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Synonyms | LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H20N4S |
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分子量 | 312.43975 | CAS No. | 132539-06-1 | |
Solubility (25°C)* | 体外 | DMSO | 62 mg/mL (198.43 mM) | |
Ethanol | 9 mg/mL (28.8 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. |
製品説明 | Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. |
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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] |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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