阿罗洛尔 /Arotinolol
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货号：A127295
Arotinolol is a blocker of both α- and β-receptor, and also acts as a β3 receptor agonist. It is used in the treatment of high blood pressure and essential tremor.
Arotinolol 化学结构
Arotinolol 3D分子结构
规格
价格
会员价
库存
数量
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Arotinolol 质控信息
Ivabradine HCl
✔
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Maprotiline hydrochloride
✔
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Cisatracurium besylate
✔
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Yohimbine HCI
✔
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BMY 7378
++
α2C-adrenoceptor, pKi: 6.54
α1D-adrenoceptor, pKi: 5.1
+
β1-adrenoceptor, pIC50: 5.1
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Asenapine maleate
++++
α2B-adrenergic receptor, pKi: 8.9
α2A-adrenergic receptor, pKi: 8.9
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Piribedil
++
adrenoceptor α2C, pKi: 7.2
adrenoceptor α2A, pKi: 7.1
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Prazosin HCl
✔
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Silodosin
✔
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Phenoxybenzamine HCl
✔
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Naftopidil
+++
α1D-adrenergic receptor, Ki: 20 nM
α1A-adrenergic receptor, Ki: 3.7 nM
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Naftopidil 2HCl
+
α1-adrenergic receptor, IC50: 0.2 μM
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Alfuzosin HCl
✔
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Terazosin HCl
✔
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Atipamezole
✔
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Phentolamine methanesulfonate salt
✔
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Doxazosin mesylate
✔
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Tolazoline HCl
✔
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Zenidolol hydrochloride
++++
β2-adrenergic receptor, Ki: 0.7nM
β1-adrenergic receptor, Ki: 611nM
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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。
Arotinolol 生物活性
描述
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol(30 mg/kg/d) relaxed vascular rings and the relaxations were attenuated by Nω-nitro-L-arginine methyl ester (L-NAME, NO synthase inhibitor) and the absence of endothelium[3] [4]
Arotinolol 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
NCT01351636
Chronic Kidney Disease
Phase 4
Unknown
September 2018
China, Shanghai
... 展开 >>
Nan Chen
Shanghai, Shanghai, China, 200025 收起 <<
NCT02612298
Essential Hypertension
Phase 4
Unknown
December 2018
China
... 展开 >> China PLA General Hospital
Recruiting
Beijing, China, 100039
Contact: Yundai Chen, MD
Contact: Yundai Chen, MD +86 010 55499209 cyundai@medmail.com.cn 收起 <<
Arotinolol 参考文献
[1] Qian Z, Xu Y, et al. Enantiospecific determination of arotinolol in rat plasma by LC-MS/MS: application to a stereoselective pharmacokinetic study. J Pharm Biomed Anal. 2015 Jan;102:299-304.
[2] Sakanashi M, Miyamoto Y, et al. Effects of a new beta-adrenoceptor blocking agent, S-596 (arotinolol), on isolated dog coronary arteries. Arch Int Pharmacodyn Ther. 1983 Jun;263(2):208-16.
[3] Zhou W, Hong M, Zhang K, Chen D, Han W, Shen W, Zhu D, Gao P. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats. PLoS One. 2014 Feb 12;9(2):e88722.
[4] Zhao J, Golozoubova V, Cannon B, Nedergaard J. Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes. Can J Physiol Pharmacol. 2001 Jul;79(7):585-93. PMID: 11478592.
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Arotinolol 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
2.69mL
0.54mL
0.27mL
13.46mL
2.69mL
1.35mL
26.91mL
5.38mL
2.69mL
Arotinolol 技术信息
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