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Carteolol HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Carteolol HCl图片
CAS NO:51781-21-6
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
Carteolol HCl (OPC-1085 hydrochloride) 是一种用于治疗青光眼的非选择性 β 受体阻滞剂。
Cas No.51781-21-6
别名盐酸卡替洛尔; OPC-1085 hydrochloride
化学名5-(3-(tert-butylamino)-2-hydroxypropoxy)-3,4-dihydroquinolin-2-ol hydrochloride
Canonical SMILESCC(C)(NCC(O)COC1=CC=CC2=C1CCC(O)=N2)C.Cl
分子式C16H25ClN2O3
分子量328.83
溶解度≥ 16.4mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Beta-adrenergic antagonist are an important class of drugs for the treatment of various heart diseases, such as high blood pressure, insufficiency of blood flow to the heart muscle, irregular heart beat, thickened heart muscle, and decreased ability of the heart to empty or fill normally. β-Blockers can also be used to treat migraine headache and increased eye pressure (glaucoma). Carteolol is a nonselective beta-adrenoceptor antagonist.

In vitro: Previous findings demonstrate that carteolol, unlike xamoterol, is a nonconventional partial agonist, which causes agonistic effects via interaction with the low-affinity propranolol-resistant site of β1-adrenoceptors and antagonistic actions by the high-affinity site of the same receptors [1].

In vivo: Both 8-OH carteolol and carteolol suppressed the water-load induced intraocular pressure (IOP) rise in rabbits. 8-OH carteolol was more effective in suppressing water-load induced IOP rise in rabbits compared with carteolol on equimolar basis. Both 8-OH carteololand carteolol caused a significant decrease in IOP in monkeys. 8-OH carteolol was estimated to be more potent than carteolol in lowering IOP on equimolar basis in monkeys [2].

Clinical trial: The new alginate formulation of long-acting carteolol 1% given once daily is as effective as standard 1% carteolol given twice daily, with no meaningful differences regarding safety. The new alginate formulation of long-acting 1% carteolol given once a day is effective and well tolerated by glaucoma patients requiring chronic treatment [3].

Reference:
[1] Maura Floreani, Guglielmina Froldi, Luigi Quintieri, Katia Varani, Pier Andrea Borea, Maria Teresa Dorigo and Paola Dorigo.  In Vitro Evidence That Carteolol Is a Nonconventional Partial Agonist of Guinea Pig Cardiac β1-Adrenoceptors: A Comparison with Xamoterol. JPET 315:1386–1395, 2005
[2] Sugiyama K, Enya T, Kitazawa Y.  Ocular hypotensive effect of 8-hydroxycarteolol, a metabolite of carteolol. Int Ophthalmol. 1989 Jan;13(1-2):85-9.
[3] Trinquand C, Romanet JP, Nordmann JP, Allaire C; Groupe d'étude.  Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study. J Fr Ophtalmol. 2003 Feb;26(2):131-6.