Results 21 to 30 of about 8,456 (200)

Rationale for Selective Muscarinic Receptor Agonists as Candidates for the Management of Cognitive and Neuropsychiatric Symptoms in Alzheimer's Disease [PDF]

Alzheimers Dement
Abstract Background Cognitive impairment and neuropsychiatric symptoms, including psychosis, are fundamental features of Alzheimer's disease (AD) and related dementias. Currently treatments for these symptoms have efficacy, safety, and tolerability limitations; new treatments with novel mechanisms are needed.
Marcus R, Vuocolo S, Ramsey I, Watson C, Kang M.   +4 more
europepmc   +2 more sources

A growing understanding of the role of muscarinic receptors in the molecular pathology and treatment of schizophrenia

Frontiers in Cellular Neuroscience, 2023
Pre-clinical models, postmortem and neuroimaging studies all support a role for muscarinic receptors in the molecular pathology of schizophrenia. From these data it was proposed that activation of the muscarinic M1 and/or M4 receptor would reduce the ...
Brian Dean, Geor Bakker, Hiroki R. Ueda, Hiroki R. Ueda, Andrew B. Tobin, Alastair Brown, Richard A. A. Kanaan   +6 more
doaj   +1 more source

Additive interaction of intrathecal ginsenosides and neostigmine in the rat formalin test [PDF]

Korean Journal of Anesthesiology, 2013
BackgroundThe authors evaluated the effect of intrathecal mixture of ginsenosides with neostigmine on formalin-induced nociception and made further clear the role of the spinal muscarinic (M) receptors on the activity of ginsenosides.MethodsA catheter ...
Cheon-Hee Park, Park-Ne Kim, Seong-Heon Lee, Myung Ha Yoon   +3 more
doaj   +1 more source

Non‐clinical Efficacy and Safety of SUVN‐L3307032, a Muscarinic M4 Positive Allosteric Modulator (M4 PAM), for the Treatment of Neuropsychiatric Symptoms. [PDF]

Alzheimers Dement
Abstract Background Neuropsychiatric symptoms (NPS) associated with Alzheimer’s disease (AD) are burdensome to the caregiver and patients. The current therapies for the treatment of NPS in AD are associated with limited efficacy and severe side effects. Hence, newer treatment options are required to effectively control these symptoms.
Abraham R, Goura V, Kallepalli R, Medapati R, Varalakshmi O, Bojja K, Shaikh A, Badange R, Manchineella S, Narasimhula T, Das A, Guduru N, Bitra K, Mukkollu K, Nissankarao M, Pandey S, Goyal V, Nirogi R.   +17 more
europepmc   +2 more sources

Muscarinic M1 and M4 receptors: Hypothesis driven drug development for schizophrenia [PDF]

Psychiatry Research, 2020
The finding that the drug KarXT, a formulation of xanomeline and tropsium which targets muscarinic receptors, has given a positive result in reducing the positive and negative symptoms of schizophrenia in a phase II trial suggests targeting muscarinic receptors is a new approach to treating the disorder.
Dean, B, Scarr, E
openaire   +3 more sources

CaMKIIα, a modulator of M4 muscarinic acetylcholine receptors

Communicative & Integrative Biology, 2010
G protein-coupled receptors (GPCRs) are subject to the regulation by protein kinases. By controlling the phosphorylation-dephosphorylation balance, protein kinases actively modify GPCR expression and function. In a recent study, we have identified a novel phosphorylation-dependent regulation of Gαi/o-coupled muscarinic acetylcholine receptors.
Ming-Lei, Guo, Zhenguo, Liu, Xiang-Ping, Chu, Li-Min, Mao, John Q, Wang   +4 more
openaire   +2 more sources

Rat Schwann cells express M1–M4 muscarinic receptor subtypes

Journal of Neuroscience Research, 2006
AbstractThe expression of different muscarinic receptor subtypes was analyzed in immature Schwann cells obtained from sciatic nerve of 2‐day neonatal rats. By using RT‐PCR analysis, we demonstrated the presence of M1, M2, M3, and M4 receptor subtypes in cultured Schwann cells, with M2 displaying the highest expression levels.
LORETI, Simona, VILARO' MT, VISENTIN S, REES H, LEVEY AI, TATA, Ada Maria   +5 more
openaire   +3 more sources

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors [PDF]

Nature, 2016
Muscarinic M1-M5 acetylcholine receptors are G-protein-coupled receptors that regulate many vital functions of the central and peripheral nervous systems. In particular, the M1 and M4 receptor subtypes have emerged as attractive drug targets for treatments of neurological disorders, such as Alzheimer's disease and schizophrenia, but the high ...
David M, Thal, Bingfa, Sun, Dan, Feng, Vindhya, Nawaratne, Katie, Leach, Christian C, Felder, Mark G, Bures, David A, Evans, William I, Weis, Priti, Bachhawat, Tong Sun, Kobilka, Patrick M, Sexton, Brian K, Kobilka, Arthur, Christopoulos   +13 more
openaire   +2 more sources

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of ¹⁸F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]

ChemMedChem
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Herrera-Rueda MA, Boateng MA, Wuest M, West FG, Wuest F.   +4 more
europepmc   +2 more sources

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie, Schaller, David, Stark, Holger, Wolber, Gerhard   +3 more
core   +2 more sources