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

Synthesis of novel and functionally selective non-competitive muscarinic antagonists as chemical probes Core structure of novel muscarinic antagonists

Ve spolupráci s Barry University byli vyvinuti noví antagonisté muskarinových receptorů.

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 M1 and M4 than at the rest of receptor subtypes.

Lidé

Mgr. Jan Jakubík, PhD
vedoucí oddělení
MUDr. Vladimír Doležal, DrSc.
zástupce vedoucího oddělení
MUDr. et Mgr. Helena Janíčková, PhD
vědecká pracovnice
Mgr. Eva Dolejší, PhD
vědecká asistentka
Mgr. Alena Janoušková (roz. Randáková), PhD
vědecká pracovnice
Alice Abbondanza, MSc
postgraduální studentka

Nikolai Chetverikov, MSc

postgraduální student

Mgr. Dominik Nelic

postgraduální student

Trisha Dhabalia
studentka

Bc. Mutale Jane Mulenga

studentka

Dana Ungerová
technická pracovnice
   
 

 

Biochemie membránových receptorů

Doc. RNDr. Petr Svoboda, DrSc.
vědecký pracovník
RNDr. Lenka Roubalová, PhD.
vědecký pracovník
RNDr. Hana UjčíkováPhD.
vědecká asistentka