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Muscarinic Acetylcholine Receptors
Current Pharmaceutical Design, 2006Muscarinic acetylcholine receptors mediate diverse physiological functions. At present, five receptor subtypes (M(1) - M(5)) have been identified. The odd-numbered receptors (M(1), M(3), and M(5)) are preferentially coupled to G(q/11) and activate phospholipase C, which initiates the phosphatidylinositol trisphosphate cascade leading to intracellular ...
Masaru Ishii, Yoshihisa Kurachi
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The Muscarinic Receptors [PDF]
, 1984 Muscarinic receptors exist in both peripheral tissues and the central nervous system. Their activation is responsible for all the effects elicited by parasympathetic stimulation in the peripheral organs and modulate ganglionic transmission (Wallis, 1979).
Giancarlo Pepeu, Ileana Marconcini Pepeu
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Acta Pharmacologica et Toxicologica, 1986
Abstract:The muscarinic cholinergic receptors in the urinary bladders of man, guinea pig, rat and rabbit were studied by means of a receptor binding technique, with L‐quinuclidinyl [phenyl4‐3H]benzilate, (‐)3H‐QNB, as radioligand. The potential role of the receptors in the supersensitivity of the rat bladder to muscarinic agonists, following ...
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Abstract:The muscarinic cholinergic receptors in the urinary bladders of man, guinea pig, rat and rabbit were studied by means of a receptor binding technique, with L‐quinuclidinyl [phenyl4‐3H]benzilate, (‐)3H‐QNB, as radioligand. The potential role of the receptors in the supersensitivity of the rat bladder to muscarinic agonists, following ...
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Muscarinic Receptor Antagonists
2016Parasympathetic activity is increased in patients with chronic obstructive pulmonary disease (COPD) and asthma and appears to be the major reversible component of airway obstruction. Therefore, treatment with muscarinic receptor antagonists is an effective bronchodilator therapy in COPD and also in asthmatic patients.
Maria Gabriella Matera, Mario Cazzola
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Muscarinic receptors in rat uterus
European Journal of Pharmacology, 1994The aim of this study was to characterise the muscarinic receptor present in the uterus of the virgin rat. Homogenate binding studies were undertaken using [3H]quinuclidinyl benzilate as the radioligand and atropine (10 microM) to determine non-specific binding.
Tracey A. Gillman +2 more
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Current Protocols in Pharmacology, 1999
AbstractIn the central and peripheral nervous systems, the actions of acetylcholine are mediated by families of ligand gated ion channels and metabotropic receptors. The latter family is composed of muscarinic receptors, since they are selectively activated by muscarine and antagonized by atropine. Five muscarinic receptor subtypes have been identified
Richard M. Eglen +3 more
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AbstractIn the central and peripheral nervous systems, the actions of acetylcholine are mediated by families of ligand gated ion channels and metabotropic receptors. The latter family is composed of muscarinic receptors, since they are selectively activated by muscarine and antagonized by atropine. Five muscarinic receptor subtypes have been identified
Richard M. Eglen +3 more
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Heterogeneity of vascular muscarinic receptors
Journal of Autonomic Pharmacology, 1990SummaryMuscarinic receptors mediate diverse effects on the vasculature. Recently, a consensus has been arrived at with regard to muscarinic receptor classification (Levine and Birdsall, 1989). As a result, it may now be possible to clarify the role of each subtype in the responses of vascular tissues to muscarinic agonists. It is apparent that vascular
R. L. Whiting, R. M. Eglen
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Regulation of muscarinic M2 receptors
Life Sciences, 1997The molecular mechanisms involved in the regulation of muscarinic receptor gene expression are poorly understood. In an effort to gain a better understanding of the regulation of M2 receptors, we have investigated homologous and heterologous regulation of M2 muscarinic receptor protein and gene expression in human embryonic lung fibroblasts (HEL 299 ...
Jonathan Rousell +2 more
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Interaction of Atropine with the Muscarinic Receptor
Nature, 1970WE report here the crystal structures of two muscarinic antagonists of acetylcholine, (−)-(S)-hyoscine hydrobromide1 and (−)-(S)-hyoscyamine hydrobromide (atropine). Correlation of these two structures and that of quinuclidinyl benzilate hydrobromide2 shows marked similarities among the three molecules although they are subjected to very different ...
Trevor J. Petcher, Peter Pauling
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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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