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Penbutolol sulfate ((-)-Terbuclomine) Sale

(Synonyms: 喷布特罗硫酸盐,(-)-Terbuclomine) 目录号 : GC32494

A β-adrenergic and 5-HT1A receptor antagonist

Penbutolol sulfate ((-)-Terbuclomine) Chemical Structure

Cas No.:38363-32-5

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10mM (in 1mL DMSO)
¥495.00
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10mg
¥450.00
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50mg
¥1,350.00
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产品描述

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)

Chemical Properties

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
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Research Update

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.