Levalbuterol, also known as (R)-Albuterol or (R)-Salbutamol, is the active (R)-enantiomer of Salbutamol and serves as a short-acting β2-adrenergic receptor agonist. It is a more potent bronchodilator than Salbutamol and holds promise for the treatment of Chronic Obstructive Pulmonary Disease (COPD).

Levalbuterol, at a concentration of 10 μM over 24 hours, selectively upregulates 11β-HSD1 mRNA expression in airway epithelial cells without affecting 11β-HSD2 expression. Additionally, it markedly inhibits NF-κB activity triggered by LPS and TNF-α, while enhancing GRE activation through an 11β-HSD1 dependent pathway in a transformed murine airway epithelial cell line (Murine Club MTCC cells). This effect is confirmed using RT-PCR, demonstrating a specific increase in 11β-HSD1 mRNA expression.

Levalbuterol, when administered via subcutaneous injection at a dosage of 1 mg/kg for 14 days, significantly reduces pulmonary inflammation in C57BL/6 female mice with a pulmonary allergic model, specifically by decreasing eosinophilia and IgE levels. This result suggests a promising effect of Levalbuterol in mitigating pulmonary inflammation following OVA sensitization.