Results 11 to 20 of about 20,015 (223)

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of ¹⁸F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]

ChemMedChem
The muscarinic acetylcholine receptor subtype M3 is validated as a promising target for imaging and therapy in breast cancer. Transcriptomic and proteomic profiling reveal its overexpression, particularly in triple‐negative breast cancer.
Herrera-Rueda MA, Boateng MA, Wuest M, West FG, Wuest F.   +4 more
europepmc   +3 more sources

M5 positive allosteric modulation alleviates parkinsonian motor deficits. [PDF]

PLoS ONE
Parkinson'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, Dominic Hall, Morgan Kaplan, Sarah Garan, Tyler Eichner, Mark S Moehle   +5 more
doaj   +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

Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor

ACS Chemical Neuroscience, 2021
The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders.
Wessel A. C. Burger, P. Gentry, Alice E. Berizzi, Ziva Vuckovic, E. T. van der Westhuizen, Geoff V. Thompson, M. Yeasmin, C. Lindsley, P. Sexton, C. Langmead, A. Tobin, A. Christopoulos, C. Valant, D. Thal   +13 more
semanticscholar   +3 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

Loss of M5 muscarinic acetylcholine receptors leads to cerebrovascular and neuronal abnormalities and cognitive deficits in mice

Neurobiology of Disease, 2006
The M5 muscarinic acetylcholine receptor (M5R) has been shown to play a crucial role in mediating acetylcholine-dependent dilation of cerebral blood vessels.
Runa Araya, Takanori Noguchi, Munehiro Yuhki, Naohito Kitamura, Makoto Higuchi, Takaomi C. Saido, Kenjiro Seki, Shigeyoshi Itohara, Masako Kawano, Kentaro Tanemura, Akihiko Takashima, Kazuyuki Yamada, Yasushi Kondoh, Iwao Kanno, Jürgen Wess, Masahisa Yamada   +15 more
doaj   +3 more sources

The M1 muscarinic acetylcholine receptor subtype is important for retinal neuron survival in aging mice

Scientific Reports, 2019
Muscarinic acetylcholine receptors have been implicated as potential neuroprotective targets for glaucoma. We tested the hypothesis that the lack of a single muscarinic receptor subtype leads to age-dependent neuron reduction in the retinal ganglion cell
Panagiotis Laspas, Mayagozel B. Zhutdieva, Christoph Brochhausen, Aytan Musayeva, Jenia Kouchek Zadeh, Norbert Pfeiffer, Ning Xia, Huige Li, Juergen Wess, Adrian Gericke   +9 more
doaj   +2 more sources

Design, Synthesis, and Evaluation of a New Fluorescent Ligand for the M₂ Muscarinic Acetylcholine Receptor. [PDF]

ACS Med Chem Lett
The M2 muscarinic acetylcholine receptor (M2R) is a G protein-coupled receptor involved in regulating cardiovascular functions and mediation of central muscarinic effects, such as movement, temperature control, and antinociceptive responses.
Szabó R, Szepesi Kovács D, Kiss DJ, Yazdi ZN, Tóth AD, Brea J, Loza MI, Meszéna D, Wittner L, Ulbert I, Volk B, Hunyady L, Keserű GM.   +12 more
europepmc   +2 more sources

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375). [PDF]

Addiction Biology, 2013
AbstractCocaine use disorder (CUD) remains a debilitating health problem in the United States for which there are no Food and Drug Administration‐approved treatment options. Accumulating anatomical and electrophysiological evidence indicates that the muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) plays a critical role in the regulation of the
P. Gentry, M. Kokubo, T. Bridges, Nathan R Kett, J. Harp, Hyekyung P. Cho, Emery Smith, P. Chase, P. Hodder, C. Niswender, J. Daniels, P. Conn, M. Wood, C. Lindsley   +13 more
semanticscholar   +3 more sources

Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation. [PDF]

The Journal of Physical Chemistry B, 2012
By performing homology modeling, molecular docking, and molecular dynamics (MD) simulations, we have developed three-dimensional (3D) structural models of the M5 muscarinic acetylcholine receptor (mAChR) and two complexes for M5 mAChR binding with antagonists SVT-40776 and solifenacin in the environment of lipid bilayer and solvent water.
Xiaoqin Huang, Guangrong Zheng, C. Zhan
semanticscholar   +3 more sources