UNLABELLED Recent efforts have suggested that the β-adrenergic receptor (β-AR) system may be a novel and viable therapeutic target for pain reduction; however, most of the work to date has focused on the β(2)-adrenergic receptor (AR). Here, we compared the antinociceptive effects of enantiomeric configurations of propranolol and bupranolol, two structurally similar nonselective β-blocking drugs...

Inhaled long-acting β(2)-adrenoceptor agonists (LABA) that act as bronchodilators and the oral anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor roflumilast are both approved therapies for chronic obstructive pulmonary disease (COPD). Here we describe the activity of a novel, inhaled, bifunctional, small molecule (R)-6-[(3-{[4-(5-{[2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethy...

Background and Aims: Hypericum microcalycinum Boiss. & Heldr. is used for inflammatory diseases in Anatolia. The involvement of liver X receptors (LXRs) free radicals diseases, activation LXRs, high radical contents cancerous tissue organs prompted us to determine the scavenging LXRα agonist activity aqueous fraction methanol extract fractions H. along with isolation studies from active fracti...

the internal mammary artery (ima) is currently the preferred conduit for myocardial revascularization. however, pre-operative vasospasm and a hypoperfusion state during maximal exercise may limit its use as a bypass graft. the mechanism of spasm has not been clearly defined. since β-adrenoceptor activation plays a major role in vasorelaxation, the present study was carried out to investigate th...

introduction: the ginger rhizome has been widely used in traditional medicine for treatment of gastrointestinal diseases. in the present study the effect of ginger alcoholic extract on mechanical activity of isolated jejunum of male rats and also its interaction with cholinergic, adrenergic and nitrergic systems were investigated. methods: seven adult male wistar rats were anesthetized by ethyl...

Objective(s): To analyze the potential influences of propofol on the oxidative stress of H2O2-induced human esophageal squamous cell carcinoma (ESCC) Eca109 cell through mediating the Wnt/β-catenin signaling pathway.Materials and Methods: Eca109 cells were classified into 5 groups: Control group, H2O2 group, Propofol + H2O2 group, Dkk1 (Dickkopf-1, Wnt/β-catenin pathway antagonist) + H2O2 group...

β-3 adrenoceptor (AR) activation opposes the effects of β-1 and β-2 AR rescues excessive catecholamines. BRL37344 (beta3-AR agonist) is antiarrhythmic in canine models. Mirabegron a agonist approved by FDA for treatment overactive bladder. A previous study showed that isoproterenol activates small conductance Ca-activated K current more female than male ventricles. To test hypothesis mirabegron...

G protein-coupled receptors (GPCRs) have critical roles in various physiological and pathophysiological processes, and more than 40% of marketed drugs target GPCRs. Although the canonical downstream target of an agonist-activated GPCR is a G protein heterotrimer; there is a growing body of evidence suggesting that other signaling molecules interact, directly or indirectly, with GPCRs. However, ...

G-protein-coupled receptors (GPCRs) are typically present in a basal, inactive state but, when bound to an agonist, activate downstream signaling cascades. In studying arrestin regulation of opioid receptors in dorsal root ganglia (DRG) neurons, we find that agonists of delta opioid receptors (δORs) activate cofilin through Rho-associated coiled-coil-containing protein kinase (ROCK), LIM domain...

Two separate lines of evidence suggested the present study. First, intracerebroventricularly (i.c.v.) administered morphine (a μ-opioid receptor agonist) and β-endorphin (an ε-opioid receptor agonist) produce antinociception by activating different descending pain inhibitory systems. Second, γ-irradiation attenuates the acute antinociceptive action of i.c.v. injected morphine, but not DPLPE (a ...