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

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

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 …

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

We previously demonstrated that brucine and some analogues allosterically enhance the
affinity of ACh at muscarinic receptor subtypes m1, M3 or M4. Here we describe allosteric …

Two fluorescent derivatives of the M1 muscarinic selective agonist AC-42 were synthesized
by coupling the lissamine rhodamine B fluorophore (in ortho and para positions) to AC42 …

Tagged biologically active molecules represent powerful pharmacological tools to study and
characterize ligand− receptor interactions. However, the labeling of such molecules is not …

Aiming to design partial agonists as well as allosteric modulators for the M1 muscarinic
acetylcholine (M1AChR) receptor, two different series of bipharmacophoric ligands and their …

We studied the interactions of strychnine, brucine, and three of the N-substituted analogues
of brucine with [3H] N-methylscopolamine (NMS) and unlabeled acetylcholine at m1–m5 …

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 …