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CAS No.: 68377-92-4

Arotinolol/阿罗洛尔 Catalog No. CSN10338

Synonyms: Almarl;阿罗洛尔

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.

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技术信息

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]. On the beta3-receptor, arotinolol was a very weak (EC50 approximately 20 mM) and only partial (approximately 50%) agonist, but arotinolol also demonstrated the properties of being a beta3-receptor antagonist with a pK(B) of 5.7^[4].
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 ... more >> Nan Chen Shanghai, Shanghai, China, 200025 Collapse <<
NCT02612298	Essential Hypertension	Phase 4	Unknown	December 2018	China ... more >> China PLA General Hospital Recruiting Beijing, China, 100039 Contact: Yundai Chen, MD Contact: Yundai Chen, MD +86 010 55499209 cyundai@medmail.com.cn Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6915 mL
- 13.4575 mL
- 26.9149 mL
- 5 mM
- 0.5383 mL
- 2.6915 mL
- 5.3830 mL
- 10 mM
- 0.2691 mL
- 1.3457 mL
- 2.6915 mL

技术信息

CAS号

68377-92-4

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H21N3O2S3

运输

蓝冰

分子量

371.54

别名

Almarl;阿罗洛尔

溶解度

DMSO	240.0 mg/mL (646.0 mM) warming

动物实验配方

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