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Levobetaxolol

Cat. No. M30933
Levobetaxolol Structure
Synonym:

(S)-Betaxolol

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 307.43
Formula C18H29NO3
CAS Number 93221-48-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tianjing Li, et al. Ophthalmology. Comparative Effectiveness of First-Line Medications for Primary Open-Angle Glaucoma: A Systematic Review and Network Meta-analysis

[2] Luciano Quaranta, et al. Clin Ophthalmol. Levobetaxolol hydrochloride: a review of its pharmacology and use in the treatment of chronic open-angle glaucoma and ocular hypertension

[3] N N Osborne, et al. Brain Res Bull. Effectiveness of levobetaxolol and timolol at blunting retinal ischaemia is related to their calcium and sodium blocking activities: relevance to glaucoma

[4] Neeraj Agarwal, et al. Exp Eye Res. Levobetaxolol-induced Up-regulation of retinal bFGF and CNTF mRNAs and preservation of retinal function against a photic-induced retinopathy

[5] N A Sharif, et al. J Ocul Pharmacol Ther. Levobetaxolol (Betaxon) and other beta-adrenergic antagonists: preclinical pharmacology, IOP-lowering activity and sites of action in human eyes

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