Eticlopride (hydrochloride)

Eticlopride is a dopamine D₂ and D₃ receptor antagonist (K_is = 0.029 and 0.46 nM in MN9D mouse neuronal cells expressing rat D₂ and human D₃ receptors, respectively).¹ It is selective for dopamine D₂ and D₃ receptors (IC₅₀s = 1 and 113 nM, respectively) over dopamine D₁, α₂-adrenergic, and β-adrenergic, histamine H₁, and muscarinic receptors (IC₅₀s = 700->100,000 nM), as well as the serotonin (5-HT) receptor subtypes 5-HT₁ and 5-HT₂ (IC₅₀s = 6,200 and 830, respectively), but does bind α₁-adrenergic receptors (α₁-ARs; IC₅₀ = 110 nM) in radioligand binding assays.² Eticlopride (10 μg/kg) inhibits stereotyped behavior in rats induced by 7-hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT).³ It also inhibits ketamine- and cocaine-induced hypermotility in rats when administered at doses of 20 and 50 μg/kg, respectively.

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1. Tang, L., Todd, R.D., Heller, A., et al. Pharmacological and functional characterization of D₂, D₃ and D₄ dopamine receptors in fibroblast and dopaminergic cell lines. J. Pharmacol. Exp. Ther. 268(1), 495-502 (1994).

2. Hall, H., Köhler, C., and Gawell, L. Some in vitro receptor binding properties of [³H]eticlopride, a novel substituted benzamide, selective for dopamine-D₂ receptors in the rat brain. Eur. J. Pharmacol. 111(2), 191-199 (1985).

3. Giuliani, D., and Ferrari, F. Involvement of dopamine receptors in the antipsychotic profile of (–) eticlopride. Physiol. Behav. 61(4), 563-567 (1997).