Penbutolol sulfate ((-)-Terbuclomine)
(Synonyms: 喷布特罗硫酸盐,(-)-Terbuclomine) 目录号 : GC32494
A β-adrenergic and 5-HT1A receptor antagonist
Cas No.:38363-32-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Penbutolol is an antagonist of β-adrenergic receptors (β-ARs; IC50 = 2.8 nM) and the serotonin (5-HT) receptor subtype 5-HT1A (IC50 = 9.9 nM).1 It inhibits adenylate cyclase activity induced by the β-AR agonist isoprenaline in guinea pig myocardial membranes with a Ki value of 2.4 nM.2 Penbutolol reduces basal renin activity and blood pressure in spontaneously hypertonic rats.3 It decreases isolation-induced aggressive behavior in mice (ED50 = 56 ?mol/kg) and reverses reductions in aggression induced by 8-hydroxy-DPAT and TFMPP with ED50 values of 8.1 and 2.1 ?mol/kg, respectively.1 Formulations containing penbutolol were previously used in the treatment of arterial hypertension.
1.Sánchez, C., Arnt, J., and Moltzen, E.K.The antiaggressive potency of (–)-penbutolol involves both 5-HT1A and 5-HT1B receptors and β-adrenoceptorsEur. J. Pharmacol.297(1-2)1-8(1996) 2.Krawietz, W., Poppert, D., Erdmann, E., et al.β-adrenergic receptors in guinea-pig myocardial tissueNaunyn Schmiedebergs Arch. Pharmacol.295(3)215-224(1976) 3.Kaiser, J., H?rtfelder, G., Lindner, E., et al.Pharmacology of the β-receptor blocker penbutololArzneimittelforschung30(3)420-427(1980)
| Cas No. | 38363-32-5 | SDF | |
| 别名 | 喷布特罗硫酸盐,(-)-Terbuclomine | ||
| Canonical SMILES | O[C@@H](CNC(C)(C)C)COC1=CC=CC=C1C2CCCC2.[0.5H2SO4] | ||
| 分子式 | C18H29NO2 . 1/2 H2O4S | 分子量 | 340.47 |
| 溶解度 | Water : 5 mg/mL (14.69 mM) | 储存条件 | Store at -20°C,sealed storage, away from moisture |
| 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 | 2.9371 mL | 14.6856 mL | 29.3712 mL |
| 5 mM | 0.5874 mL | 2.9371 mL | 5.8742 mL |
| 10 mM | 0.2937 mL | 1.4686 mL | 2.9371 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。
Influence of sonophoresis and chemical penetration enhancers on percutaneous transport of Penbutolol sulfate
Pharm Dev Technol 2016 Dec;21(8):990-995.PMID:26383739DOI:10.3109/10837450.2015.1086373.
The effect of ultrasound and chemical penetration enhancers on transcutaneous flux of Penbutolol sulfate across split-thickness porcine skin was investigated. Penbutolol sulfate is a potent, noncardioselective beta-blocker, which is used for the management of hypertension. The drug is one of the most lipid soluble of the β-adrenoceptor antagonists used clinically. It has an n-octanol/pH 7.4 buffer partition coefficient of 179 compared to a value of 22 for propranolol. The amount of Penbutolol sulfate transported across the skin is low. In this project, we studied the effect of sonophoresis and chemical penetration enhancers on transdermal delivery of Penbutolol sulfate. Low-frequency sonophoresis at a frequency of 20 kHz increased transcutaneous flux of Penbutolol sulfate by 3.5-fold (27.37 ± μg cm-2 h-1) compared to passive delivery (7.82 ± 1.72 μg cm-2 h-1). We also investigated the effect of 50% ethanol, 1% limonene and 2% isopropyl myristate (IPM) on transcutaneous permeation of Penbutolol sulfate. IPM, ethanol and limonene at the concentration of 1%, 50% and 2%, respectively, increased the steady-state flux values of Penbutolol sulfate 2.2- (17.07 ± 3.24 μg cm-2 h-1), 2.6 - (19.40 ± 6.40 μg cm-2 h-1) and 3.4-times (26.38 ± 5.01 μg cm-2 h-1) compared to passive delivery (7.76 ± 2.9 μg cm-2 h-1). The results demonstrate that although there were slight increases in flux values, ultrasound, ethanol, limonene and IPM did not significantly enhance the transdermal delivery of Penbutolol sulfate. Future studies will examine ways of optimizing sonophoretic and chemical enhancer parameters to achieve flux enhancement.
