Journal of Pharmacological Sciences, 2006 .: In mouse intestinal smooth muscle cells held at −50 mV, carbachol evoked an atropine-sensitive inward current in the intracellular presence of Cs+.
Takashi Sakamoto +6 more
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Muscarinic M2‐receptors enhance polyphosphoinositol release in rat gastric mucosal cells
FEBS Letters, 1986 Muscarinic receptor types and their effects on the inositol phosphate second messenger system were studied in enzymatically dispersed rat gastric mucosal cells. Radioreeeptor binding studies indicated the presence of a single class of binding sites (4860 ± 875 ) and affinities of 0.42 ± 0.12 nM, 176 ± 32 nM and 13 μM for N‐methylscopolamine ...
Pfeiffer, Andreas +2 more
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Internalization of the m2 Muscarinic Acetylcholine Receptor [PDF]
Journal of Biological Chemistry, 1997 Robin Pals-Rylaarsdam +5 more
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The coupling of the M2 muscarinic receptor to its G protein is voltage dependent.
PLoS ONE, 2019 G protein coupled receptors (GPCRs) participate in the majority of signal transduction processes in the body. Specifically, the binding of an external agonist promotes coupling of the GPCR to its G protein and this, in turn, induces downstream signaling.
Yair Ben-Chaim +2 more
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Quantitative surface field analysis: learning causal models to predict ligand binding affinity and pose. [PDF]
, 2018 We introduce the QuanSA method for inducing physically meaningful field-based models of ligand binding pockets based on structure-activity data alone. The method is closely related to the QMOD approach, substituting a learned scoring field for a pocket ...
Cleves, Ann E, Jain, Ajay N
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D₂ Dopamine Receptors Colocalize Regulator of G-Protein Signaling 9-2 (RGS9-2) via the RGS9 DEP Domain, and RGS9 Knock-Out Mice Develop Dyskinesias Associated with Dopamine Pathways [PDF]
, 2005 Regulator of G-protein signaling 9-2 (RGS9-2), a member of the RGS family of Gα GTPase accelerating proteins, is expressed specifically in the striatum, which participates in antipsychotic-induced tardive dyskinesia and in levodopa-induced dyskinesia. We
Axelrod, Jeffrey D. +10 more
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A Role for the Kolliker-Fuse Nucleus in Cholinergic Modulation of Breathing at Night During Wakefulness and NREM Sleep [PDF]
, 2010 For many years, acetylcholine has been known to contribute to the control of breathing and sleep. To probe further the contributions of cholinergic rostral pontine systems in control of breathing, we designed this study to test the hypothesis that ...
Bonis, Joshua M. +8 more
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Voltage dependence of M2 muscarinic receptor antagonists and allosteric modulators
Biochemical PharmacologyMuscarinic receptors are G protein-coupled receptors (GPCRs) that play a role in various physiological functions. Previous studies have shown that these receptors, along with other GPCRs, are voltage-sensitive; both their affinity toward agonists and their activation are regulated by membrane potential.
Shimrit, Hazan +2 more
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Muscarinic acetylcholine receptor M2 (CHRM2; HM2) [PDF]
Science-Business eXchange, 2012 openaire +1 more source
Exploring functional motions of muscarinic acetylcholine M2 receptor
, 2020 G-protein bağlı reseptörler (GPRs) en büyük sinyal protein ailesidir ve bu yüzden işleyiş mekanızmalarının altında yatan dinamik etkenlerin anlaşılması ilaç tasarımında büyük bir öneme sahiptir. Bu güne kadar yapılan pek çok çalışma olmasına rağmen, inaktif ve aktif yapılar arasında gerçekleşen kolektif konformasyonel değişimlerin özellikleri ve ...
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