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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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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, T. Bartfai
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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.
E C, Hulme +3 more
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Muscarinic acetylcholine receptors of the chick amnion
Biology Bulletin, 2008The presence of muscarinic (M) acetylcholine receptors in the noninnervated chick amnion makes it possible to analyze their functioning with presynaptic effects excluded. The M receptors of the amnion mediating its contraction were identified by testing with selective antagonists: pirenzepine for M1, methoctramine for M2, 4-diphenylacetoxy-N ...
B N, Manukhin, O V, Boĭko
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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 ...
Y, Kloog +4 more
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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).
S, Tucek, J, Proska
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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 ...
S. V. Penelope Jones +8 more
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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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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 ...
E C, Hulme +4 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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