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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.
Solomon H. Snyder, Henry I. Yamamura
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The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation.
ACS Chemical Neuroscience, 2018The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications.
Aaron M. Bender +2 more
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ACS Chemical Neuroscience, 2018
Abnormal hippocampal activity has been linked to impaired cognitive performance in Alzheimer's disease and schizophrenia, leading to a hypothesis that normalization of this activity may be therapeutically beneficial.
M. Popiolek +8 more
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Abnormal hippocampal activity has been linked to impaired cognitive performance in Alzheimer's disease and schizophrenia, leading to a hypothesis that normalization of this activity may be therapeutically beneficial.
M. Popiolek +8 more
semanticscholar +1 more source
Structure and activation of muscarinic acetylcholine receptors
Biochemical Society Transactions, 2003A homology model of the M1 muscarinic acetylcholine receptor, based on the X-ray structure of bovine rhodopsin, has been used to interpret the results of scanning and point mutagenesis studies on the receptor's transmembrane (TM) domain. Potential intramolecular interactions that are important for the stability of the protein fold have been identified.
Zhi-Liang Lu +3 more
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Muscarinic acetylcholine receptors and airway diseases
Pharmacology & Therapeutics, 2003Parasympathetic nerves provide the dominant autonomic innervation of the airways. Release of acetylcholine from parasympathetic nerves activates postjunctional muscarinic receptors present on airway smooth muscle, submucosal glands, and blood vessels to cause bronchoconstriction, mucus secretion, and vasodilatation, respectively.
Coulson, Fiona R., Fryer, Allison D.
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Muscarinic acetylcholine receptors in cat iris
Biochemical Pharmacology, 1979Abstract The binding of tritium labeled N- methyl -4- piperidylbenzilate ([ 3 H ]-4- NMPB ) to fractions obtained from cat irides was investigated. The binding of this highly potent muscarinic antagonist to the cat iris consisted of two components: (a) high affinity binding sites with low capacity and (b) low affinity binding sites ...
Amos D. Korczyn +4 more
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Muscarinic Acetylcholine Receptors
1988The central and peripheral actions of the endogenous neurotransmitter acetylcholine (ACh) are exerted at two main types of receptor, present in both the central and peripheral nervous system of all mammals. Their definition and pharmacological classification dates back to the work of Sir Henry Dale (1914), who demonstrated that certain actions of ACh ...
J. Järv, Tamas Bartfai
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Allosteric modulation of muscarinic acetylcholine receptors
Trends in Pharmacological Sciences, 1995Five subtypes of muscarinic acetylcholine receptors have been identified in mammalian tissues, but the selectivity of ligands that are active at these receptors is low. It is possible, however, that selective compounds may be developed by targeting their allosteric site(s).
Jan Proška, Stanislav Tuček
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The conformational switch in muscarinic acetylcholine receptors
Life Sciences, 2001The recently-determined structure of rhodopsin has provided a suitable basis for modeling the three-dimensional structure of the M1 muscarinic acetylcholine receptor. Using this as a framework for interpreting mutagenesis studies, we have been able to suggest most of the contacts which the receptor makes with acetylcholine and many of the ...
Z-L. Lu +4 more
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Muscarinic Acetylcholine Receptors
1992In 1914 Dale discovered two types of response to acetylcholine, one mimicked by muscarine and one by nicotine (Dale 1914; Dale and Ewin, 1914). This led to the subsequent discovery of nicotinic and muscarinic acetylcholine receptors. In addition to their pharmacological differences, muscarinic and nicotinic receptors can be differentiated by the ...
Allan I. Levey +8 more
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