Ziprasidone-d8

Ziprasidone-d8 is intended for use as an internal standard for the quantification of ziprasidone (Item No. 15031) by GC- or LC-MS. Ziprasidone is an atypical antipsychotic.{26444} 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]GTPyS binding assays.{54360,22640} Ziprasidone is an antagonist at 5-HT2A and dopamine D2 receptors (Kis = 1.15 and 1.29 nM, respectively) in cell-based assays.{54361} 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.