Novel long-acting antagonists of muscarinic ACh receptors.

ABSTRACT:

Background and purpose

The aim of this study was to develop potent and long-acting antagonists of muscarinic ACh receptors. The 4-hexyloxy and 4-butyloxy derivatives of 1-[2-(4-oxidobenzoyloxy)ethyl]-1,2,3,6-tetrahydropyridin-1-ium were synthesized and tested for biological activity. Antagonists with long-residence time at receptors are therapeutic targets for the treatment of several neurological and psychiatric human diseases. Their long-acting effects allow for reduced daily doses and adverse effects.

Experimental approach

The binding and antagonism of functional responses to the agonist carbachol mediated by 4-hexyloxy compounds were investigated in CHO cells expressing individual subtypes of muscarinic receptors and compared with 4-butyloxy analogues.

Key results

SUBMITTER: Randakova A 

PROVIDER: S-EPMC5913398 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature