Results 1 to 10 of about 6,339 (219)

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

A New Era of Muscarinic Acetylcholine Receptor Modulators in Neurological Diseases, Cancer and Drug Abuse [PDF]

Pharmaceuticals
The cholinergic pathways in the central nervous system (CNS) play a pivotal role in different cognitive functions of the brain, such as memory and learning.
Helena Tsimpili, Grigoris Zoidis
doaj   +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

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

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

Update on the Development of SUVN‐I6107: A True Positive Allosteric Modulator of the Muscarinic M1 Acetylcholine Receptor for the Treatment of Dementia [PDF]

Alzheimers Dement
Abstract Background SUVN‐I6107 is a novel and selective muscarinic M1 Positive Allosteric Modulator (PAM) being developed for the treatment of dementia due to neurodegenerative disorders. In the current research, the pharmacological properties of SUVN‐I6107 in various animal models of cognitive deficits were investigated.
Benade V, Shinde A, Badange R, Rasheed M, Subramanian R, Petlu S, Abraham R, Goyal V, Palacharla V, Goura V, Pandey S, Medapati R, Kallepalli R, Nirogi R.   +13 more
europepmc   +2 more sources

Cryo-EM reveals an extrahelical allosteric binding site at the M5 mAChR [PDF]

Nature Communications
The M5 muscarinic acetylcholine receptor (M5 mAChR) represents a promising therapeutic target for neurological disorders. However, the high conservation of its orthosteric binding site poses significant challenges for drug development.
Wessel A. C. Burger, Jesse I. Mobbs, Bhavika Rana, Jinan Wang, Keya Joshi, Patrick R. Gentry, Mahmuda Yeasmin, Hariprasad Venugopal, Aaron M. Bender, Craig W. Lindsley, Yinglong Miao, Arthur Christopoulos, Celine Valant, David M. Thal   +13 more
doaj   +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

Exploring the Evolving Role of Scopolamine in Pharmacotherapy: From Cognitive Impairment to Neuroplasticity?―A Narrative Review [PDF]

Molecules
Scopolamine, also known as hyoscine, is a naturally occurring tropane alkaloid derived from plants of the Solanaceae family. Clinically, the compound has long been used for the prevention of motion sickness and postoperative nausea and vomiting, as well ...
Jakub Kukla, Piotr Olejnik, Kaja Kasarełło   +2 more
doaj   +2 more sources

Further Insights Into Anticholinergic Action Informed by Japanese Anticholinergic Risk Scale. [PDF]

Geriatr Gerontol Int
ABSTRACT The increased anticholinergic burden caused by medications in older adults is one of the adverse drug reactions of particular concern, as it can exacerbate the onset of geriatric syndromes or induce cognitive dysfunction, and is also related to the issue of polypharmacy.
Mogi M, Liu S, Suzuki Y, Shibata Y, Yamada S.   +4 more
europepmc   +2 more sources