8-hydroxyloxapine

8-hydroxyloxapine Property

Melting point:

212-215°C

storage temp. 

Amber Vial, -20°C Freezer, Under Inert Atmosphere

solubility 

DMSO: soluble

form 

A solid

Stability:

Light Sensitive

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

8-hydroxyloxapine Chemical Properties,Usage,Production

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 (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).

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