Levobunolol hydrochloride (l-Bunolol hydrochloride)
(Synonyms: 盐酸左布诺洛尔; l-Bunolol hydrochloride) 目录号 : GC30167
A β-adrenergic receptor antagonist
Cas No.:27912-14-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Levobunolol (hydrochloride) is a β-adrenergic antagonist that acts as a vasodilator and increases ocular circulation when applied in solution to the eye.1,2 Topical formulations containing levobunolol are used to manage glaucoma.1
1.Tierney, D.W.Betaxolol and levobunolol: New beta-blocking antiglaucoma agentsJ. Am. Optom. Assoc.58(9)722-727(1987) 2.Morsman, C.D., Bosem, M.E., Lusky, M., et al.The effect of topical beta-adrenoceptor blocking agents on pulsatile ocular blood flowEye (Lond)9(Pt 3)344-347(1995)
| Cas No. | 27912-14-7 | SDF | |
| 别名 | 盐酸左布诺洛尔; l-Bunolol hydrochloride | ||
| Canonical SMILES | O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C.[H]Cl | ||
| 分子式 | C17H26ClNO3 | 分子量 | 327.85 |
| 溶解度 | DMSO : ≥ 62.5 mg/mL (190.64 mM);Water : 50 mg/mL (152.51 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0502 mL | 15.2509 mL | 30.5018 mL |
| 5 mM | 0.61 mL | 3.0502 mL | 6.1004 mL |
| 10 mM | 0.305 mL | 1.5251 mL | 3.0502 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Bradyarrhythmias secondary to topical Levobunolol hydrochloride solution
Clin Interv Aging 2014 Oct 13;9:1741-5.25342892 PMC4206249
An 88-year-old man was admitted with fatigue, dizziness, and heart palpitations. Both the electrocardiogram and Holter confirmed the existence of sinus bradycardia and sinus arrest. One hour prior to the onset of symptoms, he received Levobunolol hydrochloride solution topically. The Levobunolol hydrochloride solution was discontinued and the bradycardia resolved. He was diagnosed as having intermittent sinus bradycardia and sinus arrest, induced by topical β-blocker therapy. Levobunolol hydrochloride solution is an effective therapy for ocular hypertension, probably by reducing aqueous fluid production. However, it can induce cardiac side effects such as bradyarrhythmia and should be used with caution in elderly patients or patients with cardiac disease.
A comparison of the efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution QD and 0.5% Levobunolol hydrochloride BID in patients with ocular hypertension or open-angle glaucoma
J Ocul Pharmacol Ther 2002 Apr;18(2):105-13.12002664 10.1089/108076802317373860
The purpose of this study was to compare the ocular hypotensive efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution (timolol gel) and 0.5% Levobunolol hydrochloride (levobunolol). This was a randomized, double-masked, multi-center, active-controlled, 2-period, crossover study. After a 3-week, single-masked placebo run-in phase, patients with ocular hypertension or open-angle glaucoma and an intraocular pressure (IOP) > or = 22 mmHg were randomized to receive timolol gel QD or levobunolol BID for 6 weeks followed by a 3-week, placebo washout period. Patients were then crossed over to the alternate treatment for 6 weeks. IOP and heart rate (HR) were measured at 3 and 6 weeks after the start of therapy with either timolol gel or levobunolol. Of 133 patients randomized, 116 received both treatments. Timolol gel QD was comparable to levobunolol BID in reducing trough and peak IOP. At trough, HR was marginally increased with timolol gel and was decreased with levobunolol (p = < 0.001). At peak, HR was decreased with both treatments, but the decrease was significantly less with timolol gel than with levobunolol (p = 0.049). Significantly more patients experienced at least one adverse event (p = 0.024), adverse events related to special senses (p = 0.002), and burning and stinging (p < 0.001) with levobunolol compared to timolol gel. The study demonstrates that timolol gel QD has IOP-lowering effects comparable to those of levobunolol BID with fewer adverse experiences and less effect on HR.
Efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution QD compared with 0.5% Levobunolol hydrochloride BID in patients with open-angle glaucoma or ocular hypertension
Clin Ther 1998 Nov-Dec;20(6):1170-8.9916610 10.1016/s0149-2918(98)80112-4
We compared the efficacy of timolol maleate ophthalmic gel-forming solution 0.5% QD with that of Levobunolol hydrochloride 0.5% BID, as measured by change in intraocular pressure (IOP), effect on heart rate, and ocular tolerability. The study had a positive-controlled, double-masked, randomized, multicenter, 12-week, two-period (6 weeks each), crossover design. One hundred fifty-two patients with open-angle glaucoma or ocular hypertension were randomized to receive either timolol maleate gel-forming solution QD or levobunolol BID for 6 weeks, followed by a crossover to the alternate treatment. IOP and heart rate were measured at morning trough and peak during weeks 3, 6, 9, and 12. Timolol maleate gel-forming solution QD was comparable to levobunolol BID in reducing IOP at peak and trough. Although the effects on peak heart rate were similar between the two medications, the effect on trough heart rate of timolol maleate gel-forming solution QD was significantly less than that of levobunolol BID (P = 0.001). The incidence of ocular burning and stinging was comparable between the two treatments. Patients experienced significantly more blurred vision when using timolol maleate gel-forming solution than when using levobunolol (P = 0.013). Overall, more patients experienced at least one adverse event when using timolol maleate gel-forming solution. Timolol maleate gel-forming solution QD is as efficacious in reducing IOP as levobunolol BID.
Vasodilatory mechanism of levobunolol on vascular smooth muscle cells
Exp Eye Res 2007 Jun;84(6):1039-46.17459374 10.1016/j.exer.2007.01.010
Topical application of Levobunolol hydrochloride, a beta-adrenergic antagonist used for treatment of glaucoma, is reported to increase ocular blood flow. We studied the mechanism of levobunolol-induced vasodilation in arterial smooth muscle. The effects of levobunolol or other agents on isolated, pre-contracted rabbit ciliary artery were investigated using an isometric tension recording method. The effects of the same agents on intracellular free calcium ([Ca(2+)](i)) in cultured human aortic smooth muscle cells were also studied by fluorophotometry. Levobunolol relaxed ciliary artery rings that were pre-contracted with either high-K solution, 1microM histamine, 10microM phenylephrine, or 100nM endothelin-1. The relaxation induced by levobunolol was concentration-dependent over the range of 10microM to 0.3mM. Inhibition of endothelial nitric oxide synthase or denudation of the endothelium did not affect this relaxation. Histamine-induced contractions were inhibited by the histamine H(1) antagonist pyrilamine. Radioligand binding experiments showed that levobunolol did not bind to the H(1) receptor. Further, histamine induced transient contraction in Ca(2+)-free solution, and levobunolol inhibited this contraction by 74.6+/-11.0%. In cultured smooth muscle cells in the presence of extracellular Ca(2+), levobunolol significantly inhibited the histamine-induced elevation of [Ca(2+)](i). However, it did not inhibit the increase of [Ca(2+)](i) in histamine-stimulated cells incubated in Ca(2+)-free solution. These results indicate that levobunolol may relax rabbit ciliary artery by two different mechanisms. First, the relaxation could be due to the blockade of Ca(2+) entry through non-voltage-dependent Ca(2+) channels. Second, levobunolol may change the Ca(2+) sensitivity of vascular smooth muscle cells.
The effect of Levobunolol hydrochloride on the calcium and potassium channels in isolated ventricular myocytes of guinea pig
J Tongji Med Univ 1997;17(2):90-3.9639797 10.1007/BF02888242
The effects of levobunolol hydrochlorid (Bun) on the type L calcium channel currents (ICA) and delayed rectifier potassium channel currents (IK) in isolated ventricular myocytes of guinea pig were studied by using patch clamp whole cell recording techniques. The results were showed that: 1) Bun caused a dose dependent decrease in ICA and a dose-dependent increase in IK of the ventricular myocytes. The threshold concentrations of Bun for ICA and IK were 10(-8) mol/L and 10(-7) mol/L respectively. The maximum effective concentration of Bun for bot ICA and IK was 3x10(-5) mol/L, and half-maximal concentration was 3x10(-6) mol/L; 2) IK was blocked by 2x100(-6) mol/L tetraethylammonium (TEA). A concentration of 3x10(-6) mol/L Bun showed a decreasing effect on the ICA as revealed by the current-voltage relationship curve, i.e., Bun caused an elevation of the curve;3) When ICA was blocked by 2x10(-6) mol/L Isoptin (Verapamil), at a concentration of 3x10(-6) mol/L Bun showed an increasing effect on IK and the effect could be blocked by TEA. The above-mentioned results indicated that Bun had an inhibitory effect on ICA and a fascilitatory effect on IK. The results suggested that the molecular mechanisms of antihypertensive, heart rate slowing the beta -receptor blocking effects of Bun might be due to decrease of ICA and increase of IK.