In vitro transdermal iontophoretic delivery of Penbutolol sulfate
Drug Deliv 2009 Jan;16(1):11-4.PMID:19555303DOI:10.1080/10717540802396976.
Iontophoretic transport of Penbutolol sulfate across porcine ear skin was studied. Passive transdermal flux of the drug in phosphate-buffered saline was 7.65 microg/cm(2) hr. There was statistically significant flux enhancement when direct current iontophoresis was applied. Iontophoresis (0.11 mA/cm(2), 0.17 mA/cm(2), and 0.22 mA/cm(2)) for 6 hr, resulted in net transport of 87.36 microg/cm(2), 137.51 microg/cm(2), and 201.12 microg/cm(2) of Penbutolol sulfate, respectively. After 24 hr, cumulative amount of penbutolol transported were 201.63, 300.76, and 359.98 microg/cm(2), respectively. There was a 2.20- (0.11 mA/cm(2)), 3.26- (0.17 m/Acm(2)), and 4.28-fold (0.22 mA/cm(2)) enhancement in transcutaneous steady-state flux values compared to passive delivery. Steady-state fluxes of Penbutolol sulfate also increased proportionally to current density. Steady-state fluxes calculated from the linear portion of the cumulative amount versus time curves for Penbutolol sulfate were 16.68, 24.97, and 32.76 microg/cm(2)/hr at current densities of 0.11, 0.17, and 0.22 mA/cm(2). This study provides initial evidence for the potential use of iontophoresis for enhanced transdermal delivery of Penbutolol sulfate.
Newer antihypertensive agents
Postgrad Med 1991 Apr;89(5):75-81, 84, 89.PMID:2008405DOI:10.1080/00325481.1991.11700892.
Three recent additions to the list of antihypertensive agents have been approved for use as monotherapy or in combination with other drugs. Betaxolol hydrochloride (Kerlone) maintains its effect for 24 hours, making it a true once-a-day beta blocker. Penbutolol sulfate (Levatol) is as effective as other beta blockers and diuretics. Doxazosin mesylate (Cardura), a selective alpha 1 blocker, also allows once-a-day dosing and has produced favorable changes in lipid profiles. Two new drug delivery systems, one for verapamil hydrochloride (Verelan) and one for extended-release nifedipine (Procardia XL), allow less frequent dosing and may offer other advantages, such as greater compliance and a more tolerable side-effect profile.
Thermotropic liquid crystalline drugs
J Pharm Pharmacol 2005 Jul;57(7):807-16.PMID:15969938DOI:10.1211/0022357056208.
Crystalline solids are characterized by long-range positional and orientational order in three dimensions, whereas amorphous liquids lack long-range order in any dimension. Liquid crystals (mesophases) show structural, mechanical and optical properties intermediate to those of crystalline solids and the amorphous, liquid state of matter. There are two principle types of liquid crystals: thermotropic liquid crystals (TLCs) and lyotropic liquid crystals (LLCs). TLCs can be formed by heating a crystalline solid or by cooling an isotropic melt of a TLC-forming molecule (mesogen). In the first part of this review the types of liquid crystals are defined and classified and the structural properties of mesogens are explained. In the second part, ten case studies of thermotropic mesomorphous drugs and pharmaceutically relevant molecules (arsphenamine, nafoxidine hydrochloride, L-660711, palmitoyl propranolol hydrochloride, Penbutolol sulfate, itraconazole hydrochloride, fenoprofen sodium, fenoprofen calcium, ciclosporin and cholesteryl esters) are presented and their thermotropic mesomorphism is described. The review closes with a brief discussion of the unusual properties of drug mesophases and a potential use of drugs and excipients in this fourth state of matter.