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| | 8-hydroxyloxapine Basic information |
| | 8-hydroxyloxapine Chemical Properties |
| Melting point | 212-215°C | | Boiling point | 523.713±60.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.393±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | storage temp. | Amber Vial, -20°C Freezer, Under Inert Atmosphere | | solubility | DMSO: soluble | | form | A solid | | pka | 10.351±0.20(predicted) | | Stability: | Light Sensitive | | InChI | 1S/C18H18ClN3O2/c1-21-6-8-22(9-7-21)18-14-10-12(19)2-4-16(14)24-17-5-3-13(23)11-15(17)20-18/h2-5,10-11,23H,6-9H2,1H3 | | InChIKey | VNJRIWXLPIYFGI-UHFFFAOYSA-N | | SMILES | Clc1cc2c([o]c3c(nc2N4CCN(CC4)C)cc(cc3)O)cc1 |
| WGK Germany | WGK 2 | | Storage Class | 3 - Flammable liquids | | Hazard Classifications | Acute Tox. 3 Dermal
Acute Tox. 3 Inhalation
Acute Tox. 3 Oral
Flam. Liq. 2
STOT SE 1 |
| | 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 | | References | [1] MD P S, PH.D Hubert H M V T Ph D Roy Corbett Ph D. Atypical Neuroleptics Have Low Affinity for Dopamine D2 Receptors or Are Selective for D4 Receptors[J]. Neuropsychopharmacology, 1997, 16 2: 93-110. DOI: 10.1016/s0893-133x(96)00187-x
[2] YIN CHEONG WONG Zhong Z Siu Kwan Wo. Investigation of the disposition of loxapine, amoxapine and their hydroxylated metabolites in different brain regions, CSF and plasma of rat by LC–MS/MS[J]. Journal of pharmaceutical and biomedical analysis, 2012, 58: Pages 83-93. DOI: 10.1016/j.jpba.2011.09.020
[3] ANDREW J GOUDIE. H1-histamine Receptor Affinity Predicts Short-term Weight Gain for Typical and Atypical Antipsychotic Drugs[J]. Neuropsychopharmacology, 2003, 28 12: 2209-2209. DOI: 10.1038/sj.npp.1300291
[4] JUSTIN FADEN L C. Examining the safety, efficacy, and patient acceptability of inhaled loxapine for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults[J]. Neuropsychiatric Disease and Treatment, 2019, 15 1: 2273-2283. DOI: 10.2147/ndt.s173567
[5] A. FULTON G. D B T Norman. Ligand binding and platelet uptake studies of loxapine, amoxapine and their 8-hydroxylated derivatives[J]. Journal of affective disorders, 1982, 4 2: Pages 113-119. DOI: 10.1016/0165-0327(82)90041-6 |
| | 8-hydroxyloxapine Preparation Products And Raw materials |
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