93221-48-8

93221-48-8 structure

Name: LEVOBETAXOLOL
Chemical Name: (2S)-1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
CAS Number: 93221-48-8
Molecular Formula: C₁₈H₂₉NO₃
Molecular Weight: 307.42800
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2018-03-14 08:00:00
Modify Date: 2024-01-13 17:01:48
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].

Name	(2S)-1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
Synonyms	(S)-(-)-Betaxolol Levobetaxolol (S)-(-)-3-<4-<2-(cyclopropylmethoxy)ethyl>phenoxy>-1-(isopropylamino)-2-propanol UNII-75O9XHA4TU (-)-Betaxolol Levobetaxolol [INN] (S)-(-)-3-[4-[2-(cyclopropylmethoxy)]ethyl]phenoxy-1-(N-isopropylamino)-propan-2-ol

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].
Related Catalog	Research Areas >> Others Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Target	β1 adrenoceptor:33.2 nM (IC50) β2 adrenoceptor:2970 nM (IC50) β3 adrenoceptor:709 nM (IC50)
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].
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.