Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity. [PDF]
Membrane potential controls the response of the M2 muscarinic receptor to its ligands. Membrane hyperpolarization increases response to the full agonist acetylcholine (ACh) while decreasing response to the partial agonist pilocarpine.
Chen, I-Shan+2 more
core +1 more source
Revising Berg-Purcell for finite receptor kinetics [PDF]
From nutrient uptake, to chemoreception, to synaptic transmission, many systems in cell biology depend on molecules diffusing and binding to membrane receptors. Mathematical analysis of such systems often neglects the fact that receptors process molecules at finite kinetic rates.
arxiv +1 more source
Muscarinic Receptor Agonists and Antagonists [PDF]
A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed.
David R. Kelly, Kenneth J. Broadley
openaire +4 more sources
Structure of the M2 muscarinic receptor-β-arrestin complex in a lipid nanodisc
After activation by an agonist, G-protein-coupled receptors (GPCRs) recruit β-arrestin, which desensitizes heterotrimeric G-protein signalling and promotes receptor endocytosis 1 . Additionally, β-arrestin directly regulates many cell signalling pathways
D. Staus+8 more
semanticscholar +1 more source
Presynaptic M1 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in the hippocampus in vitro [PDF]
The effects of the cholinoceptor agonist, carbachol (CCh), were examined in the rat hippocampal slice preparation. Intracellular recordings from CA1 pyramidal neurones revealed that CCh (1–3 μM) inhibited excitatory postsynaptic responses evoked by ...
Sheridan, Robert D., Sutor, Bernd
core +1 more source
Neurotransmitter released from presynaptic terminals activates both ligand-gated ion channels (ionotropic receptors) and a variety of G-protein-coupled receptors (GPCRs). These neurotransmitter receptors are expressed on both presynaptic and postsynaptic
J. Dittman, J. M. Kaplan
semanticscholar +1 more source
A photoisomerizable muscarinic antagonist. Studies of binding and of conductance relaxations in frog heart [PDF]
These experiments employ the photoisomerizable compound, 3,3'-bis- [alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), to study the response to muscarinic agents in frog myocardium. In homogenates from the heart, trans-Bis-Q blocks the binding of [3H]-N-
Birdsall, Nigel J. M.+5 more
core +1 more source
Memetic Algorithms for Ligand Expulsion from Protein Cavities [PDF]
Ligand diffusion through proteins is a fundamental process governing biological signaling and enzymatic catalysis. The complex topology of protein tunnels results in difficulties with computing ligand escape pathways by standard molecular dynamics (MD) simulations. Here, two novel methods for searching of ligand exit pathways and cavity exploration are
arxiv +1 more source
Modulation of Hippocampal Circuits by Muscarinic and Nicotinic Receptors
This article provides a review of the effects of activation of muscarinic and nicotinic receptors on the physiological properties of circuits in the hippocampal formation.
Holger Dannenberg+2 more
semanticscholar +1 more source
Muscarinic modulation of M and h currents in gerbil spherical bushy cells.
Descending cholinergic fibers innervate the cochlear nucleus. Spherical bushy cells, principal neurons of the anterior part of the ventral cochlear nucleus, are depolarized by cholinergic agonists on two different time scales.
Charlène Gillet+2 more
doaj +1 more source