Results 21 to 30 of about 127,904 (323)

Transient and selective blockade of adenosine A1-receptors by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) causes sustained epileptiform activity in hippocampal CA3 neurons of guinea pigs [PDF]

, 1989
The effects of endogenously released adenosine on the excitability of hippocampal neurons were studied using the novel and highly selective adenosine A1-receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX).
Alzheimer, Christian, Sutor, Bernd, Ten Bruggencate, Gerrit   +2 more
core   +1 more source

Peripheral Antinociception by Carbamazepine in an Inflammatory Mechanical Hyperalgesia Model in the Rat: a New Target for Carbamazepine?

Journal of Pharmacological Sciences, 2006
.: This study investigated whether carbamazepine could produce local peripheral antinociception in a rat model of inflammatory mechanical hyperalgesia, and whether adenosine receptors are involved. Carbamazepine (100 – 1000 nmol/paw) coadministrated with
Sonja Vučković, Maja Tomić, Radica Stepanović-Petrović, Nenad Ugrešić, Milica Prostran, Bogdan Bošković   +5 more
doaj   +1 more source

Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization [PDF]

, 2013
Keywords:adenosine;allosterism;receptor;GPCR;dimerization;biased signalling The purine nucleoside adenosine is present in all cells in tightly regulated concentrations. It is released under a variety of physiological and pathophysiological conditions to
Albrecht-Kupper, Alexander, Amoah-Apraku, Aurelio, Aurelio, Avlani, Azzi, Baker, Baker, Bar-Yehuda, Bar-Yehuda, Baraldi, Baraldi, Barbhaiya, Briddon, Bruns, Bruns, Carr, Casadó, Chandrasekera, Chen, Chiavegatta, Chien, Christopoulos, Christopoulos, Chung, Ciruela, Clark, Cohen, Cordeaux, Corriden, Corriden, Cristovao-Ferreira, Dowling, Du, Dubey, Ellis, Fishman, Franco, Fredholm, Gao, Gao, Gao, Gao, Ge, Gessi, Goedeke, Goldman, Graaf, Gracia, Gracia, Griffin, Göblyös, Göblyös, Han, Harrison, Heitman, Hern, Hu, Ilien, Jaakola, Jacobson, Jacobson, Janusz, Kenakin, Kenakin, Keov, Kimatrai-Salvador, Klaft, Klein, Knapp, Kostenis, Kourounakis, Kuszak, Langemeijer, Lazareno, Lee, Lee, Lee, Limbird, Liu, Madi, Mares, Matherne, May, May, May, May, McCrea, Meno, Merighi, Morrison, Muller, Nikolakopoulos, Park, Peeters, Pisterzi, Rasmussen, Romagnoli, Roth, Salvatore, Smith, Sowa, Springael, Street, Suzuki, Swaminath, Tendera, Tinney, Uematsu, Urizar, Valant, Whalen, Williams, Xu   +114 more
core   +2 more sources

Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor

Scientific Reports, 2018
Despite intense interest in designing positive allosteric modulators (PAMs) as selective drugs of the adenosine A1 receptor (A1AR), structural binding modes of the receptor PAMs remain unknown.
Yinglong Miao, A. Bhattarai, A. T. Nguyen, A. Christopoulos, L. May   +4 more
semanticscholar   +1 more source

Pharmacological Characterization of FR194921, a New Potent, Selective, and Orally Active Antagonist for Central Adenosine A1 Receptors

Journal of Pharmacological Sciences, 2004
Adenosine A1 receptors in the brain are believed to play an important role in brain functioning. We have discovered a novel adenosine A1 receptor antagonist, FR194921 (2-(1-methyl-4-piperidinyl)-6-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-3(2H)-pyridazinone),
Takuya Maemoto, Miho Tada, Takuma Mihara, Noriko Ueyama, Hideaki Matsuoka, Katsuya Harada, Takayuki Yamaji, Kiyoharu Shirakawa, Satoru Kuroda, Atsushi Akahane, Akinori Iwashita, Nobuya Matsuoka, Seitaro Mutoh   +12 more
doaj   +1 more source

