An estimation of β2-adrenoceptor reserve on human bronchial smooth muscle for some sympathomimetic bronchodilators

Characterising the Mechanism of Airway Smooth Muscle β2 Adrenoceptor Desensitization by Rhinovirus Infected Bronchial Epithelial Cells

Rhinovirus (RV) infections account for approximately two thirds of all virus-induced asthma exacerbations and often result in an impaired response to β2 agonist therapy. Using an in vitro model of RV infection, we investigated the mechanisms underlying RV-induced β2 adrenoceptor desensitization in primary human airway smooth muscle cells (ASMC). RV infection of primary human bronchial epithelia...

Beta-adrenoceptor reserve in human lung: a comparison between airway smooth muscle and mast cells.

The effects of several beta-adrenoceptor agonists on the relaxation of precontracted human bronchial rings and the inhibition of IgE-mediated histamine release from human lung mast cells (HLMC) were studied. For the relaxation of bronchial rings, isoprenaline, fenoterol and terbutaline were full agonists whereas salbutamol was a full agonist in some (two out of six) experiments and a partial ag...

Adrenoceptor - Activating & Other Sympathomimetic Drugs

The ultimate effects of sympathetic stimulation are mediated by release from nerve terminals of norepinephrine that serves to activate the adrenoceptors on postsynaptic sites. Also, in response to a variety of stimuli such as stress, the adrenal medulla releases epinephrine, which is transported in the blood to target tissues; in other words, epinephrine acts as a hormone. Drugs that mimic the ...

Evidence for a Non-β2-Adrenoceptor Binding Site in Human Lung Tissue for a Subset of β2-Adrenoceptor Agonists

The aim of this study was to compare the binding profile of a range of β2-adrenoceptor (β2-AR) agonists and antagonists in human lung tissue. Radioligand saturation and competition binding experiments were performed by filtration with a β2-AR antagonist ([H]propranolol) or agonist ([H]vilanterol) radioligand and membrane fragments generated from lung parenchyma in the presence of 100 μM guanosi...

Long-acting β2-adrenoceptor agonists synergistically enhance glucocorticoid- dependent transcription in human airways epithelial and smooth muscle cells