Pharmacological characterization of abediterol, a novel inhaled β(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models.

Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models.

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 beta(2)-adrenoceptor (hbeta(2)-AR) agonist, was compared with marketed drugs, such as salmeterol and formoterol. In vitro, olodaterol sho...

Pharmacological Characterization 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), a Novel Inhaled ß2- Adrenoceptor Agonist exerting a 24-hour long Duration of Action in Preclinical Models

In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action.

Vilanterol trifenatate (vilanterol) is a novel, long-acting β(2)-adrenoceptor (β(2)-AR) agonist with 24 h activity. In this study, we describe the preclinical pharmacological profile of vilanterol using radioligand binding and cAMP studies in recombinant assays as well as human and guinea pig tissue systems to characterize β(2)-AR binding and functional properties. Vilanterol displayed a subnan...

The Preclinical Pharmacology of Indacaterol

The preclinical pharmacological profile of indacaterol, a novel, chirally pure inhaled beta(2) adrenoceptor agonist, is described in this chapter. In various in vitro systems, indacaterol is close to a full agonist at the human β2-adrenoceptor with nanomolar potency. In isolated superfused human and guinea pig trachea, indacaterol has a fast onset of and a long duration of action. In the consci...

Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist, on small airways in human and rat precision-cut lung slices.

Indacaterol is a novel once daily inhaled beta(2) adrenoceptor agonist in clinical development. This study compared the properties of indacaterol with salmeterol, formoterol, and albuterol on small airways in precision-cut lung slices from human and rat contracted with carbachol and serotonin, respectively. In human lung slices, the rank order of potency was formoterol >/= salmeterol > indacate...