Hide and seek: a comparative autoradiographic in vitro investigation of the adenosine A3 receptor

European Journal of Nuclear Medicine and Molecular Imaging
Daniela HaeuslerMarkus Mitterhauser

Abstract

Since 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. For 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. Specific 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...Continue Reading

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Citations

Jan 26, 2016·British Journal of Pharmacology·K JanesD Salvemini
Jul 7, 2017·Medicinal Research Reviews·Kenneth A JacobsonStefania Gessi
Mar 19, 2020·Pain·Kenneth A JacobsonDaniela Salvemini
Nov 29, 2020·Scientific Reports·Kerry BarkanGraham Ladds
Nov 16, 2019·The Journal of Investigative Dermatology·Erika LisztesTamás Bíró

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