Ziprasidone-d8 is intended for use as an internal standard for the quantification of ziprasidone by GC- or LC-MS. Ziprasidone is an atypical antipsychotic.1 It is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 36.31 nM for inhibition of forskolin-induced adenylate cyclase activity in HeLa cells expressing human receptors), as well as an inverse agonist of 5-HT1D receptors (IC50 = 2.69 nM) and a partial agonist of 5-HT1B receptors (EC50 = 6.17 nM) in [35S]GTPγS binding assays.2,3 Ziprasidone is an antagonist at 5-HT2A and dopamine D2 receptors (Kis = 1.15 and 1.29 nM, respectively) in cell-based assays.4 It inhibits d-amphetamine-induced hyperactivity and apomorphine-induced stereotypy in rats (ID50s = 1.53 and 2.43 mg/kg, respectively). Formulations containing ziprasidone have been used in the treatment of schizophrenia and bipolar I disorder.
1.Seeman, P.Atypical antipsychotics: Mechanism of actionCan. J. Psychiatry47(1)27-38(2002) 2.Schmidt, A.W., Lebel, L.A., Howard, H.R., Jr., et al.Ziprasidone: A novel antipsychotic agent with a unique human receptor binding profileEur. J. Pharmacol.425(3)197-201(2001) 3.Audinot, V., Newman-Tancredi, A., Cussac, D., et al.Inverse agonist properties of antipsychotic agents at cloned, human (h) serotonin (5-HT)1B and h5-HT1D receptorsNeuropsychopharmacology25(3)410-422(2001) 4.Seeger, T.F., Seymour, P.A., Schmidt, A.W., et al.Ziprasidone (CP-88,059): A new antipsychotic with combined dopamine and serotonin receptor antagonist activityJ. Pharmacol. Exp. Ther.275(1)101-113(1995)