Quetiapine-d8 (fumarate)

Quetiapine-d₈ is intended for use as an internal standard for the quantification of quetiapine by GC- or LC-MS. Quetiapine is an atypical, second generation antipsychotic compound.^1,2,3 It has effects at multiple receptors, antagonizing dopamine D₁, D₂, and D₃ receptors (K_is = 994, 379, and 340 nM, respectively), serotonin 5-HT_1A, 5-HT_2A, and 5-HT₇ receptors (K_is = 394, 118, and 307 nM, respectively), and α_1A, α_1B, and α_2C adrenergic receptors (K_is = 22, 15, and 29 nM, respectively).^4,5 Quetiapine also potently antagonizes the histamine H₁ receptor (K_i = 11 nM).⁵

1.Seeman, P.Atypical antipsychotics: Mechanism of actionCan. J. Psychiatry47(1)27-38(2002) 2.Rummel-Kluge, C., Komossa, K., Schwarz, S., et al.Second-generation antipsychotic drugs and extrapyramidal side effects: A systematic review and meta-analysis of head-to-head comparisonsSchizophr. Bull.38(1)167-177(2012) 3.Cerejeira, J., and Mukaetova-Ladinska, E.B.A clinical update on delirium: From early recognition to effective managementNurs. Res. Pract.875196(2011) 4.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 5.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)