Reduced Haloperidol

Reduced haloperidol is an active metabolite of haloperidol (Item No. 12014).¹ It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (K_is = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells.² It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (K_is = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters).¹ Reduced haloperidol (0.5 mg/kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity.³

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1. Bryan-Lluka, L.J., Siebert, G.A., and Pond, S.M. Potencies of haloperidol metabolites as inhibitors of the human noradrenaline, dopamine and serotonin transporters in transfected COS-7 cells. Naunyn Schmiedebergs Arch. Pharmacol. 360(2), 109-115 (1999).

2. Dalwadi, D.A., Kim, S., and Schetz, J.A. Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia. Neurochem Int. 105(5), 27-31 (2017).

3. Entrena, J.M., Cobos, E.J., Nieto, F.R., et al. Antagonism by haloperidol and its metabolites of mechanical hypersensitivity induced by intraplantar capsaicin in mice: Role of sigma-1 receptors. Psychopharmacology (Berl.) 205(1), 21-33 (2008).