scholarly journals Are positive allosteric modulators of α7 nAChRs clinically safe?

2015 ◽  
Vol 136 (2) ◽  
pp. 217-219 ◽  
Author(s):  
Victor Uteshev
Keyword(s):  
Allosteric Modulators ◽  
Positive Allosteric Modulators ◽  
Α7 Nachrs

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.

2,2-Dimethylcyclopropyl-benzamides: Novel positive allosteric modulators of α7 nAChRs

2009 ◽  
Vol 78 (7) ◽  
pp. 913
Author(s):  
Hans Maag ◽  
Daisy Joe Du Bois ◽  
David G. Loughhead ◽  
Jason Manka ◽  
Dinah Misner ◽  
...  
Keyword(s):  
Allosteric Modulators ◽  
Positive Allosteric Modulators ◽  
Α7 Nachrs

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

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

scholarly journals De Novo Design of Peptidic Positive Allosteric Modulators Targeting TRPV1 with Analgesic Effects

2021 ◽  
pp. 2101716
Author(s):  
Lizhen Xu ◽  
Heng Zhang ◽  
Yunfei Wang ◽  
Xiancui Lu ◽  
Zhenye Zhao ◽  
...  
Keyword(s):  
De Novo ◽  
De Novo Design ◽  
Allosteric Modulators ◽  
Analgesic Effects ◽  
Positive Allosteric Modulators
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