[PDF] Top 20 Structure Function Studies of Nicotinic Acetylcholine Receptors Using Selective Agonists and Positive Allosteric Modulators
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Structure Function Studies of Nicotinic Acetylcholine Receptors Using Selective Agonists and Positive Allosteric Modulators
... of allosteric modulators has increased due to several beneficial properties for disease ...identifying structure-function relationships of Type I PAMs in "7 ...probed using the Type ... See full document
157
Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the α7 nicotinic acetylcholine receptor
... previous studies have demonstrated that the activity of neurotransmitters acting on ligand-gated ion channels such as the nicotinic acetylcholine receptor (nAChR) can be altered by compounds binding ... See full document
12
Structure Function Studies of Nicotinic Acetylcholine Receptors Using Unnatural Amino Acids and Synthetic Agonist Analogs
... for nicotinic agonists have been proposed for four ...A structure of nicotine bound to the acetylcholine binding protein (AChBP) predicted that the binding partner of the pharmacophore’s ... See full document
262
Niessen, Karin Veronika (2019): Untersuchung der Affinität und Funktionalität von Bispyridiniumverbindungen an nikotinischen Acetylcholinrezeptoren der Subtypen αβδγ (Torpedo californica) und α7 (Homo sapiens). Dissertation, LMU München: Medizinische Fakultät
... neurotransmitter acetylcholine accumulates in cholinergic synapses and disturbs functional activity of nicotinic and muscarinic acetylcholine receptors by overstimulation and subsequent ... See full document
86
Nicotinic acetylcholine receptors: specific antibodies and functions in humoral immunity
... of nicotinic receptors in mito- chondria has initially been discussed in connec- tion with the neuroprotective role of ...other studies, the decrease of mito- chondria membrane potential caused by ... See full document
10
Effects of TI-299423 on Neuronal Nicotinic Acetylcholine Receptors
... the nicotinic receptors found on dopaminergic neurons, they have a large functional contribution to mesolimbic dopamine release [44, 48], with almost all of the dopamine release in the nucleus accumbens ... See full document
95
Organization, evolution and functions of the human and mouse Ly6/uPAR family genes
... Human chromosome 11 contains 5 prostate and testis expressed (PATE) genes while the syntenic region on murine Chromosome 9 contains 15 genes [29]. Recent evidence demonstrates that PATE proteins are much more ... See full document
19
Development of alkaloid derivatives to probe novel α4β2 nicotinic acetylcholine receptor (nAChR) binding sites
... these studies provide some insight into the binding site locations of galanthamine (23) and other nAChR positive allosteric modulators they do not definitively establish the binding site at ... See full document
213
Nematode nicotinic acetylcholine receptors: a single channel study in Ascaris suum and Caenorhabditis elegans
... by nicotinic acetylcholine receptors (nAChRs) plays important roles in both vertebrates and ...for studies of nematode ...for studies of the mechanism of the drug ... See full document
145
Binding Studies of Neuronal Nicotinic Acetylcholine Receptors Expressing Unnatural Amino Acids
... the nicotinic pharmacophore by failing to make a functionally significant additional hydrogen bond to the backbone NH of a conserved leucine residue (L119 in rat ...other nicotinic agonists studied ... See full document
138
Role of GABAA receptors in alcohol use disorders suggested by chronic intermittent ethanol (CIE) rodent model
... down-regulation of EtOH-sensitive mIPSCs and with- drawal anxiety following one or two doses of EtOH. The α2β1γ1 and α4βγ2 receptor subtypes have a similar, not easily distinguishable pharmacological profile so we could ... See full document
20
Disruption of Drug Effects (Dopamine, Nicotine, Pilocarpine, κ Opioid) in Planarians by UV Light
... of selective receptor antagonists; potentiation of ami- nobutyric acid (GABA)-induced current mediated by 122 GABA receptors [8]; and a decreased number of exposed antigenic determinants, which do not ... See full document
6
A novel angiogenic pathway mediated by non neuronal nicotinic acetylcholine receptors
... 7-selective nicotinic receptor agonist 3-(2,4)-dimethoxybenzyli- dene anabaseine (DMXB; ...supernatant using an ELISA for human VEGF according to the manufacturer’s instructions (R&D Systems ... See full document
11
Downregulation of α7 nicotinic acetylcholine receptors in peripheral blood monocytes is associated with enhanced inflammation in preeclampsia
... It is also possible that the downregulation of α7nAChR in circulatory monocytes we found in the present study may not reflect the overall state of the α7nAChR expres- sion in pregnant women with preeclampsia. Anyway, ... See full document
9
Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury
... TC-2559 difumarate (4-(5-ethoxy-3-pyridinyl)-N-methyl- (3E)-3-buten-1-amine difumarate), sazetidine A dihy- drochloride (6-[5-[(2S)-2-azetidinylmethoxy]-3-pyridinyl]-5- hexyn-1-ol dihydrochloride), and ... See full document
13
Smoking cessation in Asians: focus on varenicline
... trials but differed in the evaluation of outcomes and perfor- mance of summary statistic computation. In a clinical trial conducted in 85 Japanese smokers, the researchers evalu- ated the effect of varenicline-assisted ... See full document
6
Drug metabolism and pharmacokinetics in the lead optimisation of novel positive allosteric modulators of α1 strychnine sensitive glycine receptors
... be selective for ...both selective and non-selective NSAIDs 38; 53 ...protective function) in an attempt to maintain efficacy while reducing risk 53; 54 ... See full document
250
Lophotoxin insensitive nematode nicotinic acetylcholine receptors
... secondary structure of polypeptides (Chou and Fasman, 1978), this could generate a structural change that affects ligands binding close to the ACh binding ... See full document
8
Cortical parvalbumin and somatostatin GABA neurons express distinct endogenous modulators of nicotinic acetylcholine receptors
... folding structure or toxin fold due to a similarity to snake venom toxins such as ...impact nicotinic function by altering assembly of receptors in the endoplasmic reticulum and additionally ... See full document
11
Chemical-Scale Studies of the Nicotinic and Muscarinic Acetylcholine Receptors
... with methanethiosulfonate (MTS) derived small molecules (Figure 4.2a). A residue is said to be labeled if, after MTS application, the response of the receptor to ACh is altered 8 . By applying MTS probes both ... See full document
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