Human M1 muscarinic receptor chimeras were designed (i) to allow detection of their
interaction with the fluorescent antagonist pirenzepine labelled with Bodipy [558/568] …

Following a recent description of fluorescence resonance energy transfer between
enhanced green fluorescent protein (EGFP)-fused human muscarinic M1 receptors and …

Ligand binding to G protein-coupled receptors is a complex process that involves sequential
receptor conformational changes, ligand translocation, and possibly ligand-induced receptor …

The muscarinic agonist oxotremorine and the tricyclic muscarinic antagonists pirenzepine
and telenzepine have been derivatized using a functionalized congener approach for the …

Fluorescence resonance energy transfer (FRET), measured by fluorescence intensity-based
microscopy and fluorescence lifetime imaging, has been used to estimate the size of …

In the search for new chemical entities that interact with G-protein-coupled receptors
(GPCRs), assays that quantify efficacy and affinity are employed. Traditional methods for …

Allosteric modulators have been identified for several G protein-coupled receptors, most
notably muscarinic receptors. To study their mechanism of action, we made use of a recently …

Chimeric M1/M2 receptors were expressed in murine fibroblasts (B82) transfected with
recombinant m1/m2 receptor genes. The binding affinities of a number of muscarinic …

Equilibrium binding assays support four (M1–M4) and molecular cloning studies have
identified five (m1–m5) muscarinic receptor subtypes in the brain and peripheral tissues …

Bitopic binding properties apply to a variety of muscarinic compounds that span and
simultaneously bind to both the orthosteric and allosteric receptor sites. We provide …