The behavioral profile of a range of adenosine receptor ligands was examined in rats using a locomotor activity model. Adenosine receptor agonists, including the selective A1 receptor agonist, N6-cyclopentyladenosine (CPA) and the A2A agonist, 2-[(2-aminoethylamino)carbonylethyl-phenylethylamino]- 5'-ethylcarboxa midoadenosine (APEC), reduced spontaneous motor activity in a dose-dependent manne...

Adenosine is a potent endogenous anti-inflammatory agent released by cells in metabolically unfavorable conditions, such as hypoxia or ischemia. Adenosine modulates different functional activities in macrophages. Some of these activities are believed to be induced through the uptake of adenosine into the macrophages, while others are due to the interaction with specific cell surface receptors. ...

Abstract Background Adenosine signaling is now an accepted explanation for the therapeutic mechanism of Methotrexate (MTX) in rheumatoid arthritis (RA). receptors categorized into four subclasses: adenosine A1 receptor (ADORA1), 2a (ADORA2a), 2b (ADORA2B), and 3 (ADORA3). Our aim to check mRNA expression two receptors; ADORA2a ADORA3 whole blood cell RA patients its relation prediction MTX clin...

The purine nucleoside adenosine is a physiologically important molecule in the heart. Brief exposure of cardiomyocytes to hypoxic challenge results in the production of extracellular adenosine, which then interacts with adenosine receptors to activate compensatory signaling pathways that lead to cellular resistance to subsequence hypoxic challenge. This phenomenon is known as preconditioning (P...

The effect of adenosine receptor ligands on dizocilpine-induced locomotion was studied in mice. Dizocilpine-induced hyperactivity (0.1 mg/kg i.p.) in mice was antagonized by all adenosine receptor agonists: CPA--A1 receptor agonist, CGS 21680--A2 receptor agonist, and NECA--A1/A2 receptor agonist, but the effect of NECA was the most apparent. Locomotion induced by the threshold dose of dizocilp...

Cell-permeable orthosteric ligands can assist folding of G protein-coupled receptors in the endoplasmic reticulum (ER); this pharmacochaperoning translates into increased cell surface levels of receptors. Here we used a folding-defective mutant of human A1-adenosine receptor as a sensor to explore whether endogenously produced adenosine can exert a chaperoning effect. This A1-receptor-Y(288)A w...

We describe the immunocytochemical distribution of adenosine A1 receptors in the rat hippocampus. Adenosine A1 receptor-like immunoreactivity was seen on the cell soma and dendrites of pyramidal cells and the cell soma and proximal part of dendrites of granule cells, but not on glial cells. Developmentally, adenosine A1 receptor-like immunoreactivity was diffuse on postnatal day 7 and increased...

Adenosine has several functions within the CNS that involve an inhibitory tone of neurotransmission and neuroprotective actions in pathological conditions. The understanding of adenosine production and release in the brain is therefore of fundamental importance and has been extensively studied. Conflicting results are often obtained regarding the cellular source of adenosine, the stimulus that ...

Objective: To develop Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) method for the estimation of adenosine A 1 receptor mRNA levels in rat kidney. Material and Methods: Total cellular RNA was isolated from whole rat kidney by small-scale total RNA preparation protocol and it was reverse transcribed into cDNA. The cDNA was subjected to PCR amplification using gen specific primers. The...