Results 11 to 20 of about 3,288 (169)

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‐HT3A, and Muscarinic Receptors

ChemistryOpen
Psoralen (PSN), a naturally occurring furocoumarin, was evaluated for its antiemetic potential using integrated in vivo and in silico approaches, considering the limitations of currently available antiemetic agents.
Kishor Chandra, Sharif Uddin Bahar, Khadija Akter, Mst Muslima Khatun, Samiran Sadhukhan, Progna Saha Puja, Fazley Rohan, Md Shimul Bhuia, Mohammed Alfaifi, Faisal H. Altemani, Faisal Alsenani, Salehin Sheikh, Muhammad Torequl Islam   +12 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

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

Redirecting Alzheimer's disease therapeutics: Multitarget drugs and complementary non-pharmacological strategies. [PDF]

Alzheimers Dement
Abstract Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder driven by intersecting pathological processes. Persistent attrition in AD drug‐development pipelines highlights the limited clinical impact of single‐target therapies and has increased interest in multi‐target approaches acting on shared biological hubs.
Martínez-Orozco H, Andrade-Guerrero J, Pastén-Castrejón NJ, Rodríguez-Tanty C, Diaz-Miranda SY.   +4 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

Muscarinic M5 receptors modulate ethanol seeking in rats [PDF]

Neuropsychopharmacology, 2018
Despite the cost to both individual and society, alcohol use disorders (AUDs) remain a major health risk within society, and both relapse and heavy drinking are still poorly controlled with current medications. Here we demonstrate for the first time that a centrally active and selective negative allosteric modulator for the rat M5 muscarinic ...
Alice E. Berizzi, Christina J. Perry, David M. Shackleford, Craig W. Lindsley, Carrie K. Jones, Nicola A. Chen, Patrick M. Sexton, Arthur Christopoulos, Christopher J. Langmead, Andrew J. Lawrence   +9 more
openaire   +3 more sources

Multitargeting nature of muscarinic orthosteric agonists and antagonists

Frontiers in Physiology, 2022
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
doaj   +1 more source

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

Ultrasonic vocalizations induced by sex and amphetamine in M2, M4, M5 muscarinic and D2 dopamine receptor knockout mice. [PDF]

PLoS ONE, 2008
Adult mice communicate by emitting ultrasonic vocalizations (USVs) during the appetitive phases of sexual behavior. However, little is known about the genes important in controlling call production.
Haoran Wang, Shuyin Liang, Jeffrey Burgdorf, Jurgen Wess, John Yeomans   +4 more
doaj   +1 more source

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Journal of Pharmacological Sciences, 2004
Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi, Nozomi Kawakami, Yousuke Wakayama, Norimasa Izumi, Shuhei Horio, Hiroyuki Fukui   +5 more
doaj   +1 more source