ArticleEuropean journal of nuclear medicine and molecular imaging2015
Hide and seek: a comparative autoradiographic in vitro investigation of the adenosine A3 receptor.
Article in European journal of nuclear medicine and molecular imaging, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 19 citations in OpenAlex.
- Adenosine receptors in breast cancer.Molecular biology reports · 2024Review
- Species dependence of APurinergic signalling · 2023Review
- Pharmacological characterisation of novel adenosine AScientific reports · 2020Article
- Adenosine AJournal of neuroinflammation · 2020Article
- Article
- AMedicinal research reviews · 2018Review
- Identification of A3 adenosine receptor agonists as novel non-narcotic analgesics.British journal of pharmacology · 2016Review
- Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R.Frontiers in cellular neuroscience · 2015Article
- Article
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
Abstract
purposeSince the adenosine A3 receptor (A3R) is considered to be of high clinical importance in the diagnosis and treatment of ischaemic conditions (heart and brain), glaucoma, asthma, arthritis, cancer and inflammation, a suitable and selective A3R PET tracer such as [(18)F]FE@SUPPY would be of high clinical value for clinicians as well as patients. A3R was discovered in the late 1990s, but there is still little known regarding its distribution in the CNS and periphery. Hence, in autoradiographic experiments the distribution of A3R in human brain and rat tissues was investigated and the specific binding of the A3R antagonist FE@SUPPY and MRS1523 compared. Immunohistochemical staining (IHC) experiments were also performed to validate the autoradiographic findings.
methodsFor autoradiographic competition experiments human post-mortem brain and rat tissues were incubated with [(125)I]AB-MECA and highly selective compounds to block the other adenosine receptor subtypes. Additionally, IHC was performed with an A3 antibody.
resultsSpecific A3R binding of MRS1523 and FE@SUPPY was found in all rat peripheral tissues examined with the highest amounts in the spleen (44.0% and 46.4%), lung (44.5% and 45.0%), heart (39.9% and 42.9%) and testes (27.4% and 29.5%, respectively). Low amounts of A3R were found in rat brain tissues (5.9% and 5.6%, respectively) and human brain tissues (thalamus 8.0% and 9.1%, putamen 7.8% and 8.2%, cerebellum 6.0% and 7.8%, hippocampus 5.7% and 5.6%, caudate nucleus 4.9% and 6.4%, cortex 4.9% and 6.3%, respectively). The outcome of the A3 antibody staining experiments complemented the results of the autoradiographic experiments.
conclusionThe presence of A3R protein was verified in central and peripheral tissues by autoradiography and IHC. The specificity and selectivity of FE@SUPPY was confirmed by direct comparison with MRS1523, providing further evidence that [(18)F]FE@SUPPY may be a suitable A3 PET tracer for use in humans.
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