Results 1 to 10 of about 2,598 (108)

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

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

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

Nicotinic Acetylcholine Receptor Pathways in Cancer: From Psychiatric Clues to Therapeutic Opportunities. [PDF]

Cancer Rep (Hoboken)
ABSTRACT Background The prevalence of cancer poses significant challenges to treatment, largely because of drug resistance along with other side effects. Current studies have been investigating the growth factors more than other biologic tumor features, such as neurobiologic features.
Azadi MH, Pazooki P, Ajdary S, Shafaroodi H.   +3 more
europepmc   +2 more sources

Downstream Signaling of Muscarinic M₄ Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

Pharmacol Res Perspect
ABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M, Playle C, Palchaudhuri M, Hucke O, Gross U, Ursu D.   +5 more
europepmc   +2 more sources

Acetylcholine Receptor Stimulation Activates Protein Kinase C Mediated Internalization of the Dopamine Transporter

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
doaj   +1 more source

Expression Profiles of Neuropeptides, Neurotransmitters, and Their Receptors in Human Keratocytes In Vitro and In Situ. [PDF]

PLoS ONE, 2015
Keratocytes, the quiescent cells of the corneal stroma, play a crucial role in corneal wound healing. Neuropeptides and neurotransmitters are usually associated with neuronal signaling, but have recently been shown to be produced also by non-neuronal ...
Marta Słoniecka, Sandrine Le Roux, Peter Boman, Berit Byström, Qingjun Zhou, Patrik Danielson   +5 more
doaj   +1 more source

Long-Term—But Not Short-Term—Plasticity at the Mossy Fiber–CA3 Pyramidal Cell Synapse in Hippocampus Is Altered in M1/M3 Muscarinic Acetylcholine Receptor Double Knockout Mice

Cells, 2023
Muscarinic acetylcholine receptors are well-known for their crucial involvement in hippocampus-dependent learning and memory, but the exact roles of the various receptor subtypes (M1–M5) are still not fully understood.
Fang Zheng, Jürgen Wess, Christian Alzheimer   +2 more
doaj   +1 more source