Evaluation of antipsychotic properties of M4 muscarinic acetylcholine receptor agonists in mice
M 1 and/or M 4 muscarinic acetylcholine receptors are suggested to be involved in the pathogenesis and treatment of schizophrenia. To validate the antipsychotic potential of M 4 receptor activation, we evaluated the antipsychotic properties of the ...
Yumika Toyoshima+10 more
semanticscholar +1 more source
Dopamine D_2-receptor activation elicits akinesia, rigidity, catalepsy, and tremor in mice expressing hypersensitive 4 nicotinic receptors via a cholinergic-dependent mechanism [PDF]
Recent studies suggest that high-affinity neuronal nicotinic acetylcholine receptors (nAChRs) containing α4 and β2 subunits (α4β2*) functionally interact with G-protein-coupled dopamine (DA) D_2 receptors in basal ganglia.
Andrew R. Tapper+18 more
core +3 more sources
Cholinergic signaling plays a crucial role in the regulation of adult hippocampal neurogenesis; however, the mechanisms by which acetylcholine mediates neurogenic effects are not completely understood.
Lidia I. Madrid+9 more
semanticscholar +1 more source
Background The etiology of postural orthostatic tachycardia syndrome (POTS) is yet to be established. The disorder is often misdiagnosed as chronic anxiety or a panic disorder because the autonomic failure in these patients is not severe.
William T. Gunning+4 more
doaj +1 more source
Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen+7 more
doaj +1 more source
Expression of m1-m4 muscarinic acetylcholine receptor proteins in rat hippocampus and regulation by cholinergic innervation [PDF]
A family of muscarinic ACh receptor genes are expressed in hippocampus, but little is known about the localization of the encoded proteins and their regulation by cholinergic innervation. Subtype-specific antibodies were used to localize m1-m4 proteins in the hippocampal formation by immunocytochemistry and to determine the alterations in the subtypes ...
Allan I. Levey+4 more
openalex +5 more sources
Characterization of a Novel M4 PAM PET Radioligand [11C]PF06885190 in Nonhuman Primates (NHP)
Muscarinic acetylcholine receptors (mAChR), including M4, draw attention as therapeutic targets for several neurodegenerative diseases including Alzheimer’s disease (AD).
Sangram Nag+9 more
doaj +1 more source
Synergistic Antiemetic Effects of Nerolidol on Domperidone, Hyoscine, and Ondansetron: In Vivo and in Silico Investigations on Receptor Binding Affinity. [PDF]
Nerolidol shows prominent antiemetic activity and mitigates CuSO4.H2O‐mediated retching in chicks efficiently through its peripheral action. Additionally, the in silico studies have also shown possible antiemetic effects with greater binding affinity against muscarinic (specially, M2 and M3) and dopaminergic receptors.
Ghosh Situ S+7 more
europepmc +2 more sources
Virtual Affinity Fingerprints for Target Fishing: A New Application of Drug Profile Matching [PDF]
We recently introduced Drug Profile Matching (DPM), a novel virtual affinity fingerprinting bioactivity prediction method. DPM is based on the docking profiles of ca.
Czobor, P.+6 more
core +1 more source
The neuromodulator acetylcholine (ACh) plays an important role in arousal, attention, vigilance, learning and memory. ACh is released during different behavioural states and affects the brain microcircuit by regulating neuronal and synaptic properties ...
Guanxiao Qi+3 more
doaj +1 more source