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Olanzapine

现货
Catalog No.
B2240
5-HT2A和多巴胺D2受体的拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
1g
¥ 760.00
现货
5g
¥ 2,620.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt312.43
Cas No.132539-06-1
FormulaC17H20N4S
Solubility≥15.6mg/mL in DMSO
Chemical Name2-methyl-4-(4-methylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine
SDFDownload SDF
Canonical SMILESCC1=CC2=C(NC3=CC=CC=C3N=C2S1)N4CCN(CC4)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

U87MG和A172人胶质母细胞瘤细胞系

溶解方法

该化合物在DMSO中的溶解度大于15.6 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

给药剂量

IC50: 20–50 μM, 24 h

应用

Olanzapine抑制胶质母细胞瘤细胞系的增殖,提高temozolomide对U87MG和A172细胞的抗增殖作用。Olanzapine(20 μM及40 μM)抑制U87MG细胞的锚定非依赖性生长。Olanzapine(50 μM、100 μM)抑制A172MG细胞的迁移。Olanzapine(144小时)对胶质母细胞瘤细胞系具有促凋亡和坏死作用。Olanzapine对A172胶质母细胞瘤细胞产生显著的细胞抑制作用。

动物实验 [2]:

动物模型

大鼠

给药剂量

皮下注射,0.5 mg/kg, 3 mg/kg和10 mg/kg

应用

皮下注射0.5 mg/kg、3 mg/kg和10 mg/kg的Olanzapine以剂量依赖性方式增加大鼠前额叶皮层、伏隔核和纹状体中的细胞外多巴胺(DA)和去甲肾上腺素(NE)水平。Olanzapine还增加DA代谢物DOPAC的细胞外水平以及释放的DA代谢物3-甲氧基酪氨酸的组织浓度。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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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