Allosteric modulators are ligands that bind to a site on the receptor that is spatially separated
from the orthosteric binding site for the endogenous neurotransmitter. Allosteric modulators …

Muscarinic acetylcholine receptors are G protein-coupled receptors (GPCRs) which are
broadly expressed in the central nervous system (CNS) and other tissues in the periphery …

Disruption of cholinergic signalling via muscarinic receptors is associated with various
pathologies, like Alzheimer's disease or schizophrenia. Selective muscarinic agonists …

Allosteric modulators of muscarinic receptors act at a site apart from the common ligand
binding site of the receptor protein. These compounds affect both of the molecular events …

An allosteric modulator is a ligand that binds to an allosteric site on the receptor and
changes receptor conformation to produce increase (positive cooperativity) or decrease …

Allosteric modulation of G protein-coupled receptors has been intensively studied at
muscarinic acetylcholine receptors. Findings made with archetypal allosteric agents such as …

Bivalent ligands of G protein-coupled receptors have been shown to simultaneously either
bind to two adjacent receptors or to bridge different parts of one receptor protein. Recently …

Allosteric modulators of ligand-receptor interactions are found for a variety of receptors
(Christopoulos, 2002). Allosteric agents attach to a binding site being topographically …

The muscarinic M1 acetylcholine receptor is an important drug target for the treatment of
various neurological disorders. Designing M1 receptor-selective drugs has proven …

The five subtypes of the muscarinic acetylcholine receptor (mAChR1—5 or M1—5) are
differentially expressed G protein-coupled receptors (GPCRs) important to a variety of …