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B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor 1.0.0

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charles.hoyt@scai.fraunhofer.de at 2019-02-27 16:20:50.725670
Authors
Sandra Spalek
Contact
charles.hoyt@scai.fraunhofer.de
License
CC BY 4.0
Copyright
Copyright © 2018 Fraunhofer Institute SCAI, All rights reserved.
Number Nodes
12
Number Edges
19
Number Components
1
Network Density
0.143939393939394
Average Degree
1.58333333333333
Number Citations
1
Number BEL Errors
0

Content Statistics

Network Overlap

The node-based overlap between this network and other networks is calculated as the Szymkiewicz-Simpson coefficient of their respective nodes. Up to the top 10 are shown below.

Network Overlap
albuquerque2009 v1.0.0 25%
Nicotinic acetylcholine receptor signalling: roles in Alzheimer's disease and amyloid neuroprotection. v1.0.0 25%
Role of the nicotinic acetylcholine receptor in Alzheimer's disease pathology and treatment v1.0.1 25%
NACHO Mediates Nicotinic Acetylcholine Receptor Function throughout the Brain v1.0.0 25%
Discriminative Stimulus Properties of S(−)-Nicotine: “A Drug for All Seasons v1.0.0 17%
Nicotinic Acetylcholine Receptors and Nicotinic Cholinergic Mechanisms of the Central Nervous System v1.0.0 17%
Neural Systems Governed by Nicotinic Acetylcholine Receptors: Emerging Hypotheses v1.0.0 17%
Nicotinic Receptor Abnormalities of Alzheimer’s Disease: Therapeutic Implications v1.0.0 17%
Up-regulation of Nicotinic Receptors by Nicotine Varies with Receptor Subtype v1.0.0 12%
Selective activation of α7 nicotinic acetylcholine receptor by PHA-543613 improves Aβ25-35-mediated cognitive deficits in mice v1.0.0 9%

Sample Edges

a(CHEBI:"1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-3-isoxazolyl)urea") increases complex(a(GO:membrane), a(PUBCHEM:16068384)) View Subject | View Object

PNU-120596 and B-973 enhanced [3H]A-585539 binding to rat brain membranes (Fig. 5B,C) PubMed:28132910

Annotations
MeSH
Brain

a(CHEBI:"1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-3-isoxazolyl)urea") increases complex(a(MESH:"alpha7 Nicotinic Acetylcholine Receptor"), a(PUBCHEM:16068384)) View Subject | View Object

[3H]A-585539 saturation binding revealed that B-973 and PNU-120596 increased the affinity of the receptor for [3H]A-585539 approximately 4-fold without changing the apparent Bmax (Fig. 5D) PubMed:28132910

a(CHEBI:epibatidine) decreases complex(a(MESH:"alpha7 Nicotinic Acetylcholine Receptor"), a(PUBCHEM:16068384)) View Subject | View Object

As expected, binding was inhibited by epibatidine (Fig. 5A) PubMed:28132910

a(HBP:"B-973") increases act(a(MESH:"alpha7 Nicotinic Acetylcholine Receptor")) View Subject | View Object

Peak current was increased 2-fold and 6-fold relative to 3 mM acetylcholine in 300 nM and 1 μM B-973, respectively (Fig. 1C) PubMed:28132910

a(HBP:"B-973") negativeCorrelation act(a(MESH:"alpha7 Nicotinic Acetylcholine Receptor")) View Subject | View Object

B-973 slows receptor deactivation dramatically (Fig. 4A) PubMed:28132910

Sample Nodes

a(CHEBI:acetylcholine)

In-Edges: 64 | Out-Edges: 36 | Classes: 1 | Explore Neighborhood | Download JSON

a(CHEBI:epibatidine)

In-Edges: 13 | Out-Edges: 5 | Explore Neighborhood | Download JSON

p(MGI:Chrna7)

In-Edges: 18 | Out-Edges: 21 | Explore Neighborhood | Download JSON

a(CHEBI:"1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-3-isoxazolyl)urea")

In-Edges: 0 | Out-Edges: 3 | Explore Neighborhood | Download JSON

a(MESH:"alpha7 Nicotinic Acetylcholine Receptor")

In-Edges: 51 | Out-Edges: 36 | Explore Neighborhood | Download JSON

About

BEL Commons is developed and maintained in an academic capacity by Charles Tapley Hoyt and Daniel Domingo-Fernández at the Fraunhofer SCAI Department of Bioinformatics with support from the IMI project, AETIONOMY. It is built on top of PyBEL, an open source project. Please feel free to contact us here to give us feedback or report any issues. Also, see our Publishing Notes and Data Protection information.

If you find BEL Commons useful in your work, please consider citing: Hoyt, C. T., Domingo-Fernández, D., & Hofmann-Apitius, M. (2018). BEL Commons: an environment for exploration and analysis of networks encoded in Biological Expression Language. Database, 2018(3), 1–11.