Chlorpromazine D6 hydrochloride

Chlorpromazine-d₆ (CPZ-d₆) is intended for use as an internal standard for the quantification of CPZ by GC- or LC-MS. CPZ is a typical antipsychotic and an antagonist of dopamine D₂, D₃, and D₄ receptors (K_is = 0.66, 0.84, and 1.2 nM, respectively) as well as the serotonin (5-HT) receptor subtype 5-HT_2A (K_i = 1.8 nM).^1,2 It is also an antagonist of histamine H₁, α_1A-, α_2B-, and α_2C-adrenergic, and M₃ muscarinic acetylcholine receptors (K_is = 6, 0.28, 27, 46, and 47 nM, respectively).³ CPZ (10 mg/kg per day) increases latency to find the platform in a repealed acquisition water maze task and decreases vertical activity and stereotypic movements in the open field test in rats.⁴ CPZ (0.3, 1, and 3 mg/kg, s.c.) also reduces emesis induced by cisplatin in dogs.⁵

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 receptorsMol. Psychiatry3(2)123-134(1998) 2.Seeman, P., Corbett, R., and Van Tol, H.H.Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptorsNeuropsychopharmacology16(2)93-110(1997) 3.Kroeze, W.K., Hufeisen, S.J., Popadak, B.A., et al.H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugsNeuropsychopharmacology28(3)519-526(2003) 4.Terry, A.V., Jr., Warner, S.E., Vandenhuerk, L., et al.Negative effects of chronic oral chlorpromazine and olanzapine treatment on the performance of tasks designed to assess spatial learning and working memory in ratsNeuroscience156(4)1005-1016(2008) 5.Gylys, J.A., Doran, K.M., and Buyniski, J.P.Antagonism of cisplatin induced emesis in the dogRes. Commun. Chem. Pathol. Pharmacol.23(1)61-68(1979)