beta(2)-Adrenoceptor agonists are the most effective bronchodilators currently available, and are used for symptom management in asthmatics. However, whether beta(2)-agonists are also antitussive is controversial. Identifying an antitussive role for beta(2)-agonists and dissecting the possible mechanism of action may help to explain the inconsistencies in the clinical literature and lead to the...

The current concept of asthma therapy is based on a stepwise approach, depending on disease severity, and the aim is to reduce the symptoms that result from airway obstruction and inflammation, to prevent exacerbations and to maintain normal lung function. Beta2-adrenoceptor agonists and glucocorticoids are at present the most effective drugs for the treatment of airway obstruction and inflamma...

f3-Adrenoceptors in the myometrium of the pregnant ewe were studied both functionally and by radioligand binding techniques using (3 HI dihydroalprenolol (DHA). Spontaneous contractile activity in vitro was inhibited by 3-adrenoceptor agonists in a stereoselective manner; the order of potency suggested a 132 -adrenoceptor was involved. The effects of salbutamol were antagonized competitively by...

The mechanisms that control lipolysis in intra-abdominal fat cells from various primate species, the marmoset (Callithrix jacchus), the baboon (Papio papio), and the macaque (Macaca fascicularis), were compared to those of human intraabdominal fat cells. Selective beta 1- or beta 2-adrenoceptor agonists induced lipolysis in all species. Selective beta 3-agonists (BRL 37344, CL 316243, and SR 58...

BACKGROUND β2-adrenoceptor agonists have been shown to reduce the lipopolysaccharide (LPS)-induced cytokine release by human monocyte-derived macrophages (MDMs). We compare the expression of β2-adrenoceptors and the inhibitory effect of formoterol and salmeterol on the LPS-induced release of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and a range of chemokines (CCL2, 3, 4, and IL-8...

We investigated the a,-adrenoceptor subtypes of rabbit saphenous vein which has a mixed functional population of α1 and α2 -adrenoceptors. Lateral saphenous veins were obtained from male rabbits weighing 3.20-4 kg, which were killed by overdose with pentobarbitone sodium (i.v. injection). They were easily dissected out and placed in cold, oxygenated modified Krebs-Henselite solution (Krebs)...

The objective of this study was to evaluate the potency and efficacy (intrinsic activity) of formoterol and salmeterol and their duration of action in comparison with other beta-adrenoceptor agonists in isolated human bronchi. Human bronchi were obtained at thoracotomy from patients with lung cancer. Potency (-log of the concentration of drug inducing 50% of maximal relaxation (-log EC50)) and ...

The imidazoline compounds may produce mydriasis after systemic administration to some species (rats, cats, and mice). In mydriatic activity of imidazolines, α2D-adrenoceptors subtype(s) seems to be involved. In this study, the pupil dilatory effect evoked by 2 newly synthesized imidazoline derivatives-α2-adrenoceptor agonists: marsanidine and 7-methylmarsanidine-was compared. The compounds were...