product name Levobetaxolol HCl
Description: Levobetaxolol (also known as AL 1577A) is the S-isomer of betaxolol which exhibits a higher affinity at cloned human β1 and β2 receptors with Ki value of 0.76 nM and 32.6 nM, respectively. Levobetaxolol potently antagonizes functional activities at cloned human β1 and β2 receptors, 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.
References: J Ocul Pharmacol Ther. 2001 Aug;17(4):305-17; Exp Eye Res. 2002 Apr;74(4):445-53.
343.89
Formula
C18H29NO3.HCl
CAS No.
116209-55-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 69 mg/mL (200.6 mM)
Water: 69 mg/mL (200.6 mM)
Ethanol: 69 mg/mL (200.6 mM)
Solubility (In vivo)
Synonyms
AL 1577A
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399088
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Ocul Pharmacol Ther. 2001 Aug;17(4):305-17; Exp Eye Res. 2002 Apr;74(4):445-53. |
Related Posts
product name Levobetaxolol HCl
Description: Levobetaxolol (also known as AL 1577A) is the S-isomer of betaxolol which exhibits a higher affinity at cloned human β1 and β2 receptors with Ki value of 0.76 nM and 32.6 nM, respectively. Levobetaxolol potently antagonizes functional activities at cloned human β1 and β2 receptors, 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.
References: J Ocul Pharmacol Ther. 2001 Aug;17(4):305-17; Exp Eye Res. 2002 Apr;74(4):445-53.
343.89
Formula
C18H29NO3.HCl
CAS No.
116209-55-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 69 mg/mL (200.6 mM)
Water: 69 mg/mL (200.6 mM)
Ethanol: 69 mg/mL (200.6 mM)
Solubility (In vivo)
Synonyms
AL 1577A
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399088
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Ocul Pharmacol Ther. 2001 Aug;17(4):305-17; Exp Eye Res. 2002 Apr;74(4):445-53. |