Results 21 to 30 of about 15,706 (256)

M1 muscarinic acetylcholine receptor in Alzheimer’s disease [PDF]

Neuroscience Bulletin, 2014
The degeneration of cholinergic neurons and cholinergic hypofunction are pathologies associated with Alzheimer's disease (AD). Muscarinic acetylcholine receptors (mAChRs) mediate acetylcholine-induced neurotransmission and five mAChR subtypes (M1-M5) have been identified.
Jiang, Shangtong, Li, Yanfang, Zhang, Cuilin, Zhao, Yingjun, Bu, Guojun, Xu, Huaxi, Zhang, Yun-Wu   +6 more
openaire   +3 more sources

Neuromodulation of Persistent Activity and Working Memory Circuitry in Primate Prefrontal Cortex by Muscarinic Receptors

Frontiers in Neural Circuits, 2021
Neuromodulation by acetylcholine plays a vital role in shaping the physiology and functions of cerebral cortex. Cholinergic neuromodulation influences brain-state transitions, controls the gating of cortical sensory stimulus responses, and has been shown
Susheel Vijayraghavan, Stefan Everling, Stefan Everling   +2 more
doaj   +1 more source

Characterization of the positive and negative inotropic effects of acetylcholine in the human myocardium [PDF]

, 1995
In the human isolated myocardium, acetylcholine (10−9 to 10−3 M) elicited a biphasic inotropic effect (a decrease in the lower and an increase in the higher concentration range) in atrial and a positive inotropic effect in ventricular trabeculae. However,
Bos, E. (Egbert), Du, X.Y. (Xiaoyi), Saxena, P.R. (Pramod Ranjan), Schoemaker, R.G. (Regien)   +3 more
core   +7 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

Understanding the role of the M1 muscarinic receptor in the propagation of tau as a pathology of Alzheimer's disease [PDF]

Alzheimers Dement
Abstract Background Neurofibrillary tangles (NFTs) composed of hyperphosphorylated tau are a hallmark of Alzheimer's disease (AD). While NFT propagation correlates with disease progression, the underlying molecular mechanisms are not well understood. Loss of cholinergic neurons and disrupted cholinergic signalling also occurs throughout AD.
Gibson K, Tobin A.
europepmc   +2 more sources

Rationale for Selective Muscarinic Receptor Agonists as Candidates for the Management of Cognitive and Neuropsychiatric Symptoms in Alzheimer's Disease [PDF]

Alzheimers Dement
Abstract Background Cognitive impairment and neuropsychiatric symptoms, including psychosis, are fundamental features of Alzheimer's disease (AD) and related dementias. Currently treatments for these symptoms have efficacy, safety, and tolerability limitations; new treatments with novel mechanisms are needed.
Marcus R, Vuocolo S, Ramsey I, Watson C, Kang M.   +4 more
europepmc   +2 more sources

Molecular Determinants of Allosteric Modulation at the M1 Muscarinic Acetylcholine Receptor [PDF]

Journal of Biological Chemistry, 2014
Benzylquinolone carboxylic acid (BQCA) is an unprecedented example of a selective positive allosteric modulator of acetylcholine at the M1 muscarinic acetylcholine receptor (mAChR). To probe the structural basis underlying its selectivity, we utilized site-directed mutagenesis, analytical modeling, and molecular dynamics to delineate regions of the M1 ...
Abdul-Ridha, Alaa, López, Laura, Keov, Peter, Thal, David M., Mistry, Shailesh N., Sexton, Patrick M., Lane, J. Robert, Canals, Meritxell, Christopoulos, Arthur   +8 more
openaire   +5 more sources

Sequence of the gene encoding the human M1 muscarinic acetylcholine receptor

Nucleic Acids Research, 1987
W. Jeffrey Allard, Irving S. Sigal, Richard A. F. Dixon   +2 more
openalex   +5 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

Changes in adrenergic and cholinergic receptors on human cerebral vessels. Implications for new therapeutic strategies in Alzheimer's Disease [PDF]

Alzheimers Dement
Abstract Background Sporadic cerebral amyloid angiopathy (CAA) occurs as a result of a failure of Intramural Periarterial Drainage (IPAD) of amyloid‐beta (Aβ) along the walls of capillaries and arteries. The motive force for IPAD is provided by the spontaneous contractions of cerebrovascular smooth muscle cells (CVSMC that receive adrenergic and ...
Carare R.
europepmc   +2 more sources