(373) Muscarinic M4 Positive Allosteric Modulators are Antinociceptive in Mouse Inflammatory Pain Models

2019 ◽  
Vol 20 (4) ◽  
pp. S67 ◽  
Author(s):  
K. Gurba ◽  
S. Vogt ◽  
R. Gereau
Keyword(s):  
Inflammatory Pain ◽  
Allosteric Modulators ◽  
Pain Models ◽  
Positive Allosteric Modulators

scholarly journals Effects of alpha 7 positive allosteric modulators in murine inflammatory and chronic neuropathic pain models

2013 ◽  
Vol 65 ◽  
pp. 156-164 ◽  
Author(s):  
Kelen Freitas ◽  
Sudeshna Ghosh ◽  
F. Ivy Carroll ◽  
Aron H. Lichtman ◽  
M. Imad Damaj
Keyword(s):  
Neuropathic Pain ◽  
Allosteric Modulators ◽  
Chronic Neuropathic Pain ◽  
Pain Models ◽  
Positive Allosteric Modulators ◽  
Alpha 7

Antinociceptive effects of potent, selective and brain penetrant muscarinic M4 positive allosteric modulators in rodent pain models

2020 ◽  
Vol 1737 ◽  
pp. 146814
Author(s):  
Steven M. Grauer ◽  
Raul Sanoja ◽  
Dominic Poulin ◽  
Harunor Rashid ◽  
Nina Jochnowitz ◽  
...  
Keyword(s):  
Allosteric Modulators ◽  
Pain Models ◽  
Antinociceptive Effects ◽  
Positive Allosteric Modulators

SAR Studies on mGlu5 Receptor Positive Allosteric Modulators (2003- 2013)

2014 ◽  
Vol 14 (15) ◽  
pp. 1789-1841 ◽  
Author(s):  
Junliang Hao ◽  
Hui Xiong
Keyword(s):  
Allosteric Modulators ◽  
Sar Studies ◽  
Positive Allosteric Modulators

scholarly journals A Promising Chemical Series of Positive Allosteric Modulators of the μ-Opioid Receptor that Enhance the Antinociceptive Efficacy of Opioids but not their Adverse Effects

2021 ◽  
pp. 108673
Author(s):  
Kerri D. Pryce ◽  
Hye Jin Kang ◽  
Farhana Sakloth ◽  
Yongfeng Liu ◽  
Susan Khan ◽  
...  
Keyword(s):  
Adverse Effects ◽  
Opioid Receptor ◽  
Allosteric Modulators ◽  
Μ Opioid Receptor ◽  
Positive Allosteric Modulators

scholarly journals Novel positive allosteric modulators of GABAA receptors: Do subtle differences in activity at α1 plus α5 versus α2 plus α3 subunits account for dissimilarities in behavioral effects in rats?

2010 ◽  
Vol 34 (2) ◽  
pp. 376-386 ◽  
Author(s):  
Miroslav M. Savić ◽  
Samarpan Majumder ◽  
Shengming Huang ◽  
Rahul V. Edwankar ◽  
Roman Furtmüller ◽  
...  
Keyword(s):  
Gabaa Receptors ◽  
Behavioral Effects ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators

Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach

2021 ◽  
Vol 214 ◽  
pp. 113189
Author(s):  
István Ledneczki ◽  
Pál Tapolcsányi ◽  
Eszter Gábor ◽  
András Visegrády ◽  
Márton Vass ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Allosteric Modulators ◽  
Scaffold Hopping ◽  
Α7 Nicotinic Acetylcholine Receptor ◽  
Nicotinic Acetylcholine ◽  
Positive Allosteric Modulators

scholarly journals Natural Polyhydroxy Flavonoids, Curcuminoids, and Synthetic Curcumin Analogs as α7 nAChRs Positive Allosteric Modulators

2021 ◽  
Vol 22 (2) ◽  
pp. 973
Author(s):  
Marta Ximenis ◽  
José Mulet ◽  
Salvador Sala ◽  
Francisco Sala ◽  
Manuel Criado ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Allosteric Modulators ◽  
Α7 Nicotinic Acetylcholine Receptor ◽  
Curcumin Analogues ◽  
Curcumin Derivatives ◽  
Curcumin Analogs ◽  
Naturally Occurring ◽  
Α7 Nachr ◽  
Positive Allosteric Modulators ◽  
Α7 Nachrs

The α7 nicotinic acetylcholine receptor (α7 nAChR) is a ligand-gated ion channel that is involved in cognition disorders, schizophrenia, pain, and inflammation. Allosteric modulation of this receptor might be advantageous to reduce the toxicity in comparison with full agonists. Our previous results obtained with some hydroxy-chalcones, which were identified as positive allosteric modulators (PAMs) of α7 nAChR, prompted us to evaluate the potential of some structurally related naturally occurring flavonoids and curcuminoids and some synthetic curcumin analogues, with the aim of identifying new allosteric modulators of the α7 nAChR. Biological evaluation showed that phloretin, demethoxycurcumin, and bis-demethoxicurcuming behave as PAMs of α7 nAChR. In addition, some new curcumin derivatives were able to enhance the signal evoked by ACh; the activity values found for the tetrahydrocurcuminoid analog 23 were especially promising.

scholarly journals Discovery of small molecule positive allosteric modulators of the secretin receptor

2021 ◽  
pp. 114451
Author(s):  
Daniela G. Dengler ◽  
Kaleeckal G. Harikumar ◽  
Sirkku Pollari ◽  
Qing Sun ◽  
Brock T. Brown ◽  
...  
Keyword(s):  
Small Molecule ◽  
Allosteric Modulators ◽  
Secretin Receptor ◽  
Positive Allosteric Modulators
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