Haloperidol D4

Haloperidol-d₄ is intended for use as an internal standard for the quantification of haloperidol by GC- or LC-MS. Haloperidol is a typical antipsychotic and dopamine D₂-like receptor antagonist (K_is = 0.6, 0.2, and 22 nM, for D₂, D₃, and D₄ receptors, respectively).¹ It also acts as an inverse agonist at dopamine D₂ and D₃ receptors (IC₅₀s = 0.8 and 0.6 nM, respectively). Haloperidol also binds to α₁- and α₂- adrenergic and histamine H₁ receptors, as well as the serotonin (5-HT) receptor subtypes 5-HT_1D and 5-HT_2A (K_ds = 17, 600, 260, 40, and 61 nM, respectively).² It inhibits stereotypic behavior induced by apomorphine and amphetamine in rats (ID₅₀s = 0.532 and 0.101 μmol/kg, respectively).³ Haloperidol also inhibits apomorphine-induced decreases in prepulse inhibition of the acoustic startle response in rats in a dose-dependent manner.⁴ Formulations containing haloperidol have been used in the treatment of schizophrenia and Tourette syndrome.

1.Burstein, E.S., Ma, J., Wong, S., et al.Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonistJ. Pharmacol. Exp. Ther.315(3)1278-1287(2005) 2.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 3.Creese, I., Burt, D.R., and Snyder, S.H.Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugsJ. Neuropsychiatry Clin. Neurosci.8(2)223-226(1996) 4.Swerdlow, N.R., and Geyer, M.A.Clozapine and haloperidol in an animal model of sensorimotor gating deficits in schizophreniaPharmacol. Biochem. Behav.44(3)741-744(1993)