Results 211 to 220 of about 34,397 (264)

Desensitization of Human Muscarinic Acetylcholine Receptor m2 Subtypes Is Caused by Their Sequestration/Internalization

Journal of Biochemistry, 1998
Desensitization of human muscarinic acetylcholine receptor m2 subtypes (hm2 receptors) stably expressed in chinese hamster ovary cells was measured as decreases in the carbamylcholine-stimulated [35S]GTPgammaS binding activity in membrane preparations after pre-treatment of cells with carbamylcholine.
H, Tsuga, K, Kameyama, T, Haga
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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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Lack of m2 muscarinic acetylcholine receptor mRNA in rat lymphocytes

Journal of Neuroimmunology, 1994
The presence of muscarinic acetylcholine receptors on lymphocytes has been demonstrated by radioligand binding experiments. Although the specific subtype(s) of muscarinic acetylcholine receptors expressed in lymphocytes is still unknown, some reports suggest the presence of the m2 subtype.
Costa, P, Castoldi, A. F, Traver, D. J, Costa, L. G.   +3 more
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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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Crystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with NMS (Hg-derivative)

, 2018
Human muscarinic receptor M2 is one of the five subtypes of muscarinic receptors belonging to the family of G-protein-coupled receptors. Muscarinic receptors are targets for multiple neurodegenerative diseases.
Ryoji Suno, Sangbae Lee, S. Maeda, S. Yasuda, K. Yamashita, K. Hirata, S. Horita, Tawaramoto, Hirokazu Tsujimoto, T. Murata, M. Kinoshita, Masayuki Yamamoto, B. Kobilka, N. Vaidehi, S. Iwata, T. Kobayashi   +15 more
semanticscholar   +1 more source

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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