Relative Uptake, Metabolism, and β-Receptor Binding of (1R,2S)-4
Por um escritor misterioso
Last updated 29 maio 2024
The objective of the study was to compare relative uptake, metabolism, and β-receptor affinity of the new positron-emitting uptake-1 tracer (1 R ,2 S )-4-18F-fluorometaraminol (4-FM) with those of the SPECT pharmaceutical meta-123I-iodobenzylguanidine (MIBG) in Wistar Kyoto (WKY) rats and spontaneously hypertensive (SHR) rats. Methods: No-carrier-added 4-18F-FM was applied to SHR and WKY rats in vivo and to retrogradely perfused hearts in vitro. Cardiac and extracardiac distribution was assessed, and metabolite formation was determined by thin-layer chromatography. The in vivo experiments were repeated with no-carrier-added 123I-MIBG. By means of autoradiography, the β-receptor affinity of 4-FM was compared with that of MIBG and propranolol (10 μmol/L) through displacement of 125I-iodocyanopindolol (1.5 pmol/L) in slices of heart and spleen. Results: Cardiomyopathic hearts showed heterogeneous 4-18F-FM uptake with gradients up to 3.6 in vivo and in vitro between different regions of the heart. Control hearts showed such gradients in 4-18F-FM uptake only in vitro. 123I-MIBG exhibited a less heterogeneous in vivo distribution in SHR hearts. Extracardiac differences between WKY and SHR were found for uptake of 4-18F-FM in the spleen (63.3% ± 4% vs. 38.8% ± 5.7% of cardiac activity) and for renal uptake of 123I-MIBG (373% ± 27% vs. 81.4% ± 17% of cardiac activity). Metabolites of 4-18F-FM were found only in the liver and those of 123I-MIBG were found in the liver and kidney with a nearly equal relative fraction in both types of animals of about 20%, 60%, and 30%, respectively. 4-FM suppressed cardiac-specific β-receptor binding of 125I-iodocyanopindolol in heart and spleen of both types of animals significantly, whereas MIBG had almost no effect. Conclusion: The more heterogeneous cardiac distribution of 4-18F-FM suggests that it reflects alterations in uptake-1 better than 123I-MIBG in addition to the possibility of quantification and higher spatial resolution by PET compared with SPECT. Altered biotransformation in cardiomyopathic diseases may also impair the evaluation of 123I-MIBG-SPECT data. The β-receptor binding of 4-18F-FM must be further elucidated.
IJMS, Free Full-Text
Uptake of E1S from the blood by organic anion transporting polypeptides
Hexokinase 1 cellular localization regulates the metabolic fate of glucose - ScienceDirect
Frontiers The role of glutamate receptors in the regulation of the tumor microenvironment
How can I measure brain acetylcholine levels in vivo? Advantages and caveats of commonly used approaches - Mineur - 2023 - Journal of Neurochemistry - Wiley Online Library
Arrestin-Dependent and -Independent Internalization of G Protein–Coupled Receptors: Methods, Mechanisms, and Implications on Cell Signaling
Metabolism and epigenetics at the heart of T cell function: Trends in Immunology
Mechanisms of COVID-19 pathogenesis in diabetes American Journal of Physiology-Heart and Circulatory Physiology
G protein-coupled receptor-G protein interactions: a single-molecule perspective
Recomendado para você
-
Rapid Visco Analyzer (RVA) viscoamylogram of djulis starch by the29 maio 2024
-
Ezequiel 34:8 RVA Mobile Phone Wallpaper - Vivo yo, ha dicho el29 maio 2024
-
Baile Reviver com 'Os Mineirinhos' - Fundação Cultural de Casimiro29 maio 2024
-
Tropicabana RVA, Richmond VA29 maio 2024
-
Mark Whitten will be at Anime Ink this October! Mark is the29 maio 2024
-
9OT Remix: Top 3 Plays of the week for October 2929 maio 2024
-
Lançada mais uma edição do projeto Pinheiro Solidário da RVA29 maio 2024
-
HANUMAN,BHAGWA,HINDU,BHAGWAN,GOD VIVO V23 5G29 maio 2024
-
Imitation of RVA pasting measurement protocol in an oscillatory29 maio 2024
-
The heatmap of RVA or RVC infection compared with control. (A) The29 maio 2024
você pode gostar
-
SCP-2897 - SCP Foundation29 maio 2024
-
Pixilart - Charmander by Bunny-PixelOwO29 maio 2024
-
Frozen 3: Data de lançamento, enredo e tudo que sabemos29 maio 2024
-
Tottenham News, Fixtures, Rumours, Analysis l Last Word On Football29 maio 2024
-
Moon Knight Issue # 29b (Marvel Comics)29 maio 2024
-
Platense aprobó su balance con superavit histórico29 maio 2024
-
Akame ga Kill! Image by Tashiro Tetsuya #1136375 - Zerochan Anime Image Board29 maio 2024
-
Crianças no Banco da Moto apenas com 11 anos? - Autoescola Online - Ronaldo Cardoso29 maio 2024
-
Ari!! (AKA a brat) : r/jaidenanimations29 maio 2024
-
Crazy Frog Wall Decal by Wallmonkeys Peel and Stick Graphic (24 in H x 16 in W) WM8198929 maio 2024