Results 41 to 50 of about 29,353 (245)

First-in-Human Assessment of 11C-LSN3172176, an M1 Muscarinic Acetylcholine Receptor PET Radiotracer

Journal of Nuclear Medicine, 2020
Visual Abstract This was a first-in-human study of the PET radiotracer 11C-LSN3172176 for the muscarinic acetylcholine receptor subtype M1. The objectives of the study were to determine the appropriate kinetic model to quantify binding of the tracer to ...
M. Naganawa, N. Nabulsi, S. Henry, D. Matuskey, Shu-Fei Lin, L. Slieker, A. Schwarz, Nancy Kant, C. Jesudason, K. Ruley, Antonio Navarro, Hong Gao, J. Ropchan, D. Labaree, R. Carson, Yiyun Huang   +15 more
semanticscholar   +1 more source

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

Carbachol Induces Ca2+-Dependent Contraction via Muscarinic M2 and M3 Receptors in Rat Intestinal Subepithelial Myofibroblasts

Journal of Pharmacological Sciences, 2009
.: Intestinal myofibroblasts (IMFs) that exist adjacent to the basement membrane of intestines have contractility and contribute to physical barriers of the intestine.
Koichi Iwanaga, Takahisa Murata, Muneyoshi Okada, Masatoshi Hori, Hiroshi Ozaki   +4 more
doaj   +1 more source

Pharmaceutical Assessment Suggests Locomotion Hyperactivity in Zebrafish Triggered by Arecoline Might Be Associated with Multiple Muscarinic Acetylcholine Receptors Activation

Toxins, 2021
Arecoline is one of the nicotinic acid-based alkaloids, which is found in the betel nut. In addition to its function as a muscarinic agonist, arecoline exhibits several adverse effects, such as inducing growth retardation and causing developmental ...
Petrus Siregar, Gilbert Audira, Ling-Yi Feng, Jia-Hau Lee, Fiorency Santoso, Wen-Hao Yu, Yu-Heng Lai, Jih-Heng Li, Ying-Ting Lin, Jung-Ren Chen, Chung-Der Hsiao   +10 more
doaj   +1 more source

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

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

Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]

, 2015
Each subtype of the muscarinic receptor family of G protein-coupled receptors is activated by similar concentrations of the neurotransmitter acetylcholine or closely related synthetic analogs such as carbachol. However, pharmacological selectivity can be
Alvarez-Curto, Elisa, Aslanoglou, Despoina, Marsango, Sara, Milligan, Graeme   +3 more
core   +1 more source

Single nucleotide polymorphisms of the human M1 muscarinic acetylcholine receptor gene [PDF]

AAPS PharmSci, 2001
The gene encoding the human muscarinic receptor, type 1 (CHRM1), was genotyped from 245 samples of the Coriell Collection (Coriell Institute for Medical Research, Camden, NJ). Fifteen single nucleotide polymorphisms (SNPs) were discovered, 9 of which are located in the coding region of the receptor.
J L, Lucas, J A, DeYoung, W, Sadee
openaire   +2 more sources

Muscarinic acetylcholine receptor-dependent and NMDA receptor-dependent LTP and LTD share the common AMPAR trafficking pathway

iScience, 2023
Summary: The forebrain cholinergic system promotes higher brain function in part by signaling through the M1 muscarinic acetylcholine receptor (mAChR). Long-term potentiation (LTP) and long-term depression (LTD) of excitatory synaptic transmission in the
Tomonari Sumi, Kouji Harada
doaj   +1 more source

Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET [PDF]

, 2010
Flp-In T-REx 293 cells expressing a wild type human M muscarinic acetylcholine receptor construct constitutively and able to express a Receptor Activated Solely by Synthetic Ligand (RASSL) form of this receptor on demand maintained response to the ...
Alvarez-Curto, Elisa, Milligan, Graeme, Pediani, John D., Ward, Richard J.   +3 more
core   +2 more sources