Olanzapine
(Synonyms: 奥氮平; LY170053) 目录号 : GC12495
Olanzapine是一种单胺拮抗剂。
Cas No.:132539-06-1
Sample solution is provided at 25 µL, 10mM.
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Olanzapine is a monoamine antagonist [1]. Olanzapine inhibits 5-hydroxytryptamine 2A (5-HT2A) receptors with high affinity and antagonizes dopamine D2 receptors, thereby alleviating symptoms in patients with schizophrenia and bipolar disorder [2-3]. Olanzapine is commonly used to treat acute mania in schizophrenia and bipolar I disorder [4].
In PC12 cells, Olanzapine (100μM; 24h) pretreatment attenuated the decrease in cell viability induced by hydrogen peroxide [5]. In U87 cells, Olanzapine (0-400µM; 24-72h) inhibits tumor cell growth and induces autophagy [6].
In C57BL/6J mice, Olanzapine (6mg/kg; ig; 7 weeks) treatment increased mice food intake and body weight [7]. In Swiss–Kunming mice, Olanzapine (0.01-0.1mg/kg; sc; single injection) treatment improves spatial learning function in the Morris water maze task in mice [8].
References:
[1]. Thomas K, Saadabadi A. Olanzapine[J]. 2018.
[2]. Zhang W, Bymaster F P. The in vivo effects of olanzapine and other antipsychotic agents on receptor occupancy and antagonism of dopamine D1, D2, D3, 5HT2A and muscarinic receptors[J]. Psychopharmacology, 1999, 141(3): 267-278.
[3]. Taraskina A E, Nasyrova R F, Zabotina A M, et al. Potential diagnostic markers of olanzapine efficiency for acute psychosis: a focus on peripheral biogenic amines[J]. BMC psychiatry, 2017, 17(1): 394.
[4]. McCormack P L, Wiseman L R. Olanzapine: a review of its use in the management of bipolar I disorder[J]. Drugs, 2004, 64(23): 2709-2726
[5]. Wei Z, Bai O, Richardson J S, et al. Olanzapine protects PC12 cells from oxidative stress induced by hydrogen peroxide[J]. Journal of neuroscience research, 2003, 73(3): 364-368.
[6]. Zhu Y, Zhao Y F, Liu R S, et al. Olanzapine induced autophagy through suppression of NF‐κB activation in human glioma cells[J]. CNS Neuroscience & Therapeutics, 2019, 25(9): 911-921.
[7]. Hou P H, Chang G R, Chen C P, et al. Long-term administration of olanzapine induces adiposity and increases hepatic fatty acid desaturation protein in female C57BL/6J mice[J]. Iranian Journal of Basic Medical Sciences, 2018, 21(5): 495.
[8]. Hou Y, Wu C F, Yang J Y, et al. Differential effects of haloperidol, clozapine and olanzapine on learning and memory functions in mice[J]. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2006, 30(8): 1486-1495.
Olanzapine是一种单胺拮抗剂 [1]。Olanzapine以高亲和力抑制5-羟色胺2A（5-HT2A）受体，并拮抗多巴胺D2受体，从而缓解精神分裂症和双相情感障碍患者的症状 [2-3]。Olanzapine常用于治疗精神分裂症和I型双相情感障碍的急性躁狂症 [4]。
在PC12细胞中，Olanzapine（100μM；24h）预处理可减轻过氧化氢诱导的细胞活力下降 [5]。在U87细胞中，Olanzapine（0-400μM；24-72h）可抑制肿瘤细胞生长并诱导自噬 [6]。
在C57BL/6J小鼠中，Olanzapine（6mg/kg；ig；7周）治疗可增加小鼠的食物摄入量和体重 [7]。在瑞士昆明小鼠中，Olanzapine（0.01-0.1mg/kg；sc；单次注射）治疗可改善小鼠在Morris水迷宫任务中的空间学习功能 [8]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | After exposure to olanzapine (0 or 100μM) for 24h, and hydrogen peroxide (0 or 100μM) for 1h, cells were examined with the Annexin-V-Fluos Staining Kit, a histological procedure that differentially labels necrotic cells versus cells undergoing apoptosis. |
Reaction Conditions | 100μM; 24h |
Applications | Olanzapine pretreatment attenuated the decrease in cell viability induced by hydrogen peroxide in PC12 cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | C57BL/6J mice placed in standard rodent cages stored in quarters controlled at 22℃, were subjected to a 12-hr light–dark cycle. The mice were randomly categorized into two groups: The first group received 6mg/kg olanzapine per day through gavage for 7 weeks, and the second group (i.e., the control group) was administered 0.01mL/g normal saline once per day through gavage. |
Dosage form | 6mg/kg; ig; 7 weeks |
Applications | Olanzapine treatment increased food intake and body weight in mice. |
References: | |
| 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