Results 241 to 250 of about 30,424 (296)

Cirrhotic Cardiomyopathy: Bridging Hepatic and Cardiac Pathophysiology in the Modern Era. [PDF]

J Clin Med
Lupu D, Scârneciu CC, Țînț D, Tudoran C.   +3 more
europepmc   +1 more source

Cryo-EM reveals an extrahelical allosteric binding site at the M₅ mAChR. [PDF]

Nat Commun
Burger WAC, Mobbs JI, Rana B, Wang J, Joshi K, Gentry PR, Yeasmin M, Venugopal H, Bender AM, Lindsley CW, Miao Y, Christopoulos A, Valant C, Thal DM.   +13 more
europepmc   +1 more source

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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
semanticscholar   +3 more sources

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
openaire   +2 more sources

The structure of the third intracellular loop of the muscarinic acetylcholine receptor M2 subtype [PDF]

FEBS Letters, 2006
We have examined whether the long third intracellular loop (i3) of the muscarinic acetylcholine receptor M2 subtype has a rigid structure. Circular dichroism (CD) and nuclear magnetic resonance spectra of M2i3 expressed in and purified from Escherichia coli indicated that M2i3 consists mostly of random coil.
S. Ichiyama, Yoshiaki Oka, K. Haga, S. Kojima, Y. Tateishi, M. Shirakawa, T. Haga   +6 more
semanticscholar   +3 more sources

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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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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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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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
openaire   +2 more sources