[In vivo investigation of the A2A adenosine receptor distribution using the [11C]-CSC radioligand].
A 11C labeled selective adenosine A2A antagonist, (E)-8-(3-chlorostyryl)-1,3-dimethyl-7-[11C]-methylxanthine [(11C)-CSC] was prepared reacting (E)-8-(3-chlorostyryl)-1,3,-dimethylxanthine and [11C]-methyl iodide. A primary evaluation of [11C]-CSC as a potential tracer for mapping adenosine A2A receptors by positron emission tomography (PET) was also presented. Autoradiographic studies were carried out on Swiss mice. A high level accumulation of radioactivity was observed in the striatum and medulla oblongata in accordance with previous findings on the specific spatial distribution of A2A adenosine receptors. Dynamic PET studies on rabbits showed a fast brain uptake of CSC, reaching a maximum in less than 2 minutes. Competition experiments with the unlabeled ligand proved [11C]-CSC to bind specifically to the appropriate receptor.
Boros
István
I
Debreceni Egyetem, Orvos- és Egészségtudományi Centrum, PET Centrum, Debrecen.
Lengyel
Zsolt
Z
Balkay
László
L
Horváth
Géza
G
Szentmiklósi
A József
AJ
Fekete
István
I
Márián
Teréz
T
D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000378:metabolism*; D002110:Caffeine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D002250:Carbon Radioisotopes; D002460:Cell Line; D007553:Isotope Labeling / Q000379:methods; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D051379:Mice; D009130:Muscle, Smooth / Q000166:cytology / Q000378:metabolism*; D011817:Rabbits; D011869:Radioligand Assay / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D043705:Receptor, Adenosine A2A; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed / Q000379:methods*; D001743:Urinary Bladder / Q000378:metabolism
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D043705:Receptor, Adenosine A2A; D018047:Receptors, Purinergic P1; C081320:8-(3-chlorostyryl)caffeine; D002110:Caffeine