左旋倍他洛尔 T6565

Product Introduction
Bioactivity


英文名: Levobetaxolol hydrochloride

描述: Levobetaxolol hydrochloride ((S)-Betaxolol hydrochloride) 是 β-肾上腺素能受体抑制剂 (β阻滞剂) 。它具有降低眼压的作用，可用于研究青光眼。

体外活性: 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. [1] 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. [2]

体内活性: Levobetaxolol (150 mg/eye) is more potent than dextrobetaxolol, reducing intraocular pressure by 25.9% in conscious ocular hypertensive cynomolgus monkeys. [1] 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. [3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 64 mg/mL (186.1 mM)
Ethanol : 64 mg/mL (186.1 mM)
H2O : 63 mg/mL (183.2 mM)


关键字: Adrenergic Receptor | Levobetaxolol hydrochloride | Levobetaxolol | Inhibitor | (S)-Betaxolol | inhibit | Betaxolol Hydrochloride | Levobetaxolol Hydrochloride | Beta Receptor

相关产品: Dexmedetomidine hydrochloride | Conopeptide rho-TIA | Muscarinic toxin 3 | AVN-101 | Deoxycorticosterone acetate | Synephrine hydrochloride | Lofexidine | Faxeladol | Brefonalol HCl | Guanfacine hydrochloride

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compound Library

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