8-hydroxyloxapine
8-hydroxyloxapine Basic information
- Product Name:
- 8-hydroxyloxapine
- Synonyms:
-
- 8-hydroxyloxapine
- 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepin-8-ol
- 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepin-3-ol
- Loxapine 8-Hydroxy Impurity
- Dibenz[b,f][1,4]oxazepin-8-ol, 2-chloro-11-(4-methyl-1-piperazinyl)-
- CAS:
- 61443-77-4
- MF:
- C18H18ClN3O2
- MW:
- 343.81
- Product Categories:
-
- Heterocycles
- Intermediates & Fine Chemicals
- Metabolites & Impurities
- Pharmaceuticals
- Mol File:
- 61443-77-4.mol
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8-hydroxyloxapine Chemical Properties
- Melting point:
- 212-215°C
- storage temp.
- Amber Vial, -20°C Freezer, Under Inert Atmosphere
- solubility
- DMSO: soluble
- form
- A solid
- Stability:
- Light Sensitive
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8-hydroxyloxapine Usage And Synthesis
Description
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 (Ki values = 7, 7.7, 9.5, 12, and 31 nM for H1, 5-HT2A, 5-HT2C, D2, and α1A-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).
Chemical Properties
Pale Yellow Solid
Uses
The inactive
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