Olanzapine

製品コードS2493 バッチS249304

印刷

化学情報

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

化学式

C₁₇H₂₀N₄S

分子量

312.43975

CAS No.

132539-06-1

Solubility (25°C)*

体外

DMSO

62 mg/mL (198.43 mM)

Ethanol

7 mg/mL (22.4 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

1.5mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

参考

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カスタマーフィードバック

: 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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。