(±)-Sulpiride

(±)-Sulpiride is an atypical antipsychotic that binds to dopamine D₂ and D₃ receptors (K_is = 4.2 and 15 nM, respectively).¹ It is selective for dopamine D₂ and D₃ over D₁ receptors and the serotonin (5-HT) receptor subtypes 5-HT_1A, 5-HT_2A, 5-HT_2C, and 5-HT₃ (K_is = >10,000 nM). (±)-Sulpiride (0.5 or 1 ng per animal) increases attentional accuracy and decreases latency to respond correctly, the number of omissions, and impulsivity in the 5-choice serial reaction time task (5CSRTT) when infused directly into the nucleus accumbens in a rat model of prefrontal cortex lesion-induced attentional dysfunction.² It increases cortical and striatal demethylation of hypermethylated reelin and GAD67 promoters in mice when administered at doses ranging from 12.5 to 50 μmol/kg twice per day for three days.³ Formulations containing (±)-sulpiride have been used in the treatment of schizophrenia.

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1. Toll, L., Berzetei-Gurske, I.P., Polgar, W.E., et al. Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. NIDA Res. Monogr. 178, 440-466 (1998).

2. Pezze, M.A., Dalley, J.W., and Robbins, T.W. Remediation of attentional dysfunction in rats with lesions of the medial prefrontal cortex by intra-accumbens administration of the dopamine D₂/3 receptor antagonist sulpiride. Psychopharmacology (Berl.) 202(1-3), 307-313 (2009).

3. Dong, E., Nelson, M., Grayson, D.R., et al. Clozapine and sulpiride but not haloperidol or olanzapine activate brain DNA demethylation. Proc. Natl. Acad. Sci. USA 105(36), 13614-13619 (2008).