The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that interacts with (binds) epinephrine, a hormone and neurotransmitter (ligand synonym, adrenaline) whose signaling, via a downstream Ltype calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. Unlike other adr...

During prolonged exposure to agonist, beta2-adrenergic receptors undergo downregulation, defined by the loss of radioligand binding sites. To determine the cellular basis for beta2-adrenergic receptor downregulation, we examined HEK293 cells stably expressing beta2-adrenergic receptors with an N-terminal epitope tag. Downregulation was blocked by leupeptin, a cysteine protease inhibitor, but no...

Previous studies have reported that the numbers of beta- and alpha-adrenergic receptors increase in ischemic myocardium. In vivo studies have raised questions regarding the mechanisms involved in the adrenergic receptor alterations and the consequences of these alterations. The purpose of this study was to evaluate potential relationships among beta-adrenergic receptor changes, high energy phos...

An increase in cardiac P-adrenergic sensitivity or 8-receptor density or both has been described in several animal species after denervating the heart. The transplanted human heart is also denervated and, therefore, may exhibit supersensitivity to /3-adrenergic agonists and an increase in .3-adrenergic receptor density. In 16 patients examined 1-3 months after orthotopic cardiac transplantation...

6. Stone LS, MacMillan LB, Kitto KF, Limbird LE, Wilcox GL: The a2a adrenergic receptor subtype mediates spinal analgesia evoked by a2 agonists and is necessary for spinal adrenergic-opioid synergy. J Neurosci 1997; 17:7157-65 7. MacMillan LB, Hein L, Smith MS, Piascik MT, Limbird LE: Central hypotensive effects of the a2a-adrenergic receptor subtype. Science 1996; 273:801-3 8. Link RE, Desai K...

KEY POINTS Patients with diabetes show a blunted cardiac inotropic response to β-adrenergic stimulation despite normal cardiac contractile reserve. Acute insulin stimulation impairs β-adrenergically induced contractile function in isolated cardiomyocytes and Langendorff-perfused hearts. In this study, we aimed to examine the potential effects of hyperinsulinaemia associated with high-fat diet (...

Hypothesis / aims of study It is clinically known that anticholinergic agents, commonly used for treating overactive bladder, etc., act on the muscarinic receptor in salivary glands, causing dry mouth as an adverse effect. Not only the muscarinic receptor but also the α1-adrenergic receptor are present in human salivary glands, and are thought to accelerate saliva production. The common adverse...

Objective - to study, the dynamics of catecholamine binding on erythrocytes when modeling stimulation and blockade adrenergic regulation mechanisms using cytological method
 Material methods. The number granules was determined silver nitrate impregnation under conditions administration anapriline -adrenergic receptor blocker (2 mg/kg), acute stress, activation noradrenergic systems (maprot...

Preincubation of turkey erythrocytes with catecholamines desensitizes the beta-adrenergic receptor-adenylate cyclase complex in the plasma membranes of these cells. Photoaffinity labeling of the beta-adrenergic receptors with 125I-labeled p-azidobenzylcarazolol (125I-pABC) and subsequent analysis by NaDodSO4/polyacrylamide gel electrophoresis demonstrates an altered mobility of receptor peptide...

Administration of enantiomerically pure β-adrenergic agonists and antagonists increases their activity and reduces side effects. We report here a small-molecule artificial receptor (SMAR) that, by mimicking the β-adrenergic receptor, is able to enantioselectively extract commercial β-adrenergic interacting drugs. The selectivity is justified according to DFT calculations and X-ray diffraction e...