8-hydroxy Loxapine

8-hydroxy Loxapine (8-OH loxapine) is a metabolite formed when loxapine (Item No. 20760), an atypical antipsychotic, is metabolized by the cytochrome P450 isoform CYP1A2.{24252,36038} Loxapine displays high affinity for histamine, serotonin (5-HT), dopamine, and a1-adrenergic receptors (Ki values = 7, 7.7, 9.5, 12, and 31 nM for H1, 5-HT2A, 5-HT2C, D2, and a1A-adrenergic receptors, respectively).{24252,24253} It reduces agitation associated with schizophrenia or bipolar disorder.{32724} 8-OH Loxapine is considered inactive as it has relatively low affinity to dopamine and 5-HT receptors compared to the parent compound, however, 8-OH loxapine inhibits [14C]5-HT uptake in vitro (IC50 = 2 ?M in human platelets).{36039}