Discovery and Characterization of a Novel Dihydroisoxazole Class of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) Receptor Potentiators

2013 ◽  
Vol 56 (22) ◽  
pp. 9180-9191 ◽  
Author(s):  
Nandini C. Patel ◽  
Jacob Schwarz ◽  
Xinjun J