Results 1 to 10 of about 2,769 (106)

Xanomeline and Trospium Chloride: Mechanism of Action, Clinical, and Translational Science. [PDF]

Clin Transl Sci
ABSTRACT Xanomeline‐trospium chloride (Cobenfy, formerly KarXT) is a first‐in‐class, oral central M1/M4 muscarinic receptor agonist approved for the treatment of schizophrenia in adults. Cobenfy represents a paradigm shift by avoiding direct dopamine D2 receptor blockade and thus significantly reduces the burden of metabolic, extrapyramidal, and ...
Avila S, Chen IL.
europepmc   +2 more sources

M5 positive allosteric modulation alleviates parkinsonian motor deficits. [PDF]

PLoS ONE
Parkinson's disease is a neurodegenerative movement disorder which is characterized by cardinal motor symptoms of tremor at rest, rigidity, bradykineasia, and postural instability.
Nicole E Chambers, Dominic Hall, Morgan Kaplan, Sarah Garan, Tyler Eichner, Mark S Moehle   +5 more
doaj   +2 more sources

In Vivo Evaluation of Psoralen in a Copper Sulfate-Induced Chick (Gallus gallus domesticus) Emesis Model and In Silico Analysis of Its Interaction With D₂, 5-HT₃ _A, and Muscarinic Receptors. [PDF]

ChemistryOpen
Psoralen (PSN) demonstrates significant dose‐dependent antiemetic activity in a copper sulfate–induced chick emesis model. Integrated in vivo and in silico analyses reveal reduced retching frequency, prolonged latency, and favorable multi‐receptor interactions with D2, 5‐HT3A, and muscarinic receptors, highlighting PSN as a promising multi‐target ...
Chandra K, Bahar SU, Akter K, Khatun MM, Sadhukhan S, Puja PS, Rohan F, Bhuia MS, Alfaifi M, Altemani FH, Alsenani F, Sheikh S, Islam MT.   +12 more
europepmc   +2 more sources

Advances in Targeting Central Cholinergic Dysfunction for Neurodegenerative Diseases: From Pharmacotherapy to Neuromodulation. [PDF]

CNS Neurosci Ther
This review charts the evolution of cholinergic therapies for neurodegenerative diseases—from classical acetylcholinesterase inhibitors (AChEIs) providing symptomatic relief to precision multi‐target drugs and neuromodulation (VNS, DBS, NIBS) that restore dysfunctional circuits. Emerging gene therapy, cell regeneration, and advanced cholinergic imaging
Lei L, Hu X, Lu R, Yang JJ, Meng Q.
europepmc   +2 more sources

N-Arachidonoyl-phosphatidylethanolamide phospholipase D activation by muscarinic receptors. [PDF]

J Physiol
Abstract figure legend Activating muscarinic M3 receptors activates Gq‐pathway signalling, including the activation of phospholipase C (PLC) and release of calcium from internal stores as shown in the upper panel. It remains unclear whether the calcium acts on N‐arachidonoyl‐phosphatidylethanolamide phospholipase D (NAPE‐PLD) itself or upstream at N ...
Murataeva N, Schmitt C, Hyman E, Wager-Miller J, Matthews I, Cai R, Cai S, Li Y, Mackie K, Straiker A.   +9 more
europepmc   +2 more sources

Synergistic mechanisms of medullary cholinergic-serotonergic pathway interactions in regulating neuronal excitability and locomotor activities [PDF]

Communications Biology
Medullary serotonergic (5-HT) neurons play a pivotal role in locomotor initiation. While these neurons receive cholinergic innervation, the functional consequences and underlying mechanisms remain poorly understood. Using ePet-EYFP transgenic mice (P3–P6)
Yi Cheng, Yue Dai, Renkai Ge, Qiang Zhang   +3 more
doaj   +2 more sources

Dualsteric Agonist for M2 Muscarinic Receptor Causes Oxidative Stress and Mitochondrial Alteration in Human Glioblastoma Cancer Stem Cells. [PDF]

J Neurochem
Dualsteric agonist N8‐iper shows cytotoxic effects on glioblastoma cancer stem cells, but not on human normal astrocytes. Lipid accumulation appears as a consequence of cytotoxic stress; in fact, they are not present in healthy astrocytes. ABSTRACT Glioblastoma (GB) is the most malignant form of human brain tumor, characterized by heterogeneous cell ...
Guerriero C, De Nuccio C, Petrone M, Rinaldi T, Cirigliano A, Visentin S, Bernardo A, Conti L, Matera C, De Amici M, Dallanoce C, Tata AM.   +11 more
europepmc   +2 more sources

The Acetylcholine Esterase Inhibitor Donepezil Increases Dopamine Levels in the Nucleus Accumbens and Blocks the Alcohol Deprivation Effect in Rats. [PDF]

Addict Biol
This study examined the effects of donepezil on mesolimbic dopamine signalling and alcohol‐related behaviours in male rats. Donepezil increases nucleus accumbens dopamine via muscarinic mechanisms and prevented further dopamine elevation after alcohol administration. Although it did not reduce regular alcohol intake, it abolished relapse‐like drinking.
Loftén A, Danielsson K, Adermark L, Söderpalm B, Ericson M.   +4 more
europepmc   +2 more sources

Hypothalamic Control of Liver Health and Disease: From Circuits to Pathophysiology and Therapies. [PDF]

Adv Sci (Weinh)
This review delineates the hypothalamic circuits that control liver homeostasis via autonomic and neuroendocrine pathways. Dysregulation of this hypothalamus–liver axis drives disease progression across a spectrum including steatotic liver disease, liver inflammation and injury, fibrosis, cirrhosis, and hepatocellular carcinoma.
Tang Q, Li J, Song H, Zhang A, Zeng H, Xu Y, Mo L, He J.   +7 more
europepmc   +2 more sources

Towards Mechanism-Informed Treatments for Mental Health. [PDF]

J Neurochem
Neuropsychiatric disorders impose a major global health burden, and current treatments, which historically mostly targeted dopamine and serotonin dysfunctions, often provide only partial, symptomatic relief. This review highlights emerging evidence that additional neuromodulator systems, including acetylcholine, norepinephrine, and endocannabinoids ...
Bengoetxea de Tena I, Sallie FN, Rodriguez Abiero A, Rizzi B, Champarini LG, Corti E, Masella G, Dunn AL, Binder LB, Wenzel TJ, Robles AI, Anversa RG, Tremblay C, Fokoua AR, de Lima RMS, D'Ávila M, Truong TTT, Pierce JC, Rodrigues RS, Dinamarca-Villarroel L, Almeida FB, Piironen AK, Aguiar AFL, Jaramillo AM, Santos L, de Lange A, Nutt DJ, Lawrence AJ.   +27 more
europepmc   +2 more sources