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阿替美唑 /Atipamezole {[allProObj[0].p_purity_real_show]}

货号:A316493 同义名: MPV 1248;Antisedan

Atipamezole is a synthetic competitive α2 adrenergic receptor antagonist with Ki value of 1.6 nM.

Atipamezole 化学结构 CAS号:104054-27-5
Atipamezole 化学结构
CAS号:104054-27-5
Atipamezole 3D分子结构
CAS号:104054-27-5
Atipamezole 化学结构 CAS号:104054-27-5
Atipamezole 3D分子结构 CAS号:104054-27-5
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Atipamezole 纯度/质量文件 产品仅供科研

货号:A316493 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline hydrochloride 98%
Cisatracurium besylate 98%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

97%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Doxazosin mesylate 98%
Tolazoline HCl 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

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。

Atipamezole 生物活性

靶点
  • α-adrenergic receptor

描述 Atipamezole is an alpha2-adrenoceptor antagonist with an imidazole structure. It rapidly reverses sedation/anesthesia induced by alpha2-adrenoceptor agonists. In animals with sustained nociception, atipamezole increased pain-related responses by blocking the noradrenergic feedback inhibition of pain[3]. Atipamezole has inhibition to CYP2C9 mediated diclofenac hydroxylation in human and animal liver microsomes with IC50 values of 1.50-5.20 μM[4]. Animals receiving atipamezole (1 mg/kg, s.c.) without rehabilitation exhibited a significant motor improvement in the ladder rung walk test, but not the forelimb reaching test[5].

Atipamezole 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
NCT01435213 Healthy Phase 1 Completed - Finland ... 展开 >> University of Turku, Clinical Research Services Turku CRST Turku, Finland, 20520 University of Turku, Turku PET Centre Turku, Finland, 20520 收起 <<

Atipamezole 参考文献

[1]Pertovaara A, Haapalinna A, et al. Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.

[2]Sirvio J, Riekkinen P Jr, et al. The effects of alpha-2 adrenoceptor antagonist, atipamezole, on spatial learning in scopolamine-treated and aged rats. J Neural Transm Park Dis Dement Sect. 1992;4(2):99-106.

[3]Pertovaara A, Haapalinna A, Sirviö J, Virtanen R. Pharmacological properties, central nervous system effects, and potential therapeutic applications of atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.

[4]Li Z, Zhang Y, Gao Y, Xiang Y, Zhang W, Lu C, Zhuang X. Atipamezole is a promising non-discriminative inhibitor against pan-CYP450 including diclofenac 4'-hydroxylation: A comparison with ABT for drug ADME optimization and mechanism study. Eur J Pharm Sci. 2019 Mar 15;130:156-165.

[5]Beltran EJ, Papadopoulos CM, Tsai SY, Kartje GL, Wolf WA. Long-term motor improvement after stroke is enhanced by short-term treatment with the alpha-2 antagonist, atipamezole. Brain Res. 2010 Jul 30;1346:174-82.

Atipamezole 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.71mL

0.94mL

0.47mL

23.55mL

4.71mL

2.36mL

47.11mL

9.42mL

4.71mL

Atipamezole 技术信息

CAS号104054-27-5
分子式C14H16N2
分子量 212.29
别名 MPV 1248;Antisedan
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 30 mg/mL(141.32 mM),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

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 11 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

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