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Arotinolol

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Chemical Structure| 68377-92-4 同义名 : -
CAS号 : 68377-92-4
货号 : A127295
分子式 : C15H21N3O2S3
纯度 : 95%
分子量 : 371.541
MDL号 : MFCD00865895
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(322.98 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
动物实验配方：
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 ... 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 <<
实验方案
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
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.