown to increase memory performance in the elderly. Because of the potentail cognitive benefits of phosphatidylserine, the substance is sold as a dietary supplement to people who believe they can benefit from an increased intake.

The dietary supplement was originally processed from bovine sources however Prion disease scares in the 1990s outlawed this process, and a soy-based alternative was adopted.

生产厂家
    封装厂家
    • Professional Co.
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phospholipids
    • Amino Acids
    Substructures
    • Phospholipids
    • Carboxylic Acids and Derivatives
    • Glycerol and Derivatives
    • Hydroxy Compounds
    • Acetates
    • Phosphonic Acids and Derivatives
    • Organophosphate Esters
    • Aliphatic and Aryl Amines
    • Ethers
    • Phosphinic Acids and Derivatives
    • Amino Acids
    适应症
    药理
    Indication Phosphatidylserine has demonstrated some usefulness in treating cognitive impairment, including Alzheimer's disease, age-associated memory impairment and some non-Alzheimer's dementias. More research is needed before phosphatidylserine can be indicated for immune enhancement or for reduction of exercise stress.
    Pharmacodynamics Phosphatidylserine is indicated in the treatment of cognitive impairment, including Alzheimer's disease, age-associated memory impairment and some non-Alzheimer's dementias. Further research is required before phosphatidylserine can be indicated for immune enhancement or for reduction of exercise stress. Phosphatidylserine was first isolated from brain lipids called cephalins. The major cephalins are phosphatidylserine and phophatidylethanolamine. Phosphatidylserine is involved in signal transduction activity as well as being a basic structural component of biologic membranes.
    Mechanism of action Cholinergic hypofunction is thought to account in part for the cognitive deficits found in Alzheimer's disease. The most commonly used drugs for the treatment of Alzheimer's disease are reversible acetylcholinesterase inhibitors. The rationale of these drugs is to increase acetylcholine levels in the brains of Alzheimer's patients, and they may be somewhat effective in some cases. Phosphatidylserine restores acetylcholine release in aging humans by maintaining an adequate supply of the molecule and is able to increase the availability of endogenous choline for de novo acetylcholine synthesis. The hippocampus of the brain is believed to be important for cognitive processes and is affected in those with Alzheimer's disease. The dendritic spines of pyramidal cells, the post-synaptic target of the excitatory input to the hippocampus, have been proposed as a substrate for information storage. Age-dependent dendritic spine loss in pyramidal neurons has been reported in the human brain, and the extent of synaptic loss appears to correlate with the degree of cognitive impairment. Phosphatidylserine treatment prevents the age-related reduction in dendritic spine density in rat hippocampus. Protein kinase C facilitation of acetylcholine release has been reported in rats. Phosphatidylserine was found to restore protein kinase C activity in aging rats. Stimulation of calcium uptake by brain synaptosomes and activation of protein kinase C are yet other speculative mechanisms of phosphatidylserine's putative cognition-enhancing action.
    Absorption Absorbed in the small intestine.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Following absorption, lysophosphatidylserine is metabolized in intestinal mucosa cells, and its metabolites, which include some phosphatidylserine, enter the lymphatics draining the small intestine.
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity There are no reports of overdosage. LD50 in rats is more than 5g/kg, and in rabbits is more than 2g/kg.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    logP -3.5 Not Available
    Predicted Properties
    Property Value Source
    water solubility 3.70e+00 g/l ALOGPS
    logP -1 ALOGPS
    logP -1.6 ChemAxon
    logS -2 ALOGPS
    pKa (strongest acidic) 1.47 ChemAxon
    pKa (strongest basic) 9.38 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 7 ChemAxon
    hydrogen donor count 3 ChemAxon
    polar surface area 171.68 ChemAxon
    rotatable bond count 15 ChemAxon
    refractivity 81.81 ChemAxon
    polarizability 35.58 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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