Chemistry graduates have much scope to use their knowledge in a range of research sectors, including roles within chemical engineering, chemical and related industries, healthcare and more. In a document, author is Quadri, Marta, introducing its new discovery. Reference of 156028-26-1.
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.
Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.Interested yet? Keep reading other articles of 156028-26-1, you can contact me at any time and look forward to more communication. Reference of 156028-26-1.
Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider