Olanzapine

製品コードS2493 バッチS249303

印刷

化学情報

Chemical Structure 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 15 mg/mL (48.0 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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. This compound 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] This compound 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] It 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. This chemical also increases extracellular levels of a DA metabolite, DOPAC, and tissue concentrations of a released DA metabolite, 3-methoxytyramine. [3] It results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. [4] This agent results in substantial increases in adiposity: increased total body fat reflecting marked increases in subcutaneous and visceral adipose stores. It results in marked hepatic insulin resistance. [5]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/9265914/
  • https://pubmed.ncbi.nlm.nih.gov/10942849/
  • https://pubmed.ncbi.nlm.nih.gov/9551772/
  • https://pubmed.ncbi.nlm.nih.gov/15756305/
  • https://pubmed.ncbi.nlm.nih.gov/15734866/

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：

Dysregulated oxidative stress and lactate levels in treatment-resistant schizophrenia [ Brain Behav Immun, 2025, 130:106111] PubMed: 40962035
Dysregulated fatty acid metabolism in pericardiac adipose tissue of pulmonary hypertension due to left heart disease mice [ FASEB J, 2025, 39(3):e70355] PubMed: 39932146
Olanzapine suppresses mPFC activity-norepinephrine releasing to alleviate CLOCK-enhanced cancer stemness under chronic stress [ Cell Commun Signal, 2024, 22(1):375] PubMed: 39054537
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

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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