Olanzapine (LY170053) 是一种选择性的、具有口服活性的单胺能拮抗剂，高亲和力结合 5-羟色胺H1，5HT2A/2C，5HT3，5HT6(Ki分别为 7、4、11、57 和 5 nM)，多巴胺D1-4(Ki=11-31 nM)，毒蕈碱M1-5(Ki=1.9-25 nM) 和肾上腺素α1受体 (Ki=19 nM)。Olanzapine 是一种非典型的抗精神病剂。
| 生物活性 | Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding toserotonin H1, 5HT2A/2C, 5HT3, 5HT6(Ki=7, 4, 11, 57, and 5 nM, respectively),dopamine D1-4(Ki=11 to 31 nM),muscarinic M1-5(Ki=1.9-25 nM), andadrenergic α1 receptor(Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2]. |
| IC50& Target[1] | 5-HT2AReceptor 4 nM (Ki) | 5-HT1Receptor 7 nM (Ki) | 5-HT6Receptor 5 nM (Ki) | 5-HT2CReceptor 11 nM (Ki) | 5-HT3Receptor 57 nM (Ki) | Adrenergic α1 Receptor 19 nM (Ki) | Muscarinic M1-5 Receptor 1.9-25 nM (Ki) | Dopamine Receptor | Mitophagy | Apoptosis |
|
体外研究
(In Vitro) | Olanzapine binds weakly to GABAA, Benzodiazepine (BZD), and β-adrenergic receptors (Ki>10 μM)[1][2].
Olanzapine induces autophagy in human SH-SY5Y neuronal cell line[3].
Olanzapine (1-100 μM for 144 h under serum starvation) results in a marked anti-proliferative effect in glioblastoma cell lines as well as glioma stem-like cells[4].
Olanzapine also enhances Temozolomide’s anti-tumor activity in glioblastoma cell lines[4].
Olanzapine induces apoptosis and necrosis in glioblastoma cell lines[4].
Cell Proliferation Assay[4] | Cell Line: | U87MG and A172 glioblastoma cell lines as well as SC38 and SC40 glioma stem-like cells | | Concentration: | 1, 10, 100 μM | | Incubation Time: | 144 h; under serum starvation (1.5 % FBS) prior to performing MTT-assays | | Result: | Resulted in a marked antiproliferative effect with IC50values ranging from 25 to 79.9 μM. In U87MG cells, anchorage-independent growth was dose-dependently inhibited. In A172 cells, migration was also shown to be inhibited in a dose-dependent manner. |
Western Blot Analysis[4] | Cell Line: | U87MG and A172 cells | | Concentration: | 10, 25, 50, and 100 μM | | Incubation Time: | 7 h, 24 h, 48 h, 72 h | | Result: | Led to a dose responsive decrease of pAMPK expression after 72 h of treatment. |
|
体内研究
(In Vivo) | Olanzapine (0.75, 1.5 and 3 mg/kg) evaluates body weight and periuterine fat mass, as well as insulin, non-esterified fatty acids, triglycerides, and glucose levels in mice[5]
| Animal Model: | Forty-two, 14, and 28 female CD-1 mice[5] | | Dosage: | 0.75, 1.5 and 3 mg/kg | | Administration: | Orally and chronically administered; 35 days | | Result: | Increased body weight relative to vehicle on days 20-22, and from day 32 onwards there was a straightforward increase in body weight at 3 mg/kg.
No differences were found between control and mice administered olanzapine at both 1.5 and 0.75 mg/kg. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 20 mg/mL(64.01 mM;Need ultrasonic) 配制储备液 | 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 |
*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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (6.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (6.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2 mg/mL (6.40 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (6.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com