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Acamprosate-d3 is intended for use as an internal standard for the quantification of acamprosate by GC- or LC-MS. Acamprosate is an acetylated derivative of the GABA analog homotaurine .1 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.2,3,4 It is an NMDA receptor modulator with antagonist or agonist effects depending on brain region, receptor subunit composition, and other factors.4 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.

1.Boismare, F., Daoust, M., Moore, N., et al.A homotaurine derivative reduces the voluntary intake of ethanol by rats: Are cerebral GABA receptors involved•Pharmacol. Biochem. Behav.21(5)787-789(1984) 2.Reilly, M.T., Lobo, I.A., McCracken, L.M., et al.Effects of acamprosate on neuronal receptors and ion channels expressed in Xenopus oocytesAlcohol. Clin. Exp. Res.32(2)188-196(2008) 3.Berton, F., Francesconi, W.G., Madamba, S.G., et al.Acamprosate enhances N-methyl-D-apartate receptor-mediated neurotransmission but inhibits presynaptic GABAB receptors in nucleus accumbens neuronsAlcohol Clin. Exp. Res.22(1)183-191(1998) 4.Tomek, S.E., Lacrosse, A.L., Nemirovsky, N.E., et al.NMDA receptor modulators in the treatment of drug addictionPharmaceuticals (Basel)6(2)251-268(2013)

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