| Description |
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma[1][2].
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| Related Catalog |
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| Target |
β1 adrenoceptor:33.2 nM (IC50)
β2 adrenoceptor:2970 nM (IC50)
β3 adrenoceptor:709 nM (IC50)
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| In Vitro |
Levobetaxolol shows a higher affinity at cloned human β1 and β2 receptor with Ki values of 0.76, 32.6 nM, respectively[1]. Levobetaxolol inhibits functional activities in cells expressing human recombinant β1 and β2 receptors with Kb values of 6, 39 nM, respectively[1].
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| References |
[1]. Sharif NA, et al. Levobetaxolol (Betaxon) and other beta-adrenergic antagonists: preclinical pharmacology, IOP-lowering activity and sites of action in human eyes. J Ocul Pharmacol Ther. 2001 Aug;17(4):305-17. [2]. Osborne NN, et al. Effectiveness of levobetaxolol and timolol at blunting retinal ischaemia is related to their calcium and sodium blocking activities: relevance to glaucoma. Brain Res Bull. 2004 Feb 15;62(6):525-8.
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