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

Pharmacological characterisation of indacaterol, a novel once-daily inhaled β2-adrenoceptor agonist, on small airways in human and rat precision-cut lung slices

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

Abediterol is a novel potent, long-acting inhaled β(2)-adrenoceptor agonist in development for the treatment of asthma and chronic obstructive pulmonary disease. Abediterol shows subnanomolar affinity for the human β(2)-adrenoceptor and a functional selectivity over β(1)-adrenoceptors higher than that of formoterol and indacaterol in both a cellular model with overexpressed human receptors and ...

In Vitro and in Vivo Pharmacological Characterization of 5-[(R)- 2-(5,6-Diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H- quinolin-2-one (Indacaterol), a Novel Inhaled 2 Adrenoceptor Agonist with a 24-h Duration of Action

Here, we describe the preclinical pharmacological profile of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8hydroxy-1H-quinolin-2-one (indacaterol), a novel, chirally pure inhaled 2 adrenoceptor agonist, in comparison with marketed drugs. Indacaterol is close to a full agonist at the human 2 adrenoceptor (Emax 73 1% of the maximal effect of isoprenaline; pEC50 8.06 0.02), whereas salm...

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...