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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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Muscarinic Receptor Trafficking
2011Knowledge of the mechanisms responsible for the trafficking of neurotransmitter receptors away from the cell surface is of obvious importance in understanding what regulates their expression and function. This chapter will focus on the mechanisms responsible for the internalization and degradation of muscarinic receptors.
Cindy, Reiner, Neil M, Nathanson
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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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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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Structure and Regulation of Muscarinic Receptors
Annual Review of Physiology, 1989Our knowledge of muscarinic receptor structure, mechanism, and regulation has increased enormously over the past five years. At this time, expression of receptor subtype and coupling via signal transducing elements to specific effector systems seems to be cell or tissue specific events.
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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 ...
P J, Pauling, T J, Petcher
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Endocytosis and recycling of muscarinic receptors
Life Sciences, 1999Agonist stimulation causes the endocytosis of many G protein-coupled receptors, including muscarinic acetylcholine receptors. In this study we have investigated the agonist-triggered trafficking of the M3 muscarinic receptor expressed in SH-SY5Y human neuroblastoma cells.
J M, Edwardson, P G, Szekeres
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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.
J N, Pennefather +2 more
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Antidepressants and the Muscarinic Acetylcholine Receptor
Archives of General Psychiatry, 1977Several tricyclic antidepressants have been assessed for their potency in binding to the muscarinic acetylcholine receptor of brain and intestine. Amitriptyline hydrochloride is about ten times as potent as imipramine hydrochloride. Dimethylated drugs are more potent than monomethylated ones.
S H, Snyder, H I, Yamamura
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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 ...
P J, Barnes, E B, Haddad, J, Rousell
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