scholarly journals Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors

2017 ◽  
Vol 91 (6) ◽  
pp. 576-585 ◽  
Author(s):  
Anja Probst Larsen ◽  
Sabine Fièvre ◽  
Karla Frydenvang ◽  
Pierre Francotte ◽  
Bernard Pirotte ◽  
...  
Keyword(s):  
Structure Function ◽  
Kainate Receptors ◽  
Allosteric Modulators ◽  
Function Study ◽  
Positive Allosteric Modulators

scholarly journals 5-Arylbenzothiadiazine Type Compounds as Positive Allosteric Modulators of AMPA/Kainate Receptors

2011 ◽  
Vol 3 (1) ◽  
pp. 25-29 ◽  
Author(s):  
Umberto M. Battisti ◽  
Krzysztof Jozwiak ◽  
Giuseppe Cannazza ◽  
Giulia Puia ◽  
Gabriella Stocca ◽  
...  
Keyword(s):  
Kainate Receptors ◽  
Allosteric Modulators ◽  
Positive Allosteric Modulators

scholarly journals FAILURE OF PANCREATIC ALPHA CELLS TO RESPOND TO HYPOGLYCEMIA IS LINKED TO IMPAIRED GLUTAMATE RECEPTOR SIGNALING IN DIABETES

2021 ◽  
Author(s):  
Julia Katharina Panzer ◽  
Alejandro Tamayo ◽  
Alejandro Caicedo
Keyword(s):  
Type 1 Diabetes ◽  
Glucagon Secretion ◽  
Kainate Receptors ◽  
Kainate Receptor ◽  
Allosteric Modulators ◽  
Alpha Cells ◽  
Receptor Signaling ◽  
Pancreatic Alpha Cells ◽  
Positive Allosteric Modulators

Glucagon secretion from the pancreatic alpha cells is crucial to prevent hypoglycemia. People with type 1 diabetes, however, lose this glucoregulatory mechanism and are susceptible to dangerous insulin treatment-induced hypoglycemia. We established that activating glutamate receptors of the AMPA/kainate type in alpha cells is needed for decreases in glucose levels to elicit full glucagon responses from mouse and human islets. We performed functional studies using living pancreas slices from donors with type 1 diabetes and found that alpha cells had normal glucagon content and responded typically to KCl depolarization, but failed to respond to decreases in glucose concentration and had severely impaired AMPA/kainate receptor signaling. Reactivating residual AMPA/kainate receptor function with the positive allosteric modulators cyclothiazide and aniracetam partially rescued glucagon secretion in response to hypoglycemia. Positive allosteric modulators of AMPA/kainate receptors already approved to treat other conditions could thus be repurposed to prevent hypoglycemia and improve management of diabetes.

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 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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