Acamprosate-d3 (calcium salt) (Synonyms: N-acetyl Homotaurinate-d3, N-acetyl Homotaurine-d3)

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 GABA_A receptors but does decrease paired-pulse inhibition of GABA_A inhibitory post-synaptic currents (IPSCs) at short inter-stimulus intervals when used at a concentration of 300 µM, indicating that it may inhibit GABA_B 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)