Levobetaxolol  (Synonyms: (S)-Betaxolol)

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].

Levobetaxolol shows a higher affinity at cloned human β1 and β2 receptor with K_i values of 0.76, 32.6 nM, respectively^[1].
Levobetaxolol inhibits functional activities in cells expressing human recombinant β1 and β2 receptors with K_b values of 6, 39 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

307.43

C₁₈H₂₉NO₃

93221-48-8

O[C@H](COC1=CC=C(C=C1)CCOCC2CC2)CNC(C)C

Room temperature in continental US; may vary elsewhere.

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• [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.  [Content Brief]

  [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.  [Content Brief]