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阿扎佩隆 /Azaperone {[allProObj[0].p_purity_real_show]}

货号:A101450 同义名: 阿扎哌隆 / R-1929;Fluoperidol

Azaperone作为一种多巴胺拮抗剂,能够与D1和D2受体结合。它具有抗组胺和抗胆碱能的特性。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Azaperone 化学结构 CAS号:1649-18-9
Azaperone 化学结构
CAS号:1649-18-9
Azaperone 3D分子结构
CAS号:1649-18-9
Azaperone 化学结构 CAS号:1649-18-9
Azaperone 3D分子结构 CAS号:1649-18-9
规格 价格 会员价 库存 数量
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Azaperone 纯度/质量文件 产品仅供科研

货号:A101450 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

99%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 98% (HPLC)
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 99%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

99%
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 99%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 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

99%
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。

Azaperone 生物活性

靶点
  • Dopamine receptor

描述 Administration of azaperone at weaning had a profound effect on preovulatory LH secretion as well as growth kinetics and estrogenicity of ovarian antral follicles[3]. Thiafentanil and azaperone, with or without etorphine, delivered rapid safe, effective, reversible field anaesthesia in healthy swamp buffalo[4]. Using azaperone alone the duration of immobility was 1.9 to 10.8 hours for mice and 0.9 to 2.4 hours for rats. The withdrawal reflex was not eliminated from mice receiving azaperone alone; however, the withdrawal reflex was eliminated from 0.9 to 2.4 hours in rats receiving azaperone. Azaperone produced a tachypnea in rats and male mice while a depressed respiratory rate was observed in female mice. Overall, azaperone alone was shown to provide sedation in mice as compared to a dose dependent anesthesia in rats. Azaperone and the azaperone-ketamine combination appear to be a suitable alternative to sedatives and anesthetics currently used in rats and mice[5].

Azaperone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01486615 Anxiety Phase 4 Completed - Nepal ... 展开 >> B. P. Koirala Institute of Health Sciences Dharan, Koshi, Nepal, 56700 Dr Krishna Pokharel Dharan, Koshi, Nepal, 56700 收起 <<
NCT01486615 - Completed - -

Azaperone 参考文献

[1]Lahrmann KH, Baars J, et al. [Perioperative intensive-medical investigations regarding compatibility of the ketamine-azaperone-general anesthesia in pigs] . Berl Munch Tierarztl Wochenschr. 2014 Jan-Feb;127(1-2):3-11.

[2]Bettschart-Wolfensberger R, Stauffer S, et al. Racemic ketamine in comparison to S-ketamine in combination with azaperone and butorphanol for castration of pigs. Schweiz Arch Tierheilkd. 2013 Dec;155(12):669-75.

[3]Schwarz T, Zięcik A, Murawski M, et al. The influence of azaperone treatment at weaning on reproductive function in sows: ovarian activity and endocrine profiles during the weaning-to-ovulation interval. Animal. 2018;12(10):2089‐2097

[4]Bryant B, Pittard S, Jordan NR, McMahon CR. Chemical capture of wild swamp buffalo (Bubalus bubalis) in tropical northern Australia using thiafentanil, etorphine and azaperone combinations. Aust Vet J. 2019;97(1-2):33‐38

[5]Olson ME, Renchko P. Azaperone and azaperone-ketamine as a neuroleptic sedative and anesthetic in rats and mice. Lab Anim Sci. 1988;38(3):299‐304

Azaperone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.31mL

15.27mL

3.05mL

1.53mL

30.54mL

6.11mL

3.05mL

Azaperone 技术信息

CAS号1649-18-9
分子式C19H22FN3O
分子量 327.396
别名 阿扎哌隆 ;R-1929;Fluoperidol;Eucalmyl;Suicalm;Azaperon;Stresnil;NSC 170976
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 50 mg/mL(152.72 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 62 mg/mL suspension

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