Home GPCR & G Protein Adrenergic Receptor antagonist Levobetaxolol HCl

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Levobetaxolol HCl Adrenergic Receptor antagonist

Cat.No.S4085

Levobetaxolol (AL 1577A,(S)-Betaxolol hydrochloride) exhibits a higher affinity at cloned human β1 and β2 receptors with Ki value of 0.76 nM and 32.6 nM, respectively.
Levobetaxolol HCl Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 343.89

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Quality Control

Batch: S408501 DMSO]69 mg/mL]false]Water]69 mg/mL]false]Ethanol]69 mg/mL]false Purity: 99.53%
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99.53

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (200.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 69 mg/mL

Ethanol : 69 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 343.89 Formula

C18H29NO3.HCl

 Storage (From the date of receipt)
CAS No. 116209-55-3 Download SDF Storage of Stock Solutions

Synonyms AL 1577A,(S)-Betaxolol hydrochloride Smiles CC(C)NCC(COC1=CC=C(C=C1)CCOCC2CC2)O.Cl

Mechanism of Action

Features
An estimated 89-fold more β1-selective vs. β2.
Targets/IC50/Ki
β1-adrenergic receptor
0.76 nM(Ki)
β2-adrenergic receptor
32.6 nM(Ki)
In vitro

Levobetaxolol potently antagonizes functional activities at cloned human β1 and β2 receptors, and also at guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors with IC50s of 33.2 nM, 2970 nM and 709 nM, respectively. Levobetaxolol (Ki = 16.4 nM) is more potent than dextrobetaxolol (Ki = 2.97 μM) at inhibiting isoproterenol-induced cAMP production in human non-pigmented ciliary epithelial cells. Levobetaxolol (topically applied) has been shown to reach the back of the eye in sufficient quantities to protect retinal ganglion cells from various types of insults. Levobetaxolol displaces [3H]-nitrendipine for L-type voltage-dependent calcium channel receptor with IC50 of 29.5 μM in rat cortex. Levobetaxolol reduces NMDA-stimulated 45Ca2+ influx by 47.3%. Levobetaxolol (topically applied) reduces the b-wave amplitude caused by ischaemia/reperfusion.

In vivo

Levobetaxolol (150 mg/eye) is more potent than dextrobetaxolol, reducing intraocular pressure by 25.9% in conscious ocular hypertensive cynomolgus monkeys. Levobetaxolol (20 mg/kg) significant protects retinal function and results in significantly thicker the RPE and outer nuclear layer in a photic-induced retinopathy rat model. Levobetaxolol (20 mg/kg) results in a 10-fold up-regulation of bFGF and a two-fold up-regulation of CNTF mRNA levels, trophic factors that have been shown to inhibit retinal degeneration in a number of species.

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