A functionalized derivative of the alpha 2-selective antagonist rauwolscine formed the basis for a photoaffinity adduct that has allowed identification of the hormone-binding subunit of the brain alpha 2-adrenergic receptor protein. Rauwolscine carboxylate underwent reaction with 4-N-t-butyloxycarbonyl-aminoaniline, leading to the synthesis of rauwolscine 4-aminophenyl carboxamide (Rau-AmPC). R...

Chronic intermittent hypobaric hypoxia (CIHH) has an effective cardiac protection against ischemia-reperfusion injury. However, the underlying mechanisms are not fully known. It has been shown that blockade of beta-adrenergic receptor exerts anti-arrhythmic action and improves cardiac remodeling in ischemic myocardium. Thus we determined the influence of CIHH on beta-adrenergic receptor activit...

Nozik-Grayck, Eva, Erin J. Whalen, Jonathan S. Stamler, Timothy J. McMahon, Pasquale Chitano, and Claude A. Piantadosi. S-nitrosoglutathione inhibits 1-adrenergic receptor-mediated vasoconstriction and ligand binding in pulmonary artery. Am J Physiol Lung Cell Mol Physiol 290: L136–L143, 2006. First published August 26, 2005; doi:10.1152/ajplung.00230.2005.—Endogenous nitric oxide donor compoun...

The closely related G protein-coupled receptor kinases GRK2 and GRK3 are both expressed in cardiac myocytes. Although GRK2 has been extensively investigated in terms of regulation of cardiac beta-adrenergic receptors, the substrate specificities of the two GRK isoforms at G protein-coupled receptors (GPCR) are poorly understood. In this study, the substrate specificities of GRK2 and GRK3 at GPC...

The influence of adrenergic drugs and electrical stimulation of the splanchnic nerves on concentrating function and motility in the feline gall bladder and on heptic bile secretion have been studied in vivo. It was found that electrical stimulation of the splanchnic nerves and adrenergic alpha-receptor stimulation increase the rate of net water absorption from the gall bladder lumen. Adrenergic...

Previous studies have shown that neural stimulation of brown adipose tissue (BAT) reorganizes the expression and activity of signaling proteins in the beta-adrenergic adenylyl cyclase pathway. Cold stress increases neural stimulation of BAT and increases alpha1-adrenergic receptor number; however, the alpha1 receptor subtype involved and the mechanism of up-regulation by cold stress have not be...

Increased sympathetic outflow from the central nervous system to the periphery may contribute to the initiation of hypertension in spontaneously hypertensive rats (SHR). As this alteration in sympathetic activity may be mediated in part by a-adrenergic receptors in the central nervous system, the current study examined aradrenergic receptors in various brain areas of SHR and normotensive Wistar...

beta-Adrenergic receptors play a critical role in signal transduction in the cardiovascular system. Regulation of beta-adrenergic receptor expression depends on multiple factors, including rates of synthesis and degradation of receptor protein and trafficking of receptors between the cell surface and putative intracellular compartments. To characterize the subcellular distribution of beta-adren...

Recent developments in the characterization of the adrenergic receptors have led to the identification and purification of the binding subunits of the various catecholamine receptors. beta-Adrenergic receptors have been identified in a wide variety of tissues by photoaffinity labeling with the antagonist [125I]p-azidobenzylcrazolol and have been purified to apparent homogeneity from several of ...

The presence of sex differences in myocardial β-adrenergic responsiveness is controversial, and limited studies have addressed the mechanism underlying these differences. Studies were performed using isolated perfused hearts from male, intact female and ovariectomized female mice to investigate sex differences and the effects of ovarian hormone withdrawal on β-adrenergic receptor function. Fema...