Olanzapine
(Synonyms: 奥氮平; LY170053) 目录号 : GC12495
An atypical antipsychotic
Cas No.:132539-06-1
Sample solution is provided at 25 µL, 10mM.
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Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
The 5-HT2 serotonin and D2 dopamine receptor s are subfamily of G protein-coupled receptors(GPCRs) [1].
In vitro: Binding studies showed that olanzapine interacted with keyreceptorsof interest in schizophrenia, exihibiting a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors [1].
In vivo: Olanzapine was a potent antagonist at DAreceptorsand 5-HT receptors, but showed weaker activity at alpha-adrenergic and muscarinic receptors [1].Administration of Olanzapine at 0.5, 3 and 10 mg/kg (s.c.) increased the extracellulardopamine(DA) and norepinephrine (NE) levels in all three brain areas in a dose-dependent manner.The increases reached peaks 60-90 min after olanzapine administration and lasted for at least 2 h. The highest DA increases in the Acb and Cpu were induced by olanzapine at 3 mg/kg but at 10 mg/kg in the Pfc while the highest NE increase in the Pfc (414% ± 40) induced by 10 mg/kg olanzapine [2].In macaque monkeys, olanzapine treatment resulted in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes [3].
References:
[1]. Bymaster FP1,Rasmussen K,Calligaro DO,Nelson DL,DeLapp NW,Wong DT,Moore NA. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug.J Clin Psychiatry.1997;58Suppl 10:28-36.
[2]. Li XM1,Perry KW,Wong DT,Bymaster FP. Olanzapine increases in vivodopamineand norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum.Psychopharmacology (Berl).1998 Mar;136(2):153-61.
[3]. Dorph-Petersen KA1,Pierri JN,Perel JM,Sun Z,Sampson AR,Lewis DA. The influence of chronic exposure to antipsychotic medications on brain size before and after tissue fixation: a comparison of haloperidol and olanzapine in macaque monkeys.Neuropsychopharmacology.2005 Sep;30(9):1649-61.
| Cell experiment [1]: | |
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Cell lines |
U87MG and A172 human glioblastoma cell line |
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Preparation method |
The solubility of this compound in DMSO is >15.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
IC50: 20–50 μM, 24 h |
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Applications |
Treatment with olanzapine inhibited the proliferation of established glioblastoma cell lines and enhanced the antiproliferative effect of temozolomide on U87MG and A172 cells. Olanzapine (20 μM, 40 μM) inhibited anchorage-independent growth of U87MG cells. Treatment with olanzapine (50 μM, 100 μM) inhibited the migration of A172MG cells. Olanzapine (144 h) exerted proapoptotic and necrotizing effects on glioblastoma cell lines. Olanzapine yielded a significant cytostatic effect on A172 glioblastoma cells. |
| Animal experiment [2]: | |
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Animal models |
Rats |
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Dosage form |
Subcutaneous injection; 0.5 mg/kg, 3 mg/kg and 10 mg/kg |
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Application |
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. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Karpel-Massler G, Kast R E, Westhoff M A, et al. Olanzapine inhibits proliferation, migration and anchorage-independent growth in human glioblastoma cell lines and enhances temozolomide’s antiproliferative effect[J]. Journal of neuro-oncology, 2015, 122(1): 21-33. [2]. Li X M, Perry K W, Wong D T, et al. Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum[J]. Psychopharmacology, 1998, 136(2): 153-161. |
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| Cas No. | 132539-06-1 | SDF | |
| 别名 | 奥氮平; LY170053 | ||
| 化学名 | 2-methyl-4-(4-methylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine | ||
| Canonical SMILES | CC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C | ||
| 分子式 | C17H20N4S | 分子量 | 312.43 |
| 溶解度 | ≥ 15.6mg/mL in DMSO | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2007 mL | 16.0036 mL | 32.0072 mL |
| 5 mM | 0.6401 mL | 3.2007 mL | 6.4014 mL |
| 10 mM | 0.3201 mL | 1.6004 mL | 3.2007 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet