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...

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BACKGROUND β-Antagonists have recently been proposed for the treatment of chronic asthma; however, concerns regarding risk of acute bronchoconstriction in clinical trials remain. OBJECTIVE To determine the frequency of oral β-blocker prescribing in patients with asthma and associations with severe asthma exacerbations requiring oral steroids in patients with active asthma defined by prior ast...

BACKGROUND The aim of this study was to evaluate the effect of diabetes on the function and distribution of vascular α(1)-adrenoceptors in the abdominal aorta and distal mesenteric artery from streptozotocin (STZ)-induced diabetic rats at the level of the α(1)-adrenoceptor subtypes. METHODS Diabetes was induced by a single intravenous injection of STZ (60 mg/kg) in 8 week-old male Sprague-Daw...

Previous research has indicated that allosteric interactions across the dimer interface of β1-adrenoceptors may be responsible for a secondary low affinity binding conformation. Here we have investigated the potential for probe dependence, in the determination of antagonist pKi values at the human β1-adenoceptor, which may result from such allosterism interactions. Three fluorescent β1-adrenoce...