Results 241 to 250 of about 34,994 (277)

Medicinal Chemistry of A2A Adenosine Receptor Antagonists

Current Topics in Medicinal Chemistry, 2003
Due to the clearly demonstrated receptor-receptor interaction between adenosine A(2A) and dopamine D(2) receptors in the basal ganglia, the discovery and development of potent and selective A(2A)adenosine receptor antagonists became, in the last ten years, an attractive field of research to discovery new drugs for the treatment of neurodegenerative ...
B. CACCIARI, G. PASTORIN, SPALLUTO, GIAMPIERO   +2 more
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Adenosine A_2Areceptors and depression

Neurology, 2003
Adenosine and its analogues have been shown to induce "behavioral despair" in animal models believed to be relevant to depression. Recent data have shown that selective adenosine A2A receptor antagonists (e.g., SCH 58261, ZM241385, and KW6002) or genetic inactivation of the receptor was effective in reversing signs of behavioral despair in the tail ...
El Yacoubi, Malika, Costentin, Jean, Vaugeois, Jean-Marie   +2 more
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Adenosine enhances glial glutamate efflux via A2a adenosine receptors

Life Sciences, 2001
The present study investigated the effect of adenosine on glial glutamate efflux. Adenosine (from 1 nM to 100 microM) enhanced the release from cultured rat glial cells in a bell-shaped dose-responsive manner for the hippocampus and in a dose-dependent manner for the superior colliculus, and a similar increase was obtained with the A2a adenosine ...
X X, Li, T, Nomura, H, Aihara, T, Nishizaki   +3 more
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The A2A Adenosine Receptor Mediates Coronary Vasodilation

The Journal of Pharmacology and Experimental Therapeutics, 1998
The coronary vasodilation caused by adenosine is due to activation of A2 adenosine receptors (A2AdoRs), but the subtype or subtypes of A2AdoR (A2A and/or A2B) that mediate this action are uncertain. The purpose of this study was to test the hypothesis that A2AAdoRs mediate coronary vasodilation caused by exogenous or endogenous adenosine in the guinea ...
L, Belardinelli, J C, Shryock, S, Snowdy, Y, Zhang, A, Monopoli, G, Lozza, E, Ongini, R A, Olsson, D M, Dennis   +8 more
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Recent Developments in Adenosine A2A Receptor Ligands

2009
The development of potent and selective agonists and antagonists of adenosine receptors (ARs) has been a target of medicinal chemistry research for several decades, and recently the US Food and Drug Administration has approved Lexiscan, an adenosine derivative substituted at the 2 position, for use as a pharmacologic stress agent in radionuclide ...
CRISTALLI, Gloria, Müller CE, VOLPINI, Rosaria   +2 more
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Binding thermodynamics at A1 and A2a adenosine receptors

Life Sciences, 1996
Only recently the binding equilibrium of a number of ligands at adenosine A1 and A2a receptors has been analyzed from a thermodynamic point of view. This approach presents the advantage, with respect to usual affinity constant measurements, of a greater capability to give information about the molecular mechanisms underlying the binding process.
BOREA, Pier Andrea, DALPIAZ, Alessandro, VARANI, Katia, GESSI, Stefania, GILLI, Gastone   +4 more
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Adenosine A2A Receptor Antagonists

2014
This chapter summarizes and updates the work on adenosine A2A receptor antagonists for Parkinson’s disease. Adenosine A2A receptor antagonists were, and still are, a promising non-dopaminergic approach for the potential treatment of Parkinson’s disease.
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Binding thermodynamics of adenosine A2a receptor ligands

Biochemical Pharmacology, 1995
The thermodynamic parameters delta G degree, delta H degree, and delta S degree of the binding equilibrium of seven adenosine agonists and five xanthine antagonists binding specifically to adenosine A2a receptors were determined by means of affinity measurements at six different temperatures (0, 10, 20, 25, 30 and 35 degrees) and van't Hoff plots ...
BOREA, Pier Andrea, DALPIAZ, Alessandro, VARANI, Katia, Guerra L., GILLI, Gastone   +4 more
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Characterization of the Rat A2a Adenosine Receptor Gene

DNA and Cell Biology, 1996
To understand the molecular basis for the regulation of rat A2a adenosine receptor (A2a-R) expression, we have characterized the rat A2a-R gene and defined its promoter regions. Through a combination of restriction mapping and sequence analysis, we have demonstrated that the rat A2a-R gene is composed of two exons interrupted by a 7.2-kb intron. Primer
Y Y, Chu, K H, Tu, Y C, Lee, Z J, Kuo, H L, Lai, Y, Chern   +5 more
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Striatal adenosine A2A receptors

1998
The nucleoside adenosine exerts a modulatory action in the central nervous system by activating G-protein coupled receptors. Four such receptors are cloned and pharmacologically characterized: A1, A2A, A2B and A3. Caffeine, the most widely consumed psychostimulant, acts as an adenosine receptor antagonist predominantly on the first two.
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