Droperidol

Droperidol is a dopamine D₂ and D₄ receptor antagonist (K_is = 0.25 and 0.84 nM for human D₂ and D₄ receptors, respectively).¹ It also inhibits the voltage-gated potassium channel hERG, also known as K_v11.1 (IC₅₀ = 32 nM), and binds to the serotonin (5-HT) receptor subtype 5-HT₂ (K_i = 1.1 nM).^2,3 Droperidol (1, 5, and 10 µM) decreases action potential duration in isolated canine Purkinje fibers.⁴ It prevents apomorphine-induced vomiting in dogs (ED₅₀ = 0.0012 mg/kg) and induces catalepsy in rats (ED₅₀ = 0.13 mg/kg).⁵ Formulations containing droperidol have been used in the treatment of surgery-associated nausea and vomiting.

WARNING This product is not for human or veterinary use.

1. Seeman, P., and Tallerico, T. Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D₂ receptors, yet occupy high levels of these receptors. Mol. Psychiatry 3(2), 123-134 (2016).

2. Rajamani, R., Tounge, B.A., Li, J., et al. A two-state homology model of the hERG K⁺ channel: Application to ligand binding. Bioorg. Med. Chem. Lett. 15(6), 1737-1741 (2005).

3. Leysen, J.E., Janssen, P.M.F., Schotte, A., et al. 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).

4. Wojtczak, J., and Beresewicz, A. Electrophysiological effects of the neuroleptanalgesic drugs on the canine cardiac tissue. Naunyn Schmiedebergs Arch Pharmacol. 286(2), 211-220 (1974).

5. Niemegeers, C.J.E. Antiemetic specificity of dopamine antagonists. Psychopharmacology (Berl.) 78(3), 210-213 (1982).