| http://purl.uniprot.org/citations/35162950 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/35162950 | http://www.w3.org/2000/01/rdf-schema#comment | "A2A adenosine receptors (A2A-AR) have a cardio-protective function upon ischemia and reperfusion, but on the other hand, their stimulation could lead to arrhythmias. Our aim was to investigate the potential use of the PET radiotracer [18F]FLUDA to non-invasively determine the A2A-AR availability for diagnosis of the A2AR status. Therefore, we compared mice with cardiomyocyte-specific overexpression of the human A2A-AR (A2A-AR TG) with the respective wild type (WT). We determined: (1) the functional impact of the selective A2AR ligand FLUDA on the contractile function of atrial mouse samples, (2) the binding parameters (Bmax and KD) of [18F]FLUDA on mouse and human atrial tissue samples by autoradiographic studies, and (3) investigated the in vivo uptake of the radiotracer by dynamic PET imaging in A2A-AR TG and WT. After A2A-AR stimulation by the A2A-AR agonist CGS 21680 in isolated atrial preparations, antagonistic effects of FLUDA were found in A2A-AR-TG animals but not in WT. Radiolabelled [18F]FLUDA exhibited a KD of 5.9 ± 1.6 nM and a Bmax of 455 ± 78 fmol/mg protein in cardiac samples of A2A-AR TG, whereas in WT, as well as in human atrial preparations, only low specific binding was found. Dynamic PET studies revealed a significantly higher initial uptake of [18F]FLUDA into the myocardium of A2A-AR TG compared to WT. The hA2A-AR-specific binding of [18F]FLUDA in vivo was verified by pre-administration of the highly affine A2AAR-specific antagonist istradefylline. Conclusion: [18F]FLUDA is a promising PET probe for the non-invasive assessment of the A2A-AR as a marker for pathologies linked to an increased A2A-AR density in the heart, as shown in patients with heart failure."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.org/dc/terms/identifier | "doi:10.3390/ijms23031025"xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Hofmann B."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Lai T.H."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Neumann J."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Boknik P."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Toussaint M."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Gergs U."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Deuther-Conrad W."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Brust P."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Kopka K."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Dukic-Stefanovic S."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Teodoro R."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Gundel D."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/author | "Moldovan R.P."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/date | "2022"xsd:gYear |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/name | "Int J Mol Sci"xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/pages | "1025"xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/title | "Non-Invasive Assessment of Locally Overexpressed Human Adenosine 2A Receptors in the Heart of Transgenic Mice."xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://purl.uniprot.org/core/volume | "23"xsd:string |
| http://purl.uniprot.org/citations/35162950 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/35162950 |
| http://purl.uniprot.org/citations/35162950 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/35162950 |
| http://purl.uniprot.org/uniprot/#_A8K1F6-mappedCitation-35162950 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/35162950 |
| http://purl.uniprot.org/uniprot/#_A7UAQ1-mappedCitation-35162950 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/35162950 |