Olanzapine

Catalog No.S2493 Batch:S249303

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Technical Data

Formula

C17H20N4S

Molecular Weight 312.43975 CAS No. 132539-06-1
Solubility (25°C)* In vitro DMSO 62 mg/mL (198.43 mM)
Ethanol 15 mg/mL (48.0 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) 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 (from reference)

Customer Product Validation

Data from [Data independently produced by Asian Pac J Cancer Prev, 2014, 15(19), 8107-13]

Data from [Data independently produced by , , J Psychiatr Res, 2017, 88:18-27]

Selleck's Olanzapine has been cited by 13 publications

Label-free cell assays to determine compound uptake or drug action using MALDI-TOF mass spectrometry [ Nat Protoc, 2021, 10.1038/s41596-021-00624-z] PubMed: 34759382
Second-generation antipsychotics induce cardiotoxicity by disrupting spliceosome signaling: Implications from proteomic and transcriptomic analyses [ Pharmacol Res, 2021, 170:105714] PubMed: 34098070
Trypsin-Mediated Sensitization to Ferroptosis Increases the Severity of Pancreatitis in Mice [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X] PubMed: 34562639
Identification of Required Host Factors for SARS-CoV-2 Infection in Human Cells [ Cell, 2020, S0092-8674(20)31394-5] PubMed: 33147445
Neuroprotective effects of olanzapine against rotenone-induced toxicity in PC12 cells. [ Acta Pharmacol Sin, 2020, 10.1038/s41401-020-0378-6] PubMed: 32123301
Entry of therapeutics into the brain: Influence of exposed polarity calculated in silico and measured in vitro by supercritical fluid chromatography. [ Int J Pharm, 2019, 560:294-305] PubMed: 30771469
Olanzapine induced autophagy through suppression of NF-κB activation in human glioma cells [ CNS Neurosci Ther, 2019, 10.1111/cns.13127] PubMed: 30955240
Quetiapine induces myocardial necroptotic cell death through bidirectional regulation of cannabinoid receptors. [ Toxicol Lett, 2019, 313:77-90] PubMed: 31220554
Second generation atypical antipsychotics olanzapine and aripiprazole reduce expression and secretion of inflammatory cytokines in human immune cells [Stapel B, et al. J Psychiatr Res, 2018, 105:95-102] PubMed: 30216787
Automated analysis of lipid drug-response markers by combined fast and high-resolution whole cell MALDI mass spectrometry biotyping [Weigt D, et al. Sci Rep, 2018, 8(1):11260] PubMed: 30050068

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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