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Regulation and trafficking of muscarinic acetylcholine receptors
Neuropharmacology, 2018Fidelity of signal transduction relies on cells expressing the appropriate number of functional receptors. Fluctuation in the total number of muscarinic acetylcholine receptors has been implicated in a range of physiological and pathophysiological processes, and the mechanisms responsible for this regulation represent potential molecular targets for ...
Dmitry Zenko, James N. Hislop
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Biochemical Studies on the Muscarinic Acetylcholine Receptor [PDF]
, 1988 The muscarinic acetylcholine receptor was functionally defined, based on the actions of specific drugs on specific cells or tissues (for a review, see ref. 1). The development of specific radio-labeled ligands (2,3) enabled us to estimate and characterize the ligand-binding sites independently of their functions. Quantitative analysis of the binding of
Haruaki Uchiyama +5 more
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Muscarinic acetylcholine receptors of rat lymphocytes
Biochimica et Biophysica Acta (BBA) - General Subjects, 1983The muscarinic acetylcholine receptors on rat lymphocytes were determined by [3H]quinuclidinyl benzilate binding studies. Binding of [3H]quinuclidinyl benzilate is rapid (half saturation occurred within 120 s) and highly specific. Muscarinic receptors reveal high lability. The number of receptors on plasma membrane depends on time of incubation as well
Włodzimierz Maśliński +3 more
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Regulation of muscarinic acetylcholine receptor signaling
Pharmacology & Therapeutics, 2003Multiple mechanisms regulate the signaling of the five members of the family of the guanine nucleotide binding protein (G protein)-coupled muscarinic acetylcholine (ACh) receptors (mAChRs). Following activation by classical or allosteric agonists, mAChRs can be phosphorylated by a variety of receptor kinases and second messenger-regulated kinases.
Björn Kaiser, Chris J. van Koppen
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Constitutive Activity of Muscarinic Acetylcholine Receptors
Journal of Receptors and Signal Transduction, 2006We review the literature describing constitutive activity of the five muscarinic acetylcholine receptors in native and recombinant systems and discuss the effect of constitutive activity on muscarinic pharmacology in the context of modern models of receptor activation.
Tracy A. Spalding, Ethan S. Burstein
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Inhaled muscarinic acetylcholine receptor antagonists for treatment of COPD.
Current Medicinal Chemistry, 2013Bronchodilators, generally administered via metered dose or dry powder inhalers, are the mainstays of pharmacological treatment of stable COPD. Inhaled long-acting beta-agonists (LABA) and anticholinergics are the bronchodilators primarily used in the ...
P. Montuschi +3 more
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Muscarinic Acetylcholine Receptors
2004Muscarinic acetylcholine receptors are members of the G-protein-coupled receptor superfamily. There are five genes encoding the muscarinic receptors, which are expressed to different extents in a variety of tissues, including cardiac and smooth muscle, secretory glands, and neurons and glial cells in the central and peripheral nervous systems ...
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Molecular Biology of Muscarinic Acetylcholine Receptors
Critical Reviews™ in Neurobiology, 1996Following the molecular cloning of five distinct muscarinic acetylcholine receptor (mAChR) genes, the last decade has witnessed an explosion of new knowledge about how mAChRs function at a molecular level. These studies have been greatly facilitated by the molecular characterization of the many components of the signal transduction pathways activated ...
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Immunochemical Studies of the Muscarinic Acetylcholine Receptor
Journal of Receptor Research, 1987Muscarinic receptors have been purified from calf forebrain plasma cell membranes by affinity chromatography on a dexetimide-agarose gel. SDS-PAGE analysis showed a single 70 kDa band. Monoclonal antibodies have been prepared against these affinity purified 70 kDa protein(s).
A. Convents +7 more
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Muscarinic Acetylcholine Receptor Activators [PDF]
, 2014 Modulation of muscarinic acetylcholine receptors (mAChRs) is one of the most attractive therapeutic strategies for the treatment of schizophrenia. Pilot clinical studies of the M1/M4 mAChR-preferring agonist xanomeline as well as animal studies using M1–M5 mAChR knockout mice suggest that selective activation of M1 and/or M4 mAChRs is a key concept in ...
Takaaki Sumiyoshi +2 more
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