History suggests β agonists, the cognate ligand of the β 2 adrenoceptor, have been used as
bronchodilators for around 5,000 years, and β agonists remain today the frontline treatment …

Bronchodilators are central in the treatment of of airways disorders. They are the mainstay of
the current management of chronic obstructive pulmonary disease (COPD) and are critical in …

Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …

Since the discovery nearly 60 years ago, cAMP is envisioned as one of the most universal
and versatile second messengers. The tremendous feature of cAMP to tightly control highly …

Agonists activating β2-adrenoceptors (β2ARs) on airway smooth muscle (ASM) are the drug
of choice for rescue from acute bronchoconstriction in patients with both asthma and chronic …

G protein coupled receptors (GPCRs) were first characterized as signal transducers that
elicit downstream effects through modulation of guanine (G) nucleotide-binding proteins …

Asthma is a heterogeneous inflammatory disease of the airways that is associated with
airway hyperresponsiveness and airflow limitation. Although asthma was once simply …

Activation of β2-adrenoceptors (β2ARs) causes airway smooth muscle (ASM) relaxation and
bronchodilation, and β2AR agonists (β-agonists) are front-line treatments for asthma and …

Abstract β-Adrenergic receptors (βARs) belong to a large family of cell surface receptors
known as G protein–coupled receptors (GPCRs). They are coupled to Gs protein (Gαs) for …

Biased agonists of G protein–coupled receptors (GPCRs), which selectively activate either G
protein–or β-arrestin–mediated signaling pathways, are of major therapeutic interest …