M5 positive allosteric modulation alleviates parkinsonian motor deficits. [PDF]
PLoS ONEParkinson'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 +5 more
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A New Era of Muscarinic Acetylcholine Receptor Modulators in Neurological Diseases, Cancer and Drug Abuse [PDF]
PharmaceuticalsThe 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
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Synergistic mechanisms of medullary cholinergic-serotonergic pathway interactions in regulating neuronal excitability and locomotor activities [PDF]
Communications BiologyMedullary 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 +3 more
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Muscarinic cannabinoid suppression of excitation, a novel form of coincidence detection [PDF]
Pharmacological ResearchΔ9-tetrahydrocannabinol (THC), the chief psychoactive ingredient of cannabis, acts in the brain primarily via cannabinoid CB1 receptors. These receptors are implicated in several forms of synaptic plasticity – depolarization-induced suppression of ...
Michaela Dvorakova +2 more
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Cryo-EM reveals an extrahelical allosteric binding site at the M5 mAChR [PDF]
Nature CommunicationsThe 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 +13 more
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Exploring the Evolving Role of Scopolamine in Pharmacotherapy: From Cognitive Impairment to Neuroplasticity?―A Narrative Review [PDF]
MoleculesScopolamine, 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 +2 more
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Frontiers in Cellular Neuroscience, 2021 The dopamine transporter (DAT) clears neurotransmitters from the extracellular space and serves as an important regulator of signal amplitude and duration at sites of dopamine release. Several different intracellular signaling pathways have been observed
Suzanne M. Underhill, Susan G. Amara
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Expression of muscarinic acetylcholine receptors M3 and M5 in osteoporosis [PDF]
Medical Science Monitor, 2014 Cholinergic signaling via muscarinic acetylcholine receptors (mAChR) is known to influence various physiological functions. In bone, M3 mAChR and M5 mAChR were identified on the membrane of osteoblast-like cells. M3 mAChR seems to be particularly relevant for bone physiology, as signaling via this receptor was reported to increase bone formation and ...
Kauschke, Vivien +3 more
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Novel Allosteric Effects of Amiodarone at the Muscarinic M5 Receptor [PDF]
The Journal of Pharmacology and Experimental Therapeutics, 2010 Allosteric sites on muscarinic receptors may present superior therapeutic targets for several central nervous system disorders, due to the potential of allosteric ligands to provide more selective modulation and to preserve the spatiotemporal patterning that is characteristic of synaptic transmission.
Edward, Stahl, John, Ellis
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A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity
Pharmaceutics, 2023 Anticholinergic burden tools have relevant pharmacological gaps that may explain their limited predictive ability for clinical outcomes. The aim of this study was to provide a universal pharmacological-based list of drugs with their documented affinity ...
Marta Lavrador +5 more
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