ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
British Journal of Pharmacology, Volume 182, Issue 14, Page 3178-3210, July 2025.G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison +15 more
wiley +1 more source
M2 muscarinic receptor activation regulates schwann cell differentiation and myelin organization [PDF]
, 2014 Glial cells express acetylcholine receptors. In particular, rat Schwann cells express different muscarinic receptor subtypes, the most abundant of which is the M2 subtype. M2 receptor activation causes a reversible arrest of the cell cycle. This negative
Arthur-Farraj +52 more
core +4 more sources
Progress on the development of Class A GPCR‐biased ligands
British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales +20 more
wiley +1 more source
A fast genetically encoded fluorescent sensor for faithful in vivo acetylcholine detection in mice, fish, worms and flies [PDF]
, 2020 Here we design and optimize a genetically encoded fluorescent indicator, iAChSnFR, for the ubiquitous neurotransmitter acetylcholine, based on a bacterial periplasmic binding protein.
Borden, Philip M. +4 more
core
Positive allosteric modulation of the muscarinic M1 receptor improves efficacy of antipsychotics in mouse glutamatergic deficit models of behavior [PDF]
, 2016 Current antipsychotics are effective in treating the positive symptoms associated with schizophrenia, but they remain suboptimal in targeting cognitive dysfunction.
Arthur Christopoulos +14 more
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Chemogenetic Control of Striatal Astrocytes Improves Parkinsonian Motor Deficits in Mice
Glia, Volume 73, Issue 6, Page 1188-1202, June 2025.Main Points Dopamine depletion reduces locomotion‐induced calcium activity in dorsal striatal astrocytes. Chemogenetic activation facilitates astrocyte locomotion responses and improves motor behavior in dopamine lesioned animals. ABSTRACT Parkinson's disease (PD) is characterized by the degeneration of dopaminergic nigrostriatal inputs, which causes ...
Wesley R. Evans +7 more
wiley +1 more source
Frontiers in Molecular NeuroscienceFive muscarinic acetylcholine (mACh) receptor subtypes are divided into two classes: the M1 class (M1, M3, and M5) and the M2 class (M2 and M4). The former is coupled to Gq proteins, while the latter is coupled to Gi/o proteins.
Li-Min Mao +4 more
doaj +1 more source
P2Y₂ Nucleotide Receptors Expressed Heterologously in Sympathetic Neurons Inhibit Both N-Type Ca²⁺ and M-Type K⁺ Currents [PDF]
, 1998 The P2Y₂ receptor is a uridine/adenosine triphosphate (UTP/ATP)-sensitive G-protein-linked nucleotide receptor that previously has been reported to stimulate the phosphoinositide signaling pathway.
Barnard, EA +3 more
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Cholinergic and endocannabinoid neuromodulatory effects overlap on neurons of the pedunculopontine nucleus of mice [PDF]
, 2015 The pedunculopontine nucleus (PPN) is a part of the reticular activating system and one of the main sources of the cholinergic fibers in the midbrain, while it is also subject to cholinergic modulation.
Bordas, Csilla +2 more
core +1 more source
Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype
Journal of Pharmacological Sciences, 2004 Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi +5 more
doaj