Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 253168-94-4, Name is 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine, molecular formula is C12H19NO4S, belongs to quinuclidines compound. In a document, author is Quadri, Marta, introduce the new discover, Safety of 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine.
Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the alpha 7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation
alpha 7 nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for a variety of disorders alpha including neurodegeneration, cognitive impairment, and inflammation. Although traditionally identified as an ionotropic receptor, the alpha 7 subtype showed metabotropic-like functions, mainly linked to the modulation of immune responses. In the present work, we investigated the structure-activity relationships in a set of novel alpha 7 ligands incorporating the 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazole scaffold, i.e. derivatives 21a-34a and 21b-34b, aiming to identify the structural requirements able to preferentially trigger one of the two activation modes of this receptor subtype. The new compounds were characterized as partial and silent alpha 7 nAChR agonists in electrophysiological assays, which allowed to assess the contribution of the different groups towards the final pharmacological profile. Overall, modifications of the selected structural backbone mainly afforded partial agonists, among them tertiary bases 27a-33a, whereas additional hydrogen -bond acceptor groups in permanently charged ligands, such as 29b and 31b, favored a silent desensitizing profile at the alpha 7 nAChR. (C) 2018 Elsevier Masson SAS. All rights reserved.
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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider