Chemical Research in 91-00-9

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I found the field of Pharmacology & Pharmacy very interesting. Saw the article Enhanced arecoline derivatives as muscarinic acetylcholine receptor M1 ligands for potential application as PET radiotracers published in 2020.0. Safety of Diphenylmethanamine, Reprint Addresses Pichler, V (corresponding author), Med Univ Vienna, Dept Biomed Imaging & Image Guided Therapy, Div Nucl Med, Vienna, Austria.. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine

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.

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Reference:
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