Results 21 to 30 of about 20,015 (223)

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. [PDF]

Journal of Medicinal Chemistry, 2009
This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays ...
T. Bridges, Joy Marlo, C. Niswender, Carrie K Jones, S. Jadhav, P. Gentry, Hyekyung Plumley, C. Weaver, P. J. Conn, C. Lindsley   +9 more
semanticscholar   +3 more sources

Multiple Muscarinic Acetylcholine Receptor Subtypes Modulate Striatal Dopamine Release, as Studied with M1–M5 Muscarinic Receptor Knock-Out Mice [PDF]

The Journal of Neuroscience, 2002
A proper balance between striatal muscarinic cholinergic and dopaminergic neurotransmission is required for coordinated locomotor control. Activation of striatal muscarinic acetylcholine receptors (mAChRs) is known to modulate striatal dopamine release.
Weilie Zhang, M. Yamada, J. Gomeza, A. Basile, J. Wess   +4 more
semanticscholar   +3 more sources

Cellular responses to stimulation of the M5 muscarinic acetylcholine receptor as seen in murine L cells.

Journal of Biological Chemistry, 1990
The membrane signaling properties of the neuronal type-5 muscarinic acetylcholine receptor (M5 AChR) as expressed in murine L cells were studied. Recipient Ltk- cells responded to ATP acting through a P2-purinergic receptor by increasing phosphoinositide
Ching Fong Liao, William P. Schilling, Mariel Birnbaumer, L. Birnbaumer   +3 more
semanticscholar   +3 more sources

Computational Evaluation of Substituted 2-Aminopyrimidine Schiff Bases as Potential Antidepressant Targeting the Muscarinic Acetylcholine M5 Receptor

Journal of Neonatal Surgery
The effectiveness of existing treatments for depression, a complicated mental health condition that affects people all over the world, is limited. The ability of the muscarinic acetylcholine receptor subtype M5 (M5 mAChR) to modulate dopaminergic and ...
Smita Sunil Sawalwade, Bhavna Utkarsh Jain, Sonali Sanjay Nikam, Snehal Prakash Patil   +3 more
semanticscholar   +2 more sources

Discovery of M5 Muscarinic Acetylcholine Receptor Antagonists: 1‐Methyl‐4‐Phenylpiperidine Analogs

The FASEB Journal, 2015
Na-Ra Lee, Xuan Zhang, M. Darna, Guangrong Zheng, L. Dwoskin   +4 more
semanticscholar   +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 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, Lips, Katrin Susanne, Heiss, Christian, Schnettler, Reinhard   +3 more
openaire   +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

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

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