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The properties of muscarinic acetylcholine receptors in the cell line MCM1, derived from an SV40 T-antigen-induced atrial tumor in a transgenic mouse, were determined. Binding studies using the nonselective muscarinic antagonist [3H]quinuclidinyl benzilate, the M1-selective antagonist pirenzepine, and the M2-selective antagonist AFDX-116 indicate that the receptors have the pharmacological properties of the cardiac (M2) receptor subtype. The receptors could be immunoprecipitated with a monoclonal antibody specific for the cardiac receptor, thus confirming the identity of the receptors expressed in these cells. The types of G proteins expressed in the cells were determined by Northern blot analyses: mRNA encoding the alpha subunits of Gs, G(o), and Gi-2, but not Gi-1 or Gi-3, were detected, consistent with previous observations of neonatal mammalian atria. The muscarinic receptors were functionally active, as demonstrated by the ability of the agonist to stimulate phosphoinositide turnover and to inhibit adenylyl cyclase activity. The availability of a mammalian atrial cell line that continues to express the appropriate functionally coupled subtype of muscarinic receptor may provide a useful system for the investigation of the regulation of expression and function of cardiac muscarinic receptors.
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http://dx.doi.org/10.1161/01.res.74.4.752 | DOI Listing |
Biomed Pharmacother
March 2025
Department of Neurochemistry, Institute of Physiology, Czech Academy of Sciences, Prague, Czech Republic. Electronic address:
Antagonists with a long residence time at the receptors are desired for the possibility of reducing daily doses and side effects. KH-5 (1-{2-[4-(hexyloxy)benzoyloxy]ethyl}-1-methyl-1,2,3,6-tetrahydropyridin-1-ium iodide) is the long-acting M-preferring bitopic muscarinic antagonist with a half-life at muscarinic receptors of up to five hours. The binding of 2-hexyloxy and 3-hexyloxy analogues of KH-5 was simulated in silico, compounds were synthesized and their binding and antagonistic properties were measured experimentally in CHO cells expressing individual subtypes of muscarinic acetylcholine receptors.
View Article and Find Full Text PDFJ Assoc Physicians India
March 2025
Professor, Director of the Madras Institute of Neurology, Madras Medical College and Rajiv Gandhi Government General Hospital, Chennai, Tamil Nadu, India.
Introduction: Myasthenia gravis (MG) is characterized by defective transmission of electric impulses across the neuromuscular junction. To date, there is a lack of real-world data to understand its management, specifically in the Indian context. To bridge this gap in clinical knowledge, the current study was designed to understand the clinical management of MG in the Indian population.
View Article and Find Full Text PDFJ Am Chem Soc
March 2025
Department of Life Science and Applied Chemistry, Nagoya Institute of Technology, Showa-ku, Nagoya 466-8555, Japan.
The M muscarinic receptor (MR) is a prototypical G protein-coupled receptor (GPCR) that serves as a model system for understanding ligand recognition and GPCR activation. Here, using vibrational spectroscopy, we identify the mechanisms governing MR activation by its native agonist, acetylcholine. Combined with mutagenesis, computational chemistry, and organic synthetic chemistry, our analyses found that the precise distance between acetylcholine and Asn404, one of the amino acids constituting the ligand-binding site, is important for MR activation and that the N404Q mutant undergoes partial active state-like conformational changes.
View Article and Find Full Text PDFFront Immunol
March 2025
Department of Neurology, Guangzhou First People's Hospital, School of Medicine, South China University of Technology, Guangzhou, China.
Introduction: Myasthenia gravis (MG) is an autoimmune disorder caused by autoantibodies that target the neuromuscular junction, leading to muscle weakness and fatigability. Diagnosis is based on clinical presentation, confirmation of the presence of AChR-Ab, characteristic electromyography findings, and clinical improvement after administration of acetylcholinesterase inhibitors.MG is often associated with thymoma and other autoimmune diseases, but it is rare following allo-HSCT.
View Article and Find Full Text PDFPestic Biochem Physiol
April 2025
Department of Applied Biological Chemistry, Faculty of Agriculture, Kindai University, 3327-204 Nakamachi, Nara 631-8505, Japan; Agricultural Technology and Innovation Research Institute, Kindai University, 3327-204 Nakamachi, Nara 631-8505, Japan. Electronic address:
TMX3 is essential for the functional expression of insect nicotinic acetylcholine receptors (nAChRs) and RIC-3 and UNC-50 modulate it. In addition to these cofactors, NACHO has been shown to enhance functional expression of certain vertebrate nAChRs and an insect homomeric nAChR. Here, we have examined the impact of Drosophila melanogaster NACHO (DmNACHO) on the ACh-induced response amplitude of the fruit fly Dα1/Dβ1 nAChRs coexpressed in Xenopus laevis oocytes with DmRIC-3, DmTMX3 and DmUNC-50 and examined the actions of neonicotinoid insecticides.
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