Olanzapine | LY170053 | 5-HT2/D1/D2 Antagonist | AmBeed-信号通路专用抑制剂

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奥氮平 /Olanzapine {[allProObj[0].p_purity_real_show]}

货号：A158972 同义名： LY170053

Olanzapine is a multiple-target antagonist for 5-HT2A receptors and D2 dopamine receptors, as well as muscarinic M3 receptor.

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Olanzapine 化学结构
CAS号：132539-06-1

Olanzapine 3D分子结构
CAS号：132539-06-1

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Olanzapine 纯度/质量文件产品仅供科研

货号：A158972 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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5-羟色胺受体亚型比较
多巴胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM								98%
Venlafaxine	✔								98%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								98%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	98%
Fluoxetine HCl	✔								99.5%
Paroxetine hydrochloride	✔							AChR	97%
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						98% HPLC
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 nM						99%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
Asenapine maleate		+++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		97%
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	D1 receptor ↓ ↑	D2 receptor ↓ ↑	D3 receptor ↓ ↑	D4 receptor ↓ ↑	D5 receptor ↓ ↑	DAT ↓ ↑	Dopamine receptor ↓ ↑	其他靶点	纯度
Penfluridol	+ Dopamine receptor, Ki: 1.6 μM								98%
Ansofaxine HCl	++ Dopamine receptor, IC50: 491 nM								98%
Tetrahydroberberine,THB		+ D2 receptor, pKi: 6.08							98+%
Prochlorperazine Maleate		✔							95%
Olanzapine		✔							99+%
Trifluoperazine		++++ Dopamine D2 receptor, IC50: 1.1 nM							98%
Ropinirole hydrochloride		++ D2 receptor, Ki: 29 nM							99%
Lurasidone		++++ D2 receptor, Ki: 1 nM							98%
Levosulpiride		✔							99+%
Pridopidine		✔							95%
Metoclopramide		✔					✔		99+%
Molindone HCl		✔							98%
Sulpiride		✔							99+%
Perospirone		++++ D2 receptor, Ki: 1.4 nM							99%
Perospirone HCl		++++ D2 receptor, Ki: 1.4 nM							98+%
Phenothiazine		✔							98%
Pimozide	+ Dopamine D1 receptor, Ki: 6600 nM	+++ Dopamine D2 receptor, Ki: 3.0 nM	++++ Dopamine D3 receptor, Ki: 0.83 nM						98%
Rotundine	++ D1 receptor, IC50: 166 nM	+ D2 receptor, IC50: 1.47 μM	+ D3 receptor, IC50: 3.25 μM						98%
Domperidone		✔							99+%
ONC206		✔							97%
Pimethixene maleate	++ Dopamine D1 Receptor, pKi: 6.37	+++ Dopamine D2 Receptor, pKi: 8.19		++ Dopamine D4.4 Receptor, pKi: 7.54					97%
Loxapine succinate	++ D1 receptor (human), Ki: 26 nM D2 receptor (Human), Ki: 62 nM	++ D2 receptor (bovine), Ki: 26 nM D2 receptor (human), Ki: 24 nM		+++ D4 receptor (human), Ki: 7.5 nM					99%
Chlorprothixene	+++ D1 receptor, Ki: 18 nM	+++ D2 receptor, Ki: 2.96 nM	+++ D3 receptor, Ki: 4.56 nM		+++ D5 receptor, Ki: 9 nM				98%
SCH-23390 HCl	++++ D1 dopamine receptor, Ki: 0.2 nM				++++ D5 dopamine receptor, Ki: 0.3 nM				98%
MPP+ iodide						✔			97%
σ1 Receptor antagonist-1						+ DAT, pKi: 5.8			97%
Benztropine mesylate						++ DAT, IC50: 118 nM			98%
Azaperone							✔		98%
Ziprasidone HCl							✔		98+%
Paliperidone							✔		98%
Alizapride HCl							✔		99+%
Amisulpride							✔		98%
Quetiapine hemifumarate							✔	Adrenergic Receptor	98%
Clozapine N-oxide							✔		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Olanzapine 生物活性

靶点

5-HT2
D2 receptor

描述

Olanzapine is a D2 dopamine receptor antagonist with a high affinity for 5-HT2 serotonin. In vivo, sequential doses of olanzapine at 0.5, 3 and 10 mg/kg dose-dependently increased the extracellular dopamine (DA) and norepinephrine (NE) levels in all three brain areas. The increases appeared 30 min after olanzapine administration, reached peaks around 60 - 90 min and lasted for at least 2 h^[3]. The high dose of olanzapine (10 mg/kg ) increased the number of fos-like positive nuclei in mesolimbic areas connected to the extended amygdala^[4]. In vitro, olanzapine interacted with keyreceptorsof interest in schizophrenia, exihibiting a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors^[5].

Olanzapine 参考文献

[1]Cipriani A, Rendell JM, et al. Olanzapine in long-term treatment for bipolar disorder. Cochrane Database Syst Rev. 2009 Jan 21;(1):CD004367.

[2]Bymaster FP, Rasmussen K, et al. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug. J Clin Psychiatry. 1997;58 Suppl 10:28-36.

[3]Li XM, Perry KW, Wong DT, Bymaster FP. Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum. Psychopharmacology (Berl). 1998;136(2):153-161.

[5]Bymaster FP, Rasmussen K, Calligaro DO, et al. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug. J Clin Psychiatry. 1997;58 Suppl 10:28-36.

Olanzapine 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.00mL

3.20mL

1.60mL

32.01mL

6.40mL

3.20mL

Olanzapine 技术信息

CAS号	132539-06-1
分子式	C₁₇H₂₀N₄S
分子量	312.433

别名	LY170053
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 18 mg/mL(57.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

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大规格询价

摩尔计算器

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