Results 301 to 310 of about 124,204 (359)

Allosteric modulation of A1-adenosine receptor: a review

Drug Discovery Today: Technologies, 2013
Allosteric modulators of adenosine receptors represent an alternative to direct-acting adenosine agonists and nucleoside uptake blockers, preferably those can selectively modulate the response to adenosine in only those organs or localized areas of a given organ in which production of adenosine is increased.
M. Kimatrai Salvador, BARALDI, Pier Giovanni, ROMAGNOLI, Romeo   +2 more
openaire   +3 more sources

Adenosine receptor modelling. A1/A2a selectivity

European Journal of Medicinal Chemistry, 2006
Three-dimensional models of the A(1) and A(2a) adenosine receptors (AR) were constructed by means of a homology procedure, using bovine rhodopsin as a template. In order to validate the two models, a docking analysis of selective agonists was carried out.
TUCCINARDI, TIZIANO, ORTORE, GABRIELLA MARIA PIA, MANERA, CLEMENTINA, SACCOMANNI, GIUSEPPE, MARTINELLI, ADRIANO   +4 more
openaire   +4 more sources

4 The Adenosine A1 Receptor and its Ligands

2009
Publisher Summary This chapter discusses the adenosine A1 receptor and its ligands. The adenosine A1 receptor is a G-protein-coupled receptor of about 36 kDa with even transmembrane domain structure. Adenosine and adenosine A1 receptors are involved in the modulation of several physiological effects in heart, kidney, CNS, and lipid metabolism ...
Barbara Albrecht-Küpper, Peter Nell
openaire   +2 more sources

Allosteric Enhancers for A1 Adenosine Receptor

Mini-Reviews in Medicinal Chemistry, 2007
Allosteric enhancers at the adenosine A(1) receptor have received attention as anti-arrhythmic cardiac agents, and, more recently, as anti-lipolytic agents. In addition, allosteric modulators at the adenosine A(1) receptor have therapeutic potential as analgesics and neuroprotective agents.
BARALDI, Pier Giovanni, IACONINOTO, Antonietta, MOORMAN AR, CARRION MD, CARA CL, PRETI, Delia, LOPEZ OC, FRUTTAROLO, Francesca, AGHAZADEH TABRIZI, Mojgan, ROMAGNOLI, Romeo   +9 more
openaire   +2 more sources

Inverse agonism at adenosine A1 receptors

International Congress Series, 2003
Abstract Inverse agonism at adenosine A1 receptors was studied in a variety of experimental set-ups. As a read-out, the binding of [35S]GTPγS to membranes of either CHO or COS-7 cells expressing human adenosine A1 receptors was used. When wild-type receptors were studied, inverse agonism could only be detected at higher levels of receptor expression.
Anna Lorenzen, Rianne A.F de Ligt, Adriaan P. IJzerman   +2 more
openaire   +2 more sources

Abolished tubuloglomerular feedback and increased plasma renin in adenosine A1 receptor-deficient mice.

American Journal of Physiology. Regulatory Integrative and Comparative Physiology, 2001
The hypothesis that adenosine acting on adenosine A1 receptors (A1R) regulates several renal functions and mediates tubuloglomerular feedback (TGF) was examined using A1R knockout mice.
Russell D. Brown, A. Ollerstam, Björn Johansson, Ole Skøtt, Samuel Gebre-Medhin, B. Fredholm, A. Persson   +6 more
semanticscholar   +1 more source

The A1 adenosine receptor as a new player in microglia physiology

Glia, 2013
The purinergic system is highly involved in the regulation of microglial physiological processes. In addition to the accepted roles for the P2X4,7 and P2Y12 receptors activated by adenosine triphosphate (ATP) and adenosine diphosphate, respectively, recent evidence suggests a role for the adenosine A2A receptor in microglial cytoskeletal rearrangements.
LUONGO, Livio, GUIDA, Francesca, Imperatore R, Napolitano F, Gatta L, Cristino L, Giordano C, Siniscalco D, Di Marzo V, BELLINI, Giulia, Petrelli R, Cappellacci L, USIELLO, Alessandro, DE NOVELLIS, Vito, ROSSI, Francesca, MAIONE, Sabatino   +15 more
openaire   +4 more sources

Effects of enprofylline on A1 and A2 adenosine receptors

European Journal of Pharmacology, 1985
The effects of enprofylline were studied on A1 adenosine receptors of rat fat cells and on A2 adenosine receptors of human platelets and of guinea-pig lung. Enprofylline antagonized the 5'-N-ethylcarboxamidoadenosine (NECA)-induced stimulation of platelet adenylate cyclase activity with a KB of 130 microM.
Ulrich Schwabe, Dieter Ukena, Carl Georg Schirren   +2 more
openaire   +3 more sources

The structure and function of A1 and A2B adenosine receptors

Life Sciences, 1998
Of the four G protein coupled adenosine receptor (AR) subtypes, the A1 is best suited for studies of reconstitution with G proteins. Recombinant A1 receptors extended with hexahistidine and FLAG have been purified to near homogeneity. In reconstitution assays using pure recombinant G protein subunits, the composition of the gamma subunit influences ...
Joel Linden, Robert A. Figler, John A. Auchampach, Xiaowei Jin   +3 more
openaire   +3 more sources

Medicinal Chemistry of Adenosine A1 Receptor Ligands

Current Topics in Medicinal Chemistry, 2003
In this review the latest developments in ligand design for the adenosine A(1) receptor are summarized. Novel series of agonists and antagonists are discussed, leading to the conclusion that ligands truly selective for the human adenosine A(1) receptor are still scarce.
Ad P. IJzerman, Ineke Van Wijngaarden, Willem Soudijn   +2 more
openaire   +3 more sources