Results 1 to 10 of about 2,626 (131)

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

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

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

Downstream Signaling of Muscarinic M₄ Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

Pharmacol Res Perspect
ABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M, Playle C, Palchaudhuri M, Hucke O, Gross U, Ursu D.   +5 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

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

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

All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium [PDF]

Scientific Reports, 2017
AbstractClinical and experimental studies indicate that muscarinic acetylcholine receptors are potential pharmacological targets for the treatment of neurological diseases. Although these receptors have been described in human, bovine and rat cerebral microvascular tissue, a subtype functional characterization in mouse brain endothelium is lacking ...
Radu, Beatrice Mihaela, Osculati, Antonio Marco Maria, Suku, Eda, Banciu, Adela, Tsenov, Grygoriy, Merigo, Flavia, Di Chio, Marzia, Banciu, Daniel Dumitru, Tognoli, Cristina, Kacer, Petr, Giorgetti, Alejandro, Radu, Mihai, Bertini, Giuseppe, Fabene, Paolo   +13 more
openaire   +4 more sources