Cholinergic nerve–mediated excitatory junction potentials (EJPs) in the longitudinal muscle of mouse ileum were characterized by using M2 or M3 muscarinic receptor–knockout (KO) mice and 1-[β-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole ...
Hayato Matsuyama +5 more
doaj +1 more source
Muscarinic receptor regulation of chronic pain-induced atrial fibrillation
Atrial fibrillation (AF), one of the most common arrhythmias, is associated with chronic emotional disorder. Chronic pain represents a psychological instability condition related to cardiovascular diseases, but the mechanistic linkage connecting chronic ...
Chao Gong +10 more
doaj +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
Regulation of signal transduction at M2 muscarinic receptor
Muscarinic acetylcholine receptors mediate transmission of an extracellular signal represented by released acetylcholine to neuronal or effector cells. There are five subtypes of closely homologous muscarinic receptors which are coupled by means of heterotrimeric G-proteins to a variety of signaling pathways resulting in a multitude of target cell ...
A, Krejcí +4 more
openaire +2 more sources
Trafficking of M2 Muscarinic Acetylcholine Receptors [PDF]
Internalization is an important mechanism regulating the agonist-dependent responses of G-protein-coupled receptors. The internalization of the M(2) muscarinic cholinergic receptors (mAChR) in HEK293 cells has been demonstrated to occur by an unknown mechanism that is independent of arrestins and dynamin.
A G, Roseberry, M M, Hosey
openaire +2 more sources
Muscarinic receptor oligomerization [PDF]
G protein-coupled receptors (GPCRs) have been classically described as monomeric entities that function by binding in a 1:1 stoichiometric ratio to both ligand and downstream signalling proteins.
Alvarez-Curto, Elisa +3 more
core +1 more source
Synthesis of New Cardioselective M2 Muscarinic Receptor Antagonists.
A series of 5H-dibenz[b,f]azepine derivatives was prepared and evaluated for binding affinities to muscarinic receptors in vitro. Among them, compound 8 showed a high affinity for human recombinant M2 receptors (Ki=2.6 nm), a low affinity for M4 receptors (39-fold less than for M2 receptors) and a very low affinity for M1 and M3 receptors (119- and 112-
G R, Mandelli +5 more
openaire +3 more sources
Dysfunctional Presynaptic M2 Receptors in the Presence of Chronically High Acetylcholine Levels: Data from the PRiMA Knockout Mouse. [PDF]
The muscarinic M2 receptor (M2R) acts as a negative feedback regulator in central cholinergic systems. Activation of the M2 receptor limits acetylcholine (ACh) release, especially when ACh levels are increased because acetylcholinesterase (AChE) activity
Franziska Mohr +3 more
doaj +1 more source
Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements [PDF]
Label-free biosensor technology based on dynamic mass redistribution (DMR) of cellular constituents promises to translate GPCR signaling into complex optical 'fingerprints' in real time in living cells.
Blattermann, S +16 more
core +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

