A loxapine metabolite; inhibits [14C]5-HT uptake in vitro (IC50 = 2 μM in human platelets)

8-hydroxy Loxapine – 1 mg

Brand:
Cayman
CAS:
61443-77-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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 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).{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 μM in human platelets).{36039}  

 

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Description

A loxapine metabolite; inhibits [14C]5-HT uptake in vitro (IC50 = 2 μM in human platelets),

Formal name: 2-chloro-11-(4-methyl-1-piperazinyl)-dibenz[b,f][1,4]oxazepin-8-ol

Synonyms:  8-OH Loxapine

Molecular weight: 343.8

CAS: 61443-77-4

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Neuroscience|Behavioral Neuroscience|Bipolar Disorder||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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