Olodaterol (BI1744) is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.
In Vitro: Olodaterol shows a potent, nearly full agonistic response at the hβ2-adrenoceptor (EC50=0.1 nM; intrinsic activity=88% compared with isoprenaline) and a significant selectivity profile (241- and 2299-fold against the hβ1- and hβ3-ARs, respectively).
In Vivo: Olodaterol is a long acting β2-agonist that induces bronchodilation up to 24 h after dosing in patients with chronic obstructive pulmonary disease (COPD) . Olodaterol dose-dependently attenuates cell influx and pro-inflammatory mediator release in murine and guinea pig models of pulmonary inflammation. Once-daily olodaterol 5 μg is an effective therapy in improving lung function and symptomatic outcomes in patients with moderate to very severe (COPD) receiving other maintenance therapy, with a satisfactory safety profile.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10mM in DMSO|
Olodaterol for the treatment of chronic obstructive pulmonary disease.
Ramadan WH, et al. Am J Health Syst Pharm. 2016 Aug 1;73(15):1135-43. PMID: 27354040.
The long-acting β2 -adrenoceptor agonist olodaterol attenuates pulmonary inflammation.
Wex E, et al. Br J Pharmacol. 2015 Jul;172(14):3537-47. PMID: 25824824.
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