Formoterol Hemifumarate (C09-0895-954)

InformationFormoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316) is a potent, selective and long-actingβ2-adrenoceptoragonist used in the management of asthma and chronic obstructive pulmonary disease(COPD).In vitroFormoterol is a potent airway smooth muscle relaxant with high efficacy, and very high affinity and selectivity for the beta 2-adrenoceptor. Formoterol appears to be retained in airway smooth muscle for extended periods since its relaxant effect on human airway smooth muscle is resistant to repeated washing and formoterol displays /'reassertion/' of relaxation after washout of a beta-adrenoceptor antagonist. Formoterol has been demonstrated to potently inhibit these cells and processes in experimental test systems. Formoterol, like salbutamol and salmeterol, relaxes isolated preparations of guinea-pig trachea and human bronchus, and inhibits antigen-induced mediator release from human lung fragments in a concentration-related fashion.In vivoFormoterol causes dose-related inhibition of histamine-induced bronchoconstriction in conscious guinea-pigs. Formoterol inhibits histamine-induced plasma protein extravasation (PPE) in guinea-pig lung, with significant inhibition being observed at 10 mg /mL and 100 mg /mL. Formoterol (100 mg /mL) inhibits PPE in guinea-pig lung for 2-4 hours, a duration of action intermediate between that previously obtained for salbutamol (1 hour) and salmeterol (> 6 hours). Formoterol inhibits neutrophil accumulation (lipopolysaccharide-induced) in guinea-pig lung but at doses greater than those required to inhibit granulocyte-independent PPE (histamine-induced). Formoterol (100 mg /mL) inhibits PAF-induced eosinophil accumulation in guinea-pig lung.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C19H24N2O4·1/2C4H4O4 Molecular Weight: 402.4