Radioligandbindungsstudien : Struktur-Wirkungs-Beziehungen von Antagonisten an muskarinischen, serotonergen und histaminergen Rezeptor-Subtypen [PDF]
, 2008 GPCRs and ligand-gated ion channels mediate a great variety of physiological effects within the human brain and periphery. The search for selective ligands at these target sites as pharmacological tools or new drug candidates is of great interest.
Linder, Matthias
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The Effects of the Selective Muscarinic M3 Receptor Antagonist Darifenacin, and of Hyoscine (scopolamine), on Motion Sickness, Skin Conductance & Cognitive Function [PDF]
, 2018 Aims: The aim of this study was to compare the effects of the selective M3 muscarinic acetylcholine receptor antagonist Darifenacin, oral Hyoscine hydrobromide and Placebo on motion sickness induced by cross-coupled stimulation.
Brian R. Leaker +5 more
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Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 2019 Background The etiology of postural orthostatic tachycardia syndrome (POTS) is yet to be established. The disorder is often misdiagnosed as chronic anxiety or a panic disorder because the autonomic failure in these patients is not severe.
William T. Gunning +4 more
doaj +1 more source
G protein-coupled receptor kinase 2-mediated phosphorylation of ezrin is required for G protein-coupled receptor-dependent reorganization of the actin cytoskeleton [PDF]
, 2005 G protein-coupled receptor kinase 2 (GRK2) phosphorylates and desensitizes activated G protein-coupled receptors (GPCRs). Here, we identify ezrin as a novel non-GPCR substrate of GRK2. GRK2 phosphorylates glutathione S-transferase (GST)-ezrin, but not an
Pitcher, JA, Cant, SH
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C-terminal fusion of eGFP to the bradykinin B-2 receptor strongly affects down-regulation but not receptor internalization or signaling [PDF]
, 2006 A functional comparison was made between the wildtype bradykinin B, receptor (B(2)wt) and the chimera B(2)eGFP (enhanced green-fluorescent protein fused to the C-terminus of B(2)Wt), both stably expressed in HEK 293 cells.
Faussner, A. +4 more
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BMC Urology, 2017 Background This study determined whether changes in the expression of neuregulin (NRG) 1, erbB2 tyrosine kinase (ErbB2) and the M2 muscarinic receptor in the urothelium and detrusor muscle of the rat bladder were associated with partial bladder outlet ...
Seung Woo Yang +2 more
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Identification, expression and functional characterization of M4L, a muscarinic acetylcholine M4 receptor splice variant. [PDF]
PLoS ONE, 2017 Rodent genomic alignment sequences support a 2-exon model for muscarinic M4 receptor. Using this model a novel N-terminal extension was discovered in the human muscarinic acetylcholine M4 receptor. An open reading frame was discovered in the human, mouse
Douglas A Schober +4 more
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Relationship between membrane phosphatidylinositol-4,5-bisphosphate and receptor-mediated inhibition of native neuronal M channels [PDF]
, 2005 The relationship between receptor-induced membrane phosphatidylinositol-4'5'-bisphosphate (PIP2) hydrolysis and M-current inhibition was assessed in single-dissociated rat sympathetic neurons by simultaneous or parallel recording of membrane current and ...
Abogadie, FC +6 more
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On the Autonomic Control of Blood Flow and Secretion in Salivary Glands. Functional and morphological aspects on muscarinic receptor subtypes in different species. [PDF]
, 2008 Parasympathetic nervous activity is the principal stimulus for evoking fluid responses within salivary glands. Concomitantly to the onset of this response, the blood flow increases.
Ryberg, Anders T
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Journal of Pharmacological Sciences, 2010 We investigated pharmacological characteristics of the itch-associated response to chronic dermatitis induced by 4-ethoxymethylene-2-phenyl-2-oxazolin-5-one (oxazolone) repeated application in mice.
Yukihito Tsukumo +2 more
doaj +1 more source