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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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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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Allosteric antagonists of the muscarinic acetylcholine receptor
Biochemical Pharmacology, 1991For the most part, the interaction of these selective antagonists with muscarinic receptors has been interpreted in the context of simple competitive bimolecular reaction which obeys the law of mass action. In fact, the use of selective antagonists as a pharmacological tool to identify receptor types and subtypes is based on this premise.
Esam E. El-Fakahany, Norman H. Lee
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Muscarinic Acetylcholine Receptor Activators [PDF]
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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Function of muscarinic and nicotinic acetylcholine receptors
Nature, 1976ACETYLCHOLINE receptors in vertebrates can be classified in two categories—nicotinic and muscarinic—on the basis of differential sensitivity to agonist and antagonist compounds1,2. This pharmacological distinction, although useful both in therapeutics and in experimental physiology, has no known biological significance.
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Pharmacological Approaches to Targeting Muscarinic Acetylcholine Receptors
Recent Patents on CNS Drug Discovery, 2014The presence of cholinergic system markers and muscarinic receptor subtypes in several tissues also of nonneuronal type has been largely demonstrated. Acetylcholine, synthesized in the nervous system, can locally contribute to modulate cell proliferation, survival and apoptosis. Considering that the cholinergic system functions are impaired in a number
Claudio Matera, TATA, Ada Maria
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Allosteric interactions at muscarinic acetylcholine receptors
2021This thesis was scanned from the print manuscript for digital preservation and is copyright the author. Researchers can access this thesis by asking their local university, institution or public library to make a request on their behalf. Monash staff and postgraduate students can use the link in the References field.
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Muscarinic Acetylcholine Receptors in the Urinary Tract
2011Muscarinic receptors comprise five cloned subtypes, encoded by five distinct genes, which correspond to pharmacologically defined receptors (M(1)-M(5)). They belong to the family of G-protein-coupled receptors and couple differentially to the G-proteins.
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