Novel M₂ -selective, G_i -biased agonists of muscarinic acetylcholine receptors.

ABSTRACT:

Background and purpose

More than 30% of currently marketed medications act via GPCRs. Thus, GPCRs represent one of the most important pharmacotherapeutic targets. In contrast to traditional agonists activating multiple signalling pathways, agonists activating a single signalling pathway represent a new generation of drugs with increased specificity and fewer adverse effects.

Experimental approach

We have synthesized novel agonists of muscarinic ACh receptors and tested their binding and function (on levels of cAMP and inositol phosphates) in CHO cells expressing individual subtypes of muscarinic receptors, primary cultures of rat aortic smooth muscle cells and suspensions of digested native tissues from rats. Binding of the novel compounds to M₂ receptors was mode

SUBMITTER: Randakova A 

PROVIDER: S-EPMC7161557 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature