scholarly journals Adenosine A1, A2a, A2b, and A3 Receptors in Hematopoiesis. 1. Expression of Receptor mRNA in Four Mouse Hematopoietic Precursor Cells

2010 ◽  
pp. 133-137
Author(s):  
D Štreitová ◽  
L Šefc ◽  
F Savvulidi ◽  
M Pospíšil ◽  
J Holá ◽  
...  
Keyword(s):  
Precursor Cells ◽  
Receptor Subtypes ◽  
Mouse Bone Marrow ◽  
Thymus Cell ◽  
Receptor Mrna ◽  
A2a Receptor ◽  
A2b Receptor ◽  
Adenosine A1 ◽  
Hematopoietic Precursor ◽  
A1 Receptor

Four mouse bone marrow or thymus cell populations, namely granulopoietic/monocytopoietic, erythropoietic, B-lymphopoietic, and T-lymphopoietic precursor cells have been assayed by RTPCR technique for the presence and relative amounts of adenosine A1, A2a, A2b, and A3 receptor mRNA. It has been found that (i) all four populations studied express all four adenosine receptor subtypes, (ii) the A1 receptor is the least expressed in all populations studied, (iii) the A3 receptor is markedly expressed in the populations of granulopoietic/monocytopoietic and erythropoietic cells, (iv) the A2a receptor is markedly expressed in the populations of B-lymphopoietic and T-lymphopoietic cells, and v) the A2b receptor does not predominate in any of the precursor cells studied. Our data offer a new possibility for the assessment of the readiness of these cells to respond, by receptor-mediated mechanisms, to adenosine or its analogs present in the tissues as a result of endogenous processes and/or following their administration.

scholarly journals Adenosine A1, A2a, A2b, and A3 Receptors in Hematopoiesis. 2. Expression of Receptor mRNA in Resting and LipopolysaccharideActivated Mouse RAW 264.7 Macrophages

2010 ◽  
pp. 139-144
Author(s):  
D Štreitová ◽  
M Hofer ◽  
J Holá ◽  
A Vacek ◽  
M Pospíšil
Keyword(s):  
Adenosine Receptor ◽  
Point Of View ◽  
Receptor Subtypes ◽  
Raw 264.7 ◽  
Raw 264.7 Macrophages ◽  
Receptor Mrna ◽  
Adenosine A1 ◽  
A1 Receptor ◽  
Polymerase Chain ◽  
Receptor Mrnas

Expression of mRNA for adenosine receptor subtypes A1, A2a, A2b, and A3 in normal and lipopolysaccharide (LPS)-activated murine RAW 264.7 macrophages has been investigated using the method of quantitative real-time polymerase chain reaction. The results have shown a very low, unquantifiable expression of adenosine A1 receptor mRNA in both normal and LPS-activated macrophages. The other three adenosine receptor mRNAs have been found to be expressed at various but always quantifiable levels. Activation of the macrophages by LPS induced upregulation of the expression of adenosine receptor A2a and A2b mRNA, whereas the expression of adenosine receptor A3 mRNA was downregulated. Unstimulated macrophages exhibited a high expression of the A2b adenosine receptor mRNA. The findings are discussed from the point of view of the antiinflammatory and hematopoiesis-stimulating roles of the adenosine receptor signaling.

Opposite changes in adenosine A1 and A2A receptor mRNA in the rat following sleep deprivation

Neuroreport ◽  
2001 ◽  
Vol 12 (8) ◽  
pp. 1577-1580 ◽  
Author(s):  
Radhika Basheer ◽  
Linda Halldner ◽  
Lauri Alanko ◽  
Robert W. McCarley ◽  
Bertil B. Fredholm ◽  
...  
Keyword(s):  
Sleep Deprivation ◽  
Receptor Mrna ◽  
A2a Receptor ◽  
Adenosine A1

scholarly journals Desensitisation of the Adenosine A1 Receptor by the A2A Receptor in the Rat Striatum

2002 ◽  
Vol 69 (1) ◽  
pp. 315-321 ◽  
Author(s):  
Alistair K. Dixon ◽  
Leon Widdowson ◽  
Peter J. Richardson
Keyword(s):  
Adenosine A1 Receptor ◽  
Rat Striatum ◽  
A2a Receptor ◽  
Adenosine A1 ◽  
A1 Receptor

scholarly journals Die adenosien A1- en A2A-reseptoraffiniteit van ’n reeks 3,4-dihidropirimidoon-analoë

2017 ◽  
Vol 36 (1) ◽  
Author(s):  
Runako M. Katsidzira ◽  
Mietha M. Van der Walt ◽  
Jacobus J. Bergh ◽  
Gisella Terre’Blanche
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Adenosine A2a Receptor ◽  
Adenosine A1 Receptor ◽  
Receptor Affinity ◽  
A2a Receptors ◽  
A2a Receptor ◽  
Adenosine A1 ◽  
A1 Receptor ◽  
Adenosine A2a

Parkinson’s disease is a complex neurodegenerative condition with current treatment only focussed on symptomatic therapy that does not slow or stop the progression of the disease. Since the discovery that adenosine A1 and A2A receptors are potential drug targets for the therapy of Parkinson’s disease, various research groups have attempted to identify adenosine antagonists. So the possibility exists that the administration of an adenosine A2A receptor antagonist may prevent further neurodegeneration. Furthermore, the antagonism of adenosine A1 receptors has the potential of treating Parkinson’s disease-associated cognitive deficits. Therefore, dual antagonism of adenosine A1 and A2A receptors would be of great benefit since this would potentially treat both the motor as well as the cognitive impairment associated with Parkinson’s disease. Based on the observation that a series of 1,4-dihydropyridine derivatives possess adenosine A1 and A2A receptor affinity, the current study investigated the potential of the structurally related 3,4-dihydropyrimidone analogues as adenosine A1 and A2A receptor antagonists. Overall, the 3,4-dihyropyrimidone analogues were found to possess weak affinity for the adenosine A2A receptor, but more promising adenosine A1 receptor affinity was found, ranging in the low micromolar range. Among the investigated compounds, the p-bromophenyl substituted dihydropyrimidone (6b) possesses the best adenosine A1 receptor affinity with a Ki value of 7.39 µM. In conclusion, this 3,4-dihydropyrimidone derivative can be used as a lead for the design of novel adenosine A1 receptor antagonists, although further structural modifications are required to enhance the adenosine A2A receptor affinity before a clinically viable candidate will be available as potential treatment of Parkinson’s disease.

scholarly journals 2–Benzylidene–1–Indanone Analogues as Dual Adenosine A1/A2a Receptor Antagonists for the Potential Treatment of Neurological Conditions

Drug Research ◽  
2019 ◽  
Vol 69 (07) ◽  
pp. 382-391 ◽  
Author(s):  
HelenaDorathea Janse van Rensburg ◽  
LesetjaJ. Legoabe ◽  
Gisella Terre’Blanche ◽  
MiethaM. Van der Walt
Keyword(s):  
Radioligand Binding ◽  
Aldol Condensation ◽  
Adenosine A1 Receptor ◽  
Potential Treatment ◽  
Receptor Antagonists ◽  
A2a Receptor ◽  
Adenosine A1 ◽  
A1 Receptor ◽  
Neurological Conditions ◽  
Aldol Condensation Reactions

AbstractPrevious studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson’s disease. This study’s aim is to investigate structurally related 2-benzylidene-1-indanones with substitutions on ring A and B as novel, potent and selective adenosine A1 and A2A receptor blockers. 2-Benzylidene-1-indanone derivatives were synthesised via acid catalysed aldol condensation reactions and evaluated via radioligand binding assays to ascertain structure activity relationships to govern A1 and A2A AR affinity. The results indicated that hydroxy substitution at C4 of ring A and meta (3’), or para (4’) substitution on ring B of the 2-benzylidene-1-indanone scaffold (2c) is preferred over substitution at C5 (2d) or C6 (2e) of ring A for adenosine A1 receptor activity and selectivity in the micromolar range. Furthermore, substitution at the meta (3’) position of ring B with chlorine lead to the highly potent and selective adenosine A2A receptor antagonist, compound 2 h. Compound 2c and the 2q behaved as adenosine A1 receptor antagonists in the performed GTP shift assays. In view of these findings, compounds 2c, 2 h, 2q and 2p are potent and selective adenosine A1 and A2A receptor antagonists for the potential treatment of neurological conditions.

Inosine Reduces Pain-Related Behavior in Mice: Involvement of Adenosine A1 and A2A Receptor Subtypes and Protein Kinase C Pathways

2010 ◽  
Vol 334 (2) ◽  
pp. 590-598 ◽  
Author(s):  
Francisney P. Nascimento ◽  
Sonia M. Figueredo ◽  
Rodrigo Marcon ◽  
Daniel F. Martins ◽  
Sérgio J. Macedo ◽  
...  
Keyword(s):  
Protein Kinase C ◽  
Protein Kinase ◽  
Receptor Subtypes ◽  
Kinase C ◽  
A2a Receptor ◽  
Adenosine A1
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