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 +4 more sources
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.
I-Shan Chen +2 more
doaj +2 more sources
Is muscarinic receptor agonist effective and tolerant for schizophrenia? [PDF]
Background Several randomized clinical trials (RCTs) have recently examined the efficacy and tolerability of muscarinic receptor agonists in schizophrenia. However, whether therapeutics targeting muscarinic receptors improve symptom management and reduce
Xiaonan Guo +3 more
doaj +2 more sources
Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]
Each subtype of the muscarinic receptor family of G protein-coupled receptors is activated by similar concentrations of the neurotransmitter acetylcholine or closely related synthetic analogs such as carbachol. However, pharmacological selectivity can be
Alvarez-Curto, Elisa +3 more
core +1 more source
Carbachol increases intracellular free calcium concentrations in human granulosa-lutein cells [PDF]
We investigated whether the stimulation of human granulosa-lutein cells with muscarinic and nicotinic receptor agonists can cause increases in intracellular free calcium (Ca2+), using Fura-2 microfluorimetry.
Föhr, K. J. +3 more
core +1 more source
Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]
Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G. +4 more
core +1 more source
Brain muscarinic cholinergic receptors in Huntington's disease [PDF]
Muscarinic cholinergic receptors and choline acetyltransferase (ChAT) activity were studied in postmortem brain tissue from patients with Huntington's disease and matched control subjects.
Agid, Y. +4 more
core +1 more source
A G protein-gated K channel is activated via beta 2-adrenergic receptors and G beta gamma subunits in Xenopus oocytes [PDF]
In many tissues, inwardly rectifying K channels are coupled to seven- helix receptors via the Gi/Go family of heterotrimeric G proteins. This activation proceeds at least partially via G beta gamma subunits.
Dascal, Nathan +4 more
core +2 more sources
An in vivo biosensor for neurotransmitter release and in situ receptor activity. [PDF]
Tools from molecular biology, combined with in vivo optical imaging techniques, provide new mechanisms for noninvasively observing brain processes. Current approaches primarily probe cell-based variables, such as cytosolic calcium or membrane potential ...
Griesbeck, Oliver +6 more
core +2 more sources
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

