Results 11 to 20 of about 5,198 (201)

Molecular Conversion of Muscarinic Acetylcholine Receptor M5 to Muscarinic Toxin 7 (MT7)-Binding Protein [PDF]

Toxins, 2011
Muscarinic toxin 7 (MT7) is a mamba venom peptide that binds selectively to the M1 muscarinic acetylcholine receptor. We have previously shown that the second (ECL2) and third (ECL3) extracellular loops of the M1 receptor are critically involved in ...
Katja Näreoja, Johnny Näsman, Sergio Rondinelli   +2 more
doaj   +3 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

Muscarinic acetylcholine receptor M5 is involved in spermatogenesis through the modification of cell-cell junctions. [PDF]

Reproduction, 2021
Muscarinic acetylcholine receptor (mAChR) antagonists have been reported to decrease male fertility; however, the roles of mAChRs in spermatogenesis and the underlying mechanisms are not understood yet. During spermatogenesis, extensive remodeling between Sertoli cells and/or germ cells interfaces takes place to accommodate the transport of developing ...
Han X, Zhang C, Ma X, Yan X, Xiong B, Shen W, Yin S, Zhang H, Sun Q, Zhao Y.   +9 more
europepmc   +4 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

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators [PDF]

Molecular Pharmacology, 2016
Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular mechanisms of action remain unknown. Using radioligand-binding and functional assays of inositol phosphate (IP) accumulation and Ca(2+) mobilization in a recombinant cell line stably expressing the ...
Alice E, Berizzi, Patrick R, Gentry, Patricia, Rueda, Sandra, Den Hoedt, Patrick M, Sexton, Christopher J, Langmead, Arthur, Christopoulos   +6 more
  +8 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

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

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

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

Crystal structure of the M₅ muscarinic acetylcholine receptor [PDF]

Proceedings of the National Academy of Sciences, 2019
AbstractThe human M5 muscarinic acetylcholine receptor (mAChR) has recently emerged as an exciting therapeutic target for treating a range of disorders, including drug addiction. However, a lack of structural information for this receptor subtype has limited further drug development and validation.
Ziva Vuckovic, Patrick R. Gentry, Alice E. Berizzi, Kunio Hirata, Swapna Varghese, Geoff Thompson, Emma T. van der Westhuizen, Wessel A.C. Burger, Raphaёl Rahmani, Celine Valant, Christopher J. Langmead, Craig W. Lindsley, Jonathan Baell, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos, David M. Thal   +16 more
openaire   +3 more sources