We investigated the expression of a1-adrenergic receptor subtypes in intact human peripheral blood lymphocytes using reverse transcription–polymerase chain reaction (RT-PCR) and radioligand binding assay techniques combined with antibodies against the three subtypes of a1-adrenergic receptors (a1A, a1B, and a1D). RT-PCR amplified in peripheral blood lymphocytes a 348-bp a1A-adrenergic receptor ...

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...

The role of adenosine A1 and A3 receptors in mediating cardioprotection has been studied predominantly in rabbits, yet the pharmacological characteristics of rabbit adenosine A1 and A3 receptor subtypes are unknown. Thus, the rabbit adenosine A3 receptor was cloned and expressed, and its pharmacology was compared with that of cloned adenosine A1 receptors. Stable transfection of rabbit A1 or A3...

Several studies show that different neurotransmitter receptor systems may interact with each other, for example, by means of a shared pool of G-proteins coupled to these receptors. Along these lines, there are data suggesting cross-talk between the adenosine and serotonin receptor systems. Such an interaction between these two receptor systems may also emerge under conditions of sleep loss whic...

Partial adenosine A1 receptor agonists with reduced intrinsic activity at the cardiovascular system would be promising for therapeutic application (e.g., as antilipolytic agents). In the present study a series of 8-alkylamino [methyl (M)-, ethyl (E)-, propyl (P)-, butyl (B)- and cyclopentyl (CP)-] derivatives of N6-cyclopentyladenosine (CPA) were investigated in conscious normotensive rats. Aft...

The influence of adenosine receptor agonists and antagonists on cocaine--induced conditioned place preference (CPP) was examined in male Wistar rats. Adenosine receptor agonists, when given alone, induced place preference in some dose ranges, and it seems that adenosine A1 and A2 receptors might be involved in this reaction. All adenosine receptor agonists: 2-p-(2-carboxyethyl)phenethylamino-5'...

The A1-adenosine receptor (A1-AR) is a G protein-coupled receptor that mediates many of the physiological effects of adenosine in the brain, heart, kidney, and adipocytes. Currently, ligand interactions with the A1-AR can be quantified on large cell populations only by using radioligand binding. To increase the resolution of these measurements, we have designed and characterized a previously un...

introduction: activity of the paragigantocellularis (pgi) nucleus located in the rostral ventrolateral medulla is the mediator of dependence, tolerance and withdrawal syndrome. the most important systems which change their activity during morphine consumption include glutaminergic, opioidergicand purinergic (especially adenosine) receptors in the pgi nucleus. however, it has been shown that the...

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 have previously reported that in several renal cell types, adenosine receptor agonists inhibit adenylyl cyclase and activate phospholipase C via a pertussis toxin-sensitive G protein. In the present study, in 28A cells, both of these adenosine receptor-mediated responses were inhibited by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX), a highly selective A1 adenosine receptor antagonist. The bin...