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Remoxipride is an atypical antipsychotic and dopamine D2 receptor antagonist (Ki = 0.2 µM).1 It is selective for the dopamine D2 receptor over a panel of 33 receptors, neurotransmitter transporters, and ion channels at 10 µM but does inhibit the sigma (σ) receptor (Ki = 0.065 µM). Remoxipride (2-20 µmol/kg, i.p.) increases striatal 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) levels in rats.2 It inhibits apomorphine-induced stereotypy and hyperactivity in rats with ED50 values of 5.6 and 0.8 µmol/kg, respectively.3 Formulations containing remoxipride have previously been used in the treatment of schizophrenia.
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1. Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: Role of 5HT2 receptors. Psychopharmacology (Berl) 112(1 Suppl), S40-S54 (1993).
2. Effects of the dopamine D2 selective receptor antagonist remoxipride on dopamine turnover in the rat brain after acute and repeated administration. Pharmacol. Toxicol. 60(5), 368-373 (1987).
3. Remoxipride, a new potential antipsychotic compound with selective antidopaminergic actions in the rat brain. Eur. J. Pharmacol. 102(3-4), 459-574 (1984).