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개요Acamprosate is an acetylated derivative of the GABA analog homotaurine (tramiprosate; ). Despite its structural similarity to GABA, acamprosate does not act at GABAA receptors but does decrease paired-pulse inhibition of GABAA inhibitory post-synaptic currents (IPSCs) at short inter-stimulus intervals when used at a concentration of 300 μM, indicating that it may inhibit GABAB autoreceptor-mediated inhibition of GABA release. It is an NMDA receptor modulator with antagonist or agonist effects depending on brain region, receptor subunit composition, and other factors. Acamprosate (0.26 and 0.52 mmol/kg per day, i.p.) reduces voluntary intake of ethanol in rats, an effect that can be blocked by the GABA antagonist bicuculline . Formulations containing acamprosate have been used for the maintenance of alcohol abstinence.

용도Acamprosate calcium is a synthetic amino acid and a neurotransmitter analogue that is used as an alcohol deterrent in management of alcohol dependence and abuse. Acamprosate calcium was approved for use in the therapy of alcohol dependence and abuse in the United States in 2004.