Acamprosate calcium,77337-73-6

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产品名称：Acamprosate calcium

产品别名：阿坎酸钙

英文别名：Calcium N-acetylhomotaurinate

靶点：GABA Receptor

CAS：77337-73-6

纯度：＞98%

外观：powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Acamprosate, also known by the brand name Campral?, is a drug used for treating alcohol dependence. Acamprosate is thought to stabilize the chemical balance in the brain that would otherwise be disrupted by alcoholism, possibly by blocking glutaminergic N-methyl-D-aspartate receptors, while gamma-aminobutyric acid type A receptors are activated. Reports indicate that acamprosate only works with a combination of attending support groups and abstinence from alcohol. Certain serious side effects include allergic reactions, irregular heartbeats, and low or high blood pressure, while less serious side effects include headaches, insomnia, and impotence. Acamprosate should not be taken by people with kidney problems or allergies to the drug.

溶解性：water : 20.2 mg/mL (100 mM)

体外研究：

Acamprosate binds to a specific spermidine-sensitive site that modulates the NMDA receptor in a complex way.

体内研究：Acamprosate is absorbed via the gastrointestinal tract, with pharmacokinetic linearity in terms of dose and time. Absolute bioavailability of acamprosate under fasting conditions is approximately 11%. After food intake, bioavailability decreases by approximately 20%, but this decrease lacks clinical significance. Steady-state plasma concentrations of acamprosate are reached within 5 days of dosing and the terminal half-life ranges from 20–33 hours following the standard 2 × 333 dosing regime. Plasma protein binding is negligible. Acamprosate is not metabolized in the liver and is excreted unchanged in the urine. Acamprosate may have neuroprotective effects. Acamprosate appears to work by normalizing the dysregulation of NMDA-mediated glutamatergic neurotransmission that occurs during chronic alcohol consumption and withdrawal, and thus attenuates one of the physiological mechanisms that may prompt relapse.

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