Betaxolol HCl

产品说明书

Print
Chemical Structure| 63659-19-8 同义名 : SL75212; Betaxolol (hydrochloride); ALO 140102; Kerlon; Betoptic; Kerlone; Betoptima; SL 75212 HCl; Betaxolol hydrochloride
CAS号 : 63659-19-8
货号 : A461855
分子式 : C18H30ClNO3
纯度 : 97%
分子量 : 343.89
MDL号 : MFCD00242959
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(305.33 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

H2O: 10 mg/mL(29.08 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 50 mg/mL clear

生物活性
靶点

  • β-adrenergic receptor

    β1-adrenergic receptor, IC50:6 μM
描述 Betaxolol hydrochloride (BH) is a cardioselective betaadrenergic receptor blocking agent used in the treatment of hypertension and glaucoma[3]. Betaxolol inhibited specific [3H]-batrachotoxinin-A 20-α-benzoate ([3H]-BTX-B) binding to neurotoxin site 2 in a concentration-dependent manner with an IC50 value of 9.8 μM. Betaxolol inhibited veratridine-stimulated Na+ influx in rat cortical synaptosomes with an IC50 value of 28.3 μM[4]. Moreover, the anxiolytic-like effect of betaxolol on cocaine-induced anxiety may be related to its effect on amygdalar beta(1)-adrenergic receptors that are up-regulated during early phases of drug withdrawal[5].
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
NCT01316952 - Completed - -
NCT02617459 Primary Open-angle Glaucoma ... 展开 >> Ocular Hypertension 收起 << Phase 3 Unknown November 2016 China, Guangdong ... 展开 >> Zhongshan ophthalmic center, Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Jian Ge, MD    0+86-20-87330000       Principal Investigator: Jian Ge, MD 收起 <<
NCT00000132 Open-Angle Glaucoma Phase 3 Unknown - Sweden ... 展开 >> Department of Ophthalmology, Helsingborg Hospital Helsingborg, Sweden Department of Ophthalmology, Malmo University Hospital, University of Lund Malmo, Sweden 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.54mL

2.91mL

1.45mL

29.08mL

5.82mL

2.91mL
参考文献

[1]Wood JP, Schmidt KG, et al. The beta-adrenoceptor antagonists metipranolol and timolol are retinal neuroprotectants: comparison with betaxolol. Exp Eye Res. 2003 Apr;76(4):505-16.

[2]Tang LQ, Hong PH, et al. Effect of beta-adrenergic agents on intracellular potential of rabbit ciliary epithelium. Curr Eye Res. 1998 Jan;17(1):24-30.

[3]Auvity, S., Chiadmi, F., Cisternino, S., et al. A Rapid Stability-Indicating RP-HPLC Method for the Determination of Betaxolol Hydrochloride in Pharmaceutical Tablets. Anal Chem Insight. 2013; 8: 1-7.

[4]Chidlow, G., Melena, J., Osborne, NN. Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists. Br J Pharmacol. 2000 Jum; 130(4):759-66.

[5]Rudoy, CA., Bockstaele, EJV. Betaxolol, a selective beta(1)-adrenergic receptor antagonist, diminishes anxiety-like behavior during early withdrawal from chronic cocaine administration in rats. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Jun 30; 31(5): 1119-29.