61443-77-4

8-hydroxy Loxapine (8-OH loxapine) is a metabolite formed when loxapine , an atypical antipsychotic, is metabolized by the cytochrome P450 isoform CYP1A2. Loxapine displays high affinity for histamine, serotonin (5-HT), dopamine, and α₁-adrenergic receptors (K_i values = 7, 7.7, 9.5, 12, and 31 nM for H₁, 5-HT_2A, 5-HT_2C, D₂, and α_1A-adrenergic receptors, respectively). It reduces agitation associated with schizophrenia or bipolar disorder. 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 μM in human platelets).

Pale Yellow Solid

The inactive

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