In 2020.0 EUR J MED CHEM published article about HUMAN BRAIN; ARECAIDINE; AGONIST; LOGP; OPPORTUNITIES; GUVACINE; SUBTYPES in [Ozenil, Marius; Pacher, Katharina; Balber, Theresa; Vraka, Chrysoula; Mitterhauser, Markus; Wadsak, Wolfgang; Hacker, Marcus; Pichler, Verena] Med Univ Vienna, Dept Biomed Imaging & Image Guided Therapy, Div Nucl Med, Vienna, Austria; [Balber, Theresa; Mitterhauser, Markus] Ludwig Boltzmann Inst Appl Diagnost, Vienna, Austria; [Roller, Alexander] Univ Vienna, Fac Chem, Xray Struct Anal Ctr, Vienna, Austria; [Holzer, Wolfgang; Spreitzer, Helmut] Univ Vienna, Fac Life Sci, Dept Pharmaceut Chem, Vienna, Austria; [Wadsak, Wolfgang] CBmed GmbH, Ctr Biomarker Res Med, Graz, Austria in 2020.0, Cited 50.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9. COA of Formula: C13H13N
Supported by their involvement in many neurodegenerative disorders, muscarinic acetylcholine receptors ( mAChRs) are an interesting target for PET imaging. Nevertheless, no radiotracer is established in clinical routine. Within this work we aim to develop novel PET tracers based on the structure of arecoline. Fifteen novel arecoline derivatives were synthesized, characterized and tested for their affinity to the mAChRs M1-M5 and the conceivable off-target acetylcholinesterase. Five arecoline derivatives and arecoline were labeled with carbon-11 in good yields. Arecaidine diphenylmethyl ester (3b), arecaidine bis(4-fluorophenyl)methyl ester (3c) and arecaidine (4-bromophenyl)(4-fluorophenyl)methyl ester (3e) showed a tremendous gain in mAChR affinity compared to arecoline and a pronounced subtype selectivity for M1. Metabolic stability and serum protein binding of [C-11] 3b and [C-11] 3c were in line with properties of established brain tracers. Nonspecific binding of [C-11]3c was prevalent in kinetic and endpoint experiment on living cells as well as in autoradiography on native mouse brain sections, which motivates us to decrease the lipophilicity of this substance class prior to in vivo experiments. (C) 2020 The Author(s). Published by Elsevier Masson SAS.
COA of Formula: C13H13N. About Diphenylmethanamine, If you have any questions, you can contact Ozenil, M; Pacher, K; Balber, T; Vraka, C; Roller, A; Holzer, W; Spreitzer, H; Mitterhauser, M; Wadsak, W; Hacker, M; Pichler, V or concate me.
Reference:
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