Olanzapine

Catalog No.S2493 Synonyms: LY170053

Olanzapine Chemical Structure

Molecular Weight(MW): 312.43975

Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

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In DMSO USD 130 In stock
USD 97 In stock
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Cited by 4 Publications

2 Customer Reviews

  • Punctuates of LC3 proteins in olanzapine-treated T98 and LN229 cells. Cells were incubated with olanzapine (0, 0.1M, 0.2mM) for 48h and then stained with the anti-LC3 antibody. Cells were examined by fluorescence confocal microscopy. Green: FITC-labeled LC3; Blue: DAPI-labeled nucleus. Magnification: x 400

    Asian Pac J Cancer Prev 2014 15(19), 8107-13. Olanzapine purchased from Selleck.

    Olanzapine and aripiprazole differentially regulate cellular glucose uptake of PBMC. Bar graphs depict cellular glucose uptake assessed by 18F-FDG in PBMC after 72 h of stimulation with the indicated concentrations of olanzapine (Olan, A) or aripiprazole (Arip, B) relative to corresponding DMSO controls (Ctrl) and normalized to protein content. Data are depicted as mean ± SD. P-values were computed by one-way ANOVA followed by Dunnett's Multiple Comparison Test. ***P < 0.001, **P < 0.01, *P < 0.05 versus control; results were obtained from n ¼ 4e6 independent cell isolations measured in duplicate.

    J Psychiatr Res, 2017, 88:18-27. Olanzapine purchased from Selleck.

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Biological Activity

Description Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Targets
5-HT2 [1] D2 receptor [1]
In vitro

Olanzapine interacts with key receptors of interest in schizophrenia, having a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors. Olanzapine has a receptor profile that is similar to that of clozapine: it is relatively nonselective at dopamine receptor subtypes and it shows selectivity for mesolimbic and mesocortical over striatal dopamine tracts (electrophysiology; Fos). [1]

In vivo Olanzapine is a potent antagonist at DA receptors (DOPAC levels; pergolide-stimulated increases in plasma corticosterone) and 5-HT receptors (quipazine-stimulated increases in corticosterone), but is weaker at alpha-adrenergic and muscarinic receptors. [1] Olanzapine combined with fluoxetine produces robust, sustained increases of extracellular levels of dopamine ([DA](ex)) and norepinephrine ([NE](ex)) up to 361% and 272% of the baseline in rat prefrontal cortex, respectively, which are significantly greater than either drug alone. [2] Olanzapine at 0.5 mg/kg, 3 mg/kg and 10 mg/kg (s.c.) dose-dependently increases the extracellular dopamine (DA) and norepinephrine (NE) levels in rat prefrontal cortex, nucleus accumbens and striatum. Olanzapine also increases extracellular levels of a DA metabolite, DOPAC, and tissue concentrations of a released DA metabolite, 3-methoxytyramine. [3] Olanzapine results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. [4] Olanzapine results in substantial increases in adiposity: increased total body fat reflecting marked increases in subcutaneous and visceral adipose stores. Olanzapine results in marked hepatic insulin resistance. [5]

Protocol

Solubility (25°C)

In vitro DMSO 62 mg/mL (198.43 mM)
Ethanol 9 mg/mL (28.8 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 312.43975
Formula

C17H20N4S

CAS No. 132539-06-1
Storage powder
in solvent
Synonyms LY170053

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03857581 Not yet recruiting Psychosis|Substance Use Disorders Augusta University May 2019 Phase 4
NCT03857581 Not yet recruiting Psychosis|Substance Use Disorders Augusta University May 2019 Phase 4
NCT03877562 Not yet recruiting Antipsychotic-induced Weight Gain Corcept Therapeutics April 1 2019 Phase 1
NCT03877562 Not yet recruiting Antipsychotic-induced Weight Gain Corcept Therapeutics April 1 2019 Phase 1
NCT03876938 Recruiting Antiemetic for Highly Emetogenic Chemotherapy Mahidol University March 1 2019 Phase 3
NCT03741478 Not yet recruiting Healthy Controls Centre for Addiction and Mental Health|University Health Network Toronto March 2019 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID