Levalbuterol (hemitartrate)

Levalbuterol (Levosalbutamol) hemitartrate is a β₂-adrenergic receptor agonist and PI3 kinase inhibitor. Levalbuterol hemitartrate inhibits PI3 kinase activity, reduces NF-κB and Rb protein expression, activates the cAMP/PKA pathway, and stimulates cAMP release. Levalbuterol hemitartrate suppresses bronchial smooth muscle proliferation, relaxes airway smooth muscle, reduces intracellular calcium levels, and inhibits spasmogen-induced contractions. Levalbuterol hemitartrate can be used for the research of asthma and moderate-to-severe asthma^[1][2][3]. In Vitro:Levalbuterol (0.001-100 μM; 24 h) inhibits human bronchial smooth muscle cell proliferation in a biphasic manner, with maximum 80% inhibition at 0.1 μM, via β₂-adrenergic receptor and cAMP/PKA pathway activation^[1].
Levalbuterol (1 μM; 24 h) hemitartrate has an inhibitory effect on human bronchial smooth muscle cell proliferation that is completely abrogated by preincubation with 1 μM β₂-adrenergic receptor antagonist ICI-118551 (HY-100543) (2 h preincubation)^[1].
Levalbuterol (1 μM; 2 h) hemitartrate has an inhibitory effect on human bronchial smooth muscle cell proliferation that is attenuated or abrogated, respectively, by co-treatment with 1 μM or 10 μM (S)-Albuterol (HY-137311A) (24 h)^[1].
Levalbuterol (1 μM; 24 h) hemitartrate has an inhibitory effect on human bronchial smooth muscle cell proliferation that is enhanced by co-treatment with 10 μM 8-Br-cAMP (HY-12306A) (2 h preincubation) and completely abrogated by co-treatment with 10 μM Rp-cAMPS (HY-100530A) (2 h preincubation), confirming involvement of the cAMP/PKA pathway^[1].
Levalbuterol (0.1-1.0 μM; 15 min) hemitartrate stimulates cAMP release in human bronchial smooth muscle cells, an effect that is attenuated by 65% with co-treatment of 1.0 μM (S)-Albuterol (15 min)^[1].
Levalbuterol (1.0 μM; 20 min) hemitartrate inhibits inositol phosphate release by 50% in human bronchial smooth muscle cells, indicating inhibition of PI-3 kinase activity^[1].
Levalbuterol (1.0 μM; 24 h) hemitartrate inhibits NF-κB protein expression by 50% and Rb protein expression by 40% in human bronchial smooth muscle cells^[1].
Levalbuterol hemitartrate induces airway smooth muscle relaxation and reduces spasmogen-induced contractions in in vitro ASM cells/tissues from horse, cow, guinea pig, mouse, and human sources via β₂-adrenoreceptor ligation-dependent mechanisms^[3].
Levalbuterol hemitartrate exerts anti-inflammatory effects in human eosinophils and T lymphocytes by inhibiting proinflammatory mediator release and T-cell proliferation via β₂-adrenoreceptor ligation^[3].
Levalbuterol hemitartrate reduces proinflammatory GM-CSF release from human ASM cells, enhances corticosteroid-mediated suppression of cytokine release, and modulates intracellular cAMP and NF-κB signaling pathways via β₂-adrenoreceptors^[3].