阿替美唑 /Atipamezole
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货号：A316493
同义名：
MPV 1248;Antisedan
Atipamezole 是一种合成的竞争性 α2 肾上腺能受体拮抗剂，Ki 值为 1.6 nM。
Atipamezole 化学结构
Atipamezole 3D分子结构
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Atipamezole 纯度/质量文件 产品仅供科研
货号：A316493
标准纯度：
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产品说明书
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Atipamezole 质控信息
Ivabradine HCl
✔
98%
Maprotiline hydrochloride
✔
98%
Cisatracurium besylate
✔
96%
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
+++
α1A-adrenergic receptor, Ki: 3.7 nM
α1D-adrenergic receptor, Ki: 20 nM
98%
Naftopidil 2HCl
+
α1-adrenergic receptor, IC50: 0.2 μM
99%
Alfuzosin HCl
✔
98%
Terazosin HCl
✔
99%
Atipamezole
✔
95%
Phentolamine methanesulfonate salt
✔
99%
Doxazosin mesylate
✔
99%
Tolazoline HCl
✔
98%
Zenidolol hydrochloride
++++
β1-adrenergic receptor, Ki: 611nM
β2-adrenergic receptor, Ki: 0.7nM
98%
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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
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] [4] [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.
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Atipamezole 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
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
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