Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]
, 2007 Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung +3 more
core +1 more source
Allergy, EarlyView.This study identifies that Ach levels are elevated in eCRSwNP and primarily released from SCCs rather than neurons. Ach induces epithelial remodeling in eCRSwNP by binding to M1R/M3R and activating YAP signaling in basal cells, driving basal cell hyperplasia and abnormal differentiation. Blocking M1R/M3R with TB inhibits eCRSwNP progression.
Bowen Zheng +20 more
wiley +1 more source
Inhibition of Connexin43 hemichannels impairs spatial short-term memory without affecting spatial working memory [PDF]
, 2016 Astrocytes are active players in higher brain function as they can release gliotransmitters, which are essential for synaptic plasticity. Various mechanisms have been proposed for gliotransmission, including vesicular mechanisms as well as non-vesicular ...
Albertini, Giulia +5 more
core +2 more sources
Effects of tetrahydroaminoacridine on M1 and M2 muscarine receptors
Neuroscience Letters, 1988 Tetrahydroaminoacridine (THA) has been reported to improve the memory of persons with Alzheimer's disease, but its mechanism of action is uncertain. We found that clinically effective concentrations, 0.03-0.3 microM, readily inhibit acetylcholinesterase and butyrylcholinesterase from rabbit hippocampal tissue in artificial cerebrospinal fluid (CSF) at ...
B D, Pearce, L T, Potter
openaire +2 more sources
Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials
British Journal of Pharmacology, EarlyView.Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen +2 more
wiley +1 more source
Engineering of three-finger fold toxins creates ligands with original pharmacological profiles for muscarinic and adrenergic receptors. [PDF]
PLoS ONE, 2012 Protein engineering approaches are often a combination of rational design and directed evolution using display technologies. Here, we test "loop grafting," a rational design method, on three-finger fold proteins.
Carole Fruchart-Gaillard +8 more
doaj +1 more source
Cholinergic regulation of mood: from basic and clinical studies to emerging therapeutics. [PDF]
, 2019 Mood disorders are highly prevalent and are the leading cause of disability worldwide. The neurobiological mechanisms underlying depression remain poorly understood, although theories regarding dysfunction within various neurotransmitter systems have ...
Dulawa, Stephanie C, Janowsky, David S
core
Recovery of hippocampal functions and modulation of muscarinic response by electroacupuncture in young diabetic rats [PDF]
, 2017 The muscarinic receptor response to acetylcholine regulates the hippocampal-related learning, memory, neural plasticity and the production and processing of the pro-nerve growth factor (proNGF) by hippocampal cells.
Berretta, Erica +9 more
core +2 more sources
Lower density of calretinin‐immunopositive neurons in the putamen of subjects with schizophrenia
Journal of Anatomy, Volume 246, Issue 4, Page 505-516, April 2025.Recent neuroimaging and histological studies highlight the striatum as a key area involved in SCH, but the specific impairment of neuronal subtypes in subcortical structures is not fully understood. This study is the first detailed investigation of neuroanatomical changes in the putamen in SCH, specifically examining the density of calretinin ...
Paz Kelmer +4 more
wiley +1 more source
Two Types of K⁺ Channel Subunit, Erg1 and KCNQ2/3, Contribute to the M-Like Current in a Mammalian Neuronal Cell [PDF]
, 1999 The potassium M current was originally identified in sympathetic ganglion cells, and analogous currents have been reported in some central neurons and also in some neural cell lines.
Abogadie, FC +7 more
core +1 more source