BACKGROUND Adenosine is an endogenous purine nucleoside that has a neuromodulatory role in the central nervous system. The amphetamine derivative (±)-3,4-methylenedioxymethamphetamine (MDMA or ecstasy) is a synthetic amphetamine analogue used recreationally to obtain an enhanced affiliated emotional response. MDMA is a potent monoaminergic neurotoxin with the potential of damage to brain neuron...

A panel of docking scaffolds was developed for the known molecular targets of the anticancer agents, thieno[2,3-b]pyridines, in order to glean insight into their mechanism of action. The reported targets are the copper-trafficking antioxidant 1 protein, tyrosyl DNA phosphodiesterase 1, the colchicine binding site in tubulin, adenosine A2A receptor, and, finally, phospholipase C-δ1. According to...

We characterized the in vivo cardiovascular profile of SCH 58261, 7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2, 4-triazolo[1,5-c] pyrimidine, a selective A2A adenosine receptor antagonist, in conscious, freely moving rats by use of the telemetry system. In normotensive rats, SCH 58261, at 10 mg/kg i.p., significantly (P < .05) inhibited hypotension and tachycardia induced by the A...

OBJECTIVES For determining the mechanism of anti-asthmatic effect of thymoquinone, this investigation evaluated the effect of thymoquinone in the presence of selective A2A and A2B adenosine receptor antagonists (ZM241385 and MRS1706, respectively). MATERIALS AND METHODS Seventy guinea pigs were randomly divided to 7 groups; control (C), sensitized with ovalbumin (S), sensitized groups pretrea...

BACKGROUND The inhibitory effect of adenosine on platelet aggregation is abrogated after the addition of adenosine-deaminase. Inosine is a naturally occurring nucleoside degraded from adenosine. OBJECTIVES The mechanisms of antiplatelet action of adenosine and inosine in vitro and in vivo, and their differential biological effects by molecular modeling were investigated. RESULTS Adenosine (...

BACKGROUND AND AIMS During fibrosis hepatic stellate cells (HSC) undergo activation, proliferation, and senescence but the regulation of these important processes is poorly understood. The adenosine A2A receptor (A2A) is known to be present on HSC, and its activation results in liver fibrosis. In this study, we tested if A2A has a role in the regulation of HSC proliferation, apoptosis, senescen...

According to the Gα subunit amino acid sequence homology, G proteins divide into four families that can couple to different GPCRs. To investigate the combination of interaction between G proteins (Gs, Gi/Go, q11 and 12/13) and A2A, D2R, or A2A/D2 respectively, Föster resonance energy transfer (FRET) and bimolecular fluorescence complementation (BiFC) assays, with the advantage to analyze protei...

Received: 19/Dec/2007, Accepted: 15/Mar/2008 Objective: It has been suggested that low frequency stimulation (LFS) exerts its inhibitory effect on epileptogenesis through adenosine receptors activation. In the present study, effect of different LFS frequencies on A1 and A2A receptors gene expression was investigated in perforant path kindled seizures. Materials and Methods: Animals were kindled...

In this opinion paper, we provide scientific-based reasons about the huge therapeutic potential of adenosine A2A receptor antagonists, and about the huge challenges to demonstrate efficacy in clinical trials, i.e., to provide data now required to approve a new medication by the regulatory bodies, such as U.S. Food and Drug Administration (FDA). Adenosine is an autacoid present in all tissue and...

Background The A2A adenosine receptor is a prototypical G proteincoupled receptor. It is expressed in a wide variety of cells including as different types as neurons, platelets, cells of the immune system and muscle. The cell-specific expression of the A2A adenosine receptor is controlled by at least three different upstream non-coding exons and their corresponding promotors. Compared to other ...