Landiolol

Landiolol (ONO1101) is a highly selective, ultra-short-acting competitive inhibitor of β₁ adrenergic receptors. Landiolol specifically blocks cardiac β₁ receptors, reducing heart rate and myocardial oxygen consumption. Landiolol inhibits TNF-α-induced excessive mitochondrial oxygen consumption and reactive oxygen species production in a sepsis model, alleviating renal injury. Landiolol has little effect on cardiac ion channels (such as L-type calcium current and inward rectifier potassium current) and has a weak negative inotropic effect. Landiolol can be used for perioperative tachycardia control and protection studies of sepsis-related acute kidney injury^[1][2][3]. IC50 & Target:Beta-Adrenergic Receptor In Vitro:Landiolol (10 μM; 24 h) significantly inhibits the increase in mitochondrial oxygen consumption rate (OCR) induced by TNF-α (0.5 nM) in HEK293 cells, reducing the basal OCR from 123% to 94.8%, and reduces the generation of reactive oxygen species (ROS)^[1].
Landiolol (10 μM; 24 h) inhibits the excessive glycolytic capacity of HEK293 cells induced by TNF-α (0.5 nM), but does not significantly affect its basal glycolytic (ECAR) level^[1]. In Vivo:Landiolol (0.1 mg/kg/min; intravenous infusion; single dose; 6 h) significantly reduces serum creatinine and lactate concentrations and alleviates renal tubular necrosis and inflammatory damage in the lipopolysaccharide (LPS)-induced acute kidney injury model in rats. Landiolol may not mediate renal protection through systemic anti-inflammatory or antioxidant effects^[2].
Landiolol has less effect on cardiac function than Esmolol (HY-B1392A) and does not directly shorten the action potential duration (APD)^[3].