Pharmacological Characterization of Olodaterol, a Novel Inhaled β2-Adrenoceptor Agonist Exerting a 24-Hour-Long Duration of Action in Preclinical Models

  title={Pharmacological Characterization of Olodaterol, a Novel Inhaled $\beta$2-Adrenoceptor Agonist Exerting a 24-Hour-Long Duration of Action in Preclinical Models},
  author={Thierry Bouyssou and Paola Casarosa and Emmanuel Naline and Sabine Pestel and Ingo Konetzki and Philippe Devillier and Andreas Schnapp},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={53 - 62}
The preclinical pharmacological profile of 6-hydroxy-8-[(1R)-1-hydroxy-2-[[2-(4-methoxyphenyl)-1,1-dimethylethyl]amino]ethyl]-2H-1,4-benzoxazin-3(4H)-one monohydrochloride (olodaterol, previously known as BI 1744 CL), a novel, enantiomeric pure, inhaled human β2-adrenoceptor (hβ2-AR) agonist, was compared with marketed drugs, such as salmeterol and formoterol. In vitro, olodaterol showed a potent, nearly full agonistic response at the hβ2-AR (EC50 = 0.1 nM; intrinsic activity = 88% compared… 

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