Targeting the M1 muscarinic receptor in Alzheimer's Disease
نویسندگان
چکیده
منابع مشابه
Muscarinic M1 Receptor Coupling to G-protein is Intact in Parkinson's Disease Dementia.
BACKGROUND Postsynaptic cholinergic deficits, including reduced cortical muscarinic M1 receptor coupling to G-proteins, are neurochemical findings postulated to underlie the limited efficacy of presynaptically-targeted cholinergic replacement therapies in Alzheimer's disease (AD). While the loss of M1-G-protein coupling has been associated with β-amyloid (Aβ) burden in AD, the status of M1 coup...
متن کاملM1 Muscarinic Receptor Activation Mediates Cell Death in M1-HEK293 Cells
HEK293 cells have been used extensively to generate stable cell lines to study G protein-coupled receptors, such as muscarinic acetylcholine receptors (mAChRs). The activation of M1 mAChRs in various cell types in vitro has been shown to be protective. To further investigate M1 mAChR-mediated cell survival, we generated stable HEK293 cell-lines expressing the human M1 mAChR. M1 mAChRs were effi...
متن کاملMuscarinic M1 receptor agonists: can they improve cognitive performance?
Due to their potential roles in the pathophysiologies of a number of central nervous system disorders such as depression (Dilsaver, 1986), schizophrenia (Raedler et al. 2006), Alzheimer’s disease (Araujo et al. 1988) and Parkinson’s disease (Ruberg et al. 1982), modulation of the muscarinic system has been a focus of drug discovery for decades. Particular attention has been paid to developing l...
متن کاملFlavonoids with M1 muscarinic acetylcholine receptor binding activity.
Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer's disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at human cloned M1 muscarinic receptors. Several compounds were found to possess competitive binding affinity (Ki=40-110 µM), comparable to that of...
متن کاملThe m1 muscarinic acetylcholine receptor transactivates the EGF receptor to modulate ion channel activity.
Intracellular tyrosine kinases link the G protein-coupled m1 muscarinic acetylcholine receptor (mAChR) to multiple cellular responses. However, the mechanisms by which m1 mAChRs stimulate tyrosine kinase activity and the identity of the kinases within particular signaling pathways remain largely unknown. We show that the epidermal growth factor receptor (EGFR), a single transmembrane receptor t...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Proceedings for Annual Meeting of The Japanese Pharmacological Society
سال: 2018
ISSN: 2435-4953
DOI: 10.1254/jpssuppl.wcp2018.0_sy85-2