aladdin 阿拉丁 L413091 左旋倍他洛尔盐酸盐 116209-55-3 98%

中文名：左旋倍他洛尔盐酸盐

英文名：Levobetaxolol HCl

纯度：≥98%

货号：L413091

Cas号：116209-55-3

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Levobetaxolol (AL 1577A) exhibits a higher affinity at cloned human β1 and β2 receptors with Kivalue of 0.76 nM and 32.6 nM, respectively.

Targets

β1-adrenergic receptor ; β2-adrenergic receptor 0.76 nM(Ki); 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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