An internal standard for the quantification of chlorpromazine
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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 (Kis = 0.66, 0.84, and 1.2 nM, respectively) as well as the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 1.8 nM).1,2 It is also an antagonist of histamine H1, α1A-, α2B-, and α2C-adrenergic, and M3 muscarinic acetylcholine receptors (Kis = 6, 0.28, 27, 46, and 47 nM, respectively).3 CPZ (10 mg/kg per day) increases latency to find the platform in a repealed acquisition water maze task and decreases vertical activity and stereotypic movements in the open field test in rats.4 CPZ (0.3, 1, and 3 mg/kg, s.c.) also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)
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