Evidence for the presence of A1 adenosine receptors in the aorta of spontaneously hypertensive rats [PDF]

, 2001
1 Isolated aortic rings (endothelium-intact and -denuded) from spontaneously hypertensive (SHR) and Wistar-Kyoto (WKY) rats were used in this study to examine the vasoactive e ects of various adenosine analogues.
AUCH-SCHWELK, AZEVEDO, BARRETT, BELARDINELLI, BIAGGIONI, BRUNS, BRUNS, CAPARROTTA, CUSHING, EVANS, FAHIM, ILLES, KATUSIC, LAURENT, LEWIS, LI, LINDEN, LOCKETTE, LUSCHER, LUSCHER, MAKUJINA, MUSTAFA, NEELY, PARSONS, PRENTICE, RAMAGOPAL, SCHIEMANN, STOGGALL, TADDEI, TESFAMARIAM, TODOKI, TRIVEDI, VANGALEN   +32 more
core   +2 more sources

NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization

SLAS discovery : advancing life sciences R & D, 2019
Receptor internalization in response to prolonged agonist treatment is an important regulator of G protein–coupled receptor (GPCR) function. The adenosine A1 receptor (A1AR) is one of the adenosine receptor family of GPCRs, and evidence for its agonist ...
Mark Soave, B. Kellam, J. Woolard, S. Briddon, S. Hill   +4 more
semanticscholar   +1 more source

Degranulation of rat omental mast cells by A1 receptor agonists in vitro

Mediators of Inflammation, 1996
The haemodynamic effects of adenosine are thought to result in part from a release of mast cell amines via A3 receptor stimulation. To investigate the nature of the receptors involved in adenosine-induced mast cell degranulation in the rat isolated ...
A. M. Northover, B. J. Northover
doaj   +1 more source

Adenosine A1 Receptor Protects Against Cisplatin Ototoxicity by Suppressing the NOX3/STAT1 Inflammatory Pathway in the Cochlea

Journal of Neuroscience, 2016
Cisplatin is a commonly used antineoplastic agent that produces ototoxicity that is mediated in part by increasing levels of reactive oxygen species (ROS) via the NOX3 NADPH oxidase pathway in the cochlea.
Tejbeer Kaur, V. Borse, Sandeep Sheth, Kelly Sheehan, Sumana Ghosh, Srinivasan Tupal, S. Jajoo, D. Mukherjea, L. Rybak, V. Ramkumar   +9 more
semanticscholar   +1 more source

Disinhibition of hippocampal CA3 neurons induced by suppression of an adenosine A1 receptor-mediated inhibitory tonus: Pre- and postsynaptic components [PDF]

, 1993
Intracellular recordings were performed on hippocampal CA3 neuronsin vitro to investigate the inhibitory tonus generated by endogenously produced adenosine in this brain region.
Alzheimer, Alzheimer, Alzheimer, Alzheimer, Andreasen, Arai, Ault, Ault, B. Sutor, Bauer, Beavo, Beavo, Ben-Ari, Bruns, Bruns, C. Alzheimer, Chamberlin, Daly, Dragunow, Dragunow, Dunwiddie, Dunwiddie, Dunwiddie, Fredholm, G. Ten Bruggencate, Gerber, Greene, Greene, Haas, Hablitz, Hablitz, Jackisch, Johnston, Linden, Linden, Llinás, Lohse, Madison, Malenka, Meghji, Miles, Moraidis, Nicholson, Pockett, Prestwich, Prince, Scholz, Schubert, Schubert, Smellie, Smellie, Smith, Snyder, Snyder, Sutor, Tanaka, Thompson, Thompson, Van Calker, Williams, Zetterström   +60 more
core   +1 more source