Loxapine succinate | 丁二酸洛沙平 | CL 71,563 | Dopamine/5-HT Receptor Inhibitor

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琥珀酸洛沙平 /Loxapine succinate {[allProObj[0].p_purity_real_show]}

货号：A945672 同义名： 丁二酸洛沙平 / CL 71,563;Loxapine (succinate)

Loxapine succinate salt is an multiple-target antagonist of both D2/D4 dopamine receptor and 5-HT2A/2B, 5-H7 serotonin receptor, used as an antipsychotic agent.

Loxapine succinate 化学结构
CAS号：27833-64-3

Loxapine succinate 3D分子结构
CAS号：27833-64-3

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Loxapine succinate 纯度/质量文件产品仅供科研

货号：A945672 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。

Loxapine succinate 生物活性

靶点

5-HT2

5-HT2 (bovine), Ki:6.6 nM

5-HT2 (human), Ki:6.8 nM
D4 receptor

D4 receptor (human), Ki:7.5 nM
D1 receptor

D1 receptor (human), Ki:26 nM

D2 receptor (Human), Ki:62 nM
D2 receptor

D2 receptor (bovine), Ki:26 nM

D2 receptor (human), Ki:24 nM

描述

Loxapine succinate, the succinate form of loxapine, is a kind of typical antipsychotic. In vitro studies, it was found that loxapine succinate showed high affinity for the human recombinant D2 receptor, intermediate affinity for the D1, D4, D5 and 5-HT2C receptors, and low affinity toward D3, 5-HT1A, 5-HT4, 5-HT6 and 5-HT7 receptors in transfected CHO cells and HEK-293 cells, which demonstrated that loxapine should be rightly classified as a DS-RAn agent in the neuroscience based nomenclature classification^[3]. Besides this, loxapine could inhibit the sodium-potassium ATPase activity by 25-35% at 0.1mM in rat brain^[4]. In vivo studies, loxapine could contribute to the significant depression of the paradoxical sleep (PS) with maximal within 30min and lasting about 24hr in Wistar albino rats, while only slightly influence the synchronized sleep, when given 0.4–1.6mg/kg in one single dose. In addition, loxapine could also affect the frequency and mean duration of PS episodes^[5].

Loxapine succinate 参考文献

[1]Labuzek K, Kowalski J, et al. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures. Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30.

[2]Singh AN, Barlas C, et al. A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes. J Psychiatry Neurosci. 1996 Jan;21(1):29-35.

[3]Ferreri F, Drapier D, Baloche E, Ouzid M, Zimmer L, Llorca PM. The in Vitro Actions of Loxapine on Dopaminergic and Serotonergic Receptors. Time to Consider Atypical Classification of This Antipsychotic Drug? Int J Neuropsychopharmacol. 2018 Apr 1;21(4):355-360. doi: 10.1093/ijnp/pyx102. PMID: 29106549; PMCID: PMC5887516.

[4]Velasco-Martín A, Garcia JL, Dueñas A. Effects of several neuroleptics, antidepressants and monoamine uptake blockers on ATPase activity and related oxygen uptake in rat brain in vitro. Methods Find Exp Clin Pharmacol. 1989 Dec;11(12):737-41. PMID: 2576298.

[5]Schmidek WR, Timo-Iaria C, Schmidek M, Krakowiak M, Delmutti EE, Alves MR. Influence of loxapine on the sleep-wakefulness cycle of the rat. Pharmacol Biochem Behav. 1974 Nov-Dec;2(6):747-51. doi: 10.1016/0091-3057(74)90105-1. PMID: 4377026.

Loxapine succinate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.21mL

2.24mL

1.12mL

22.43mL

4.49mL

2.24mL

Loxapine succinate 技术信息

CAS号	27833-64-3
分子式	C₂₂H₂₄ClN₃O₅
分子量	445.896

别名	丁二酸洛沙平 ;CL 71,563;Loxapine (succinate);Succinate, Loxapine;Oxilapine;Maleate, Loxipine;Daxolin;Cloxazepin;Loxapac;Loxapine succinate salt;NSC 759578
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,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(235.48 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

H₂O: 2.5 mg/mL(5.61 mM)，配合低频超声，并水浴加热至45℃助溶

动物实验配方

琥珀酸洛沙平 /Loxapine succinate {[allProObj[0].p_purity_real_show]}

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5-HT2	5-HT2 (bovine), Ki:6.6 nM 5-HT2 (human), Ki:6.8 nM
D4 receptor	D4 receptor (human), Ki:7.5 nM
D1 receptor	D1 receptor (human), Ki:26 nM D2 receptor (Human), Ki:62 nM
D2 receptor	D2 receptor (bovine), Ki:26 nM D2 receptor (human), Ki:24 nM

琥珀酸洛沙平 /Loxapine succinate {[allProObj[0].p_purity_real_show]}

Loxapine succinate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Loxapine succinate 质控信息

Loxapine succinate 生物活性

Loxapine succinate 参考文献

Loxapine succinate 实验方案

Loxapine succinate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Loxapine succinate 纯度/质量文件产品仅供科研