Results 181 to 190 of about 8,829 (221)

Primary structure of porcine cardiac muscarinic acetylcholine receptor deduced from the cDNA sequence

FEBS Letters, 1986
The complete amino acid sequence of the porcine cardiac muscarinic acetylcholine receptor has been deduced by cloning and sequencing the cDNA. The tissue location of the RNA hybridizing with the cDNA suggests that this muscarinic receptor species ...
Tai Kubo, Akito Maeda, Katsunori Sugimoto   +2 more
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A model of the human M2 muscarinic acetylcholine receptor

Journal of Computer-Aided Molecular Design, 2002
The M2 muscarinic acetylcholine receptor belongs to the family of rhodopsin like G-Protein Coupled Receptors. This subtype of muscarinic receptors is of special interest because it bears, aside from an orthosteric binding site, also an allosteric binding site.
Kirstin Jöhren, Hans-Dieter Höltje
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Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors

European Journal of Pharmacology, 1996
The interaction of heptane-1,7-bis(dimethyl-3'-phthalimidopropylammonium bromide) (C7/3'-phth), with several agonists, was investigated at the muscarinic M2 receptor in guinea-pig left atria. C7/3'-phth shifted concentration-response curves for the agonists, carbachol, oxotremorine-M and (+)-cis-dioxolane, to the right in a parallel fashion ...
A, Lanzafame, A, Christopoulos, F, Mitchelson   +2 more
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Acetylcholine hyperpolarizes central neurones by acting on an M2 muscarinic receptor

Nature, 1986
Acetylcholine (ACh) is considered to act as a neurotransmitter in the mammalian brain by binding to membrane receptors and bringing about a change in neurone excitability. In the case of muscarinic receptors, cell excitability is usually increased; this effect results from a closure of membrane potassium channels in cortical cells.
T M, Egan, R A, North
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The optimization of a novel selective antagonist for human M2 muscarinic acetylcholine receptor

Bioorganic & Medicinal Chemistry Letters, 2020
Muscarinic acetylcholine receptors (mAChRs) comprise five distinct subtypes denoted M1 to M5. The antagonism of M2 subtype could increase the release of acetylcholine from vesicles into the synaptic cleft and improve postsynaptic functions in the hippocampus via M1 receptor activation, displaying therapeutic potentials for Alzheimer's disease. However,
Miaomiao Li, Chen Huang, Xingyu Wu, Fan Ding, Zhoumi Hu, Yan Zhu, Lanxue Zhao, Lina Hou, Hongzhuan Chen, Hao Wang, Jianrong Xu, Dewei Tang   +11 more
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Allosteric regulation of the binding of [3H]acetylcholine to m2 muscarinic receptors

Biochemical Pharmacology, 1996
Muscarinic receptors of the m2 subtype expressed in Chinese hamster ovary cells were labeled with [methyl-3H]acetylcholine([3H]ACh), and the rate of dissociation in the presence and absence of several compounds known to exert allosteric effects on labeled antagonist binding was observed.
A, Gnagey, J, Ellis
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Constitutive Activity and Inverse Agonism at the M2 Muscarinic Acetylcholine Receptor

The Journal of Pharmacology and Experimental Therapeutics, 2006
Introduction of a single-point mutation (Asn to Tyr) at position 410 at the junction between transmembrane domain 6 and the third extracellular loop of the human M(2) muscarinic acetylcholine (mACh) receptor generated a mutant receptor (N410Y) that possesses many of the hallmark features of a constitutively active mutant receptor.
Nelson, Carl P., Nahorski, Stefan R., Challiss, R.A. John   +2 more
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Structure-Function Studies of Allosteric Agonism at M2 Muscarinic Acetylcholine Receptors

Molecular Pharmacology, 2007
The M2 muscarinic acetylcholine receptor (mAChR) possesses at least one binding site for allosteric modulators that is dependent on the residues (172)EDGE(175), Tyr(177), and Thr(423). However, the contribution of these residues to actions of allosteric agonists, as opposed to modulators, is unknown.
Lauren T, May, Vimesh A, Avlani, Christopher J, Langmead, Hugh J, Herdon, Martyn D, Wood, Patrick M, Sexton, Arthur, Christopoulos   +6 more
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Nature of the oligomers formed by muscarinic m2 acetylcholine receptors in Sf9 cells

European Journal of Pharmacology, 2001
Wild-type, FLAG-tagged, and c-myc-tagged muscarinic m2 receptors extracted in digitonin-cholate from singly and co-infected Sf9 (Spodoptera frugiperda) cells were indistinguishable in their binding of [3H]quinuclidinylbenzilate, either before or after purification.
P, Park, C S, Sum, D R, Hampson, H H, Van Tol, J W, Wells   +4 more
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Interaction of Edrophonium with Muscarinic Acetylcholine M2and M3Receptors

Anesthesiology, 2001
Background It has been reported that edrophonium can antagonize the negative chronotropic effect of carbachol. This study was undertaken to evaluate in detail the interaction of edrophonium with muscarinic Mz and M3 receptors. Methods A functional study was conducted to evaluate the
Y, Tanito, T, Miwa, M, Endou, Y, Hirose, M, Gamoh, H, Nakaya, F, Okumura   +6 more
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