Synthesis of novel and functionally selective non‐competitive muscarinic antagonists as chemical probes

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F18%3A00489202" target="_blank" >RIV/67985823:_____/18:00489202 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1111/cbdd.13059" target="_blank" >http://dx.doi.org/10.1111/cbdd.13059</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1111/cbdd.13059" target="_blank" >10.1111/cbdd.13059</a>

Result language
angličtina
Original language name
Synthesis of novel and functionally selective non‐competitive muscarinic antagonists as chemical probes
Original language description
Muscarinic receptors are known to play important biological roles and are drug targets for several human diseases. In a pilot study, novel muscarinic antagonists were synthesized and used as chemical probes to obtain additional information of the muscarinic pharmacophore. The design of these ligands made use of current orthosteric and allosteric models of drug-receptor interactions together with chemical motifs known to achieve muscarinic receptor selectivity. This approach has led to the discovery of several non-competitive muscarinic ligands that strongly bind at a secondary receptor site. These compounds were found to be non-competitive antagonists that completely abolished carbachol activation in functional assays. Several of these compounds antagonized functional response to carbachol with great potency at M-1 and M-4 than at the rest of receptor subtypes.
Czech name
—
Czech description
—

Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
30105 - Physiology (including cytology)

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Similar results(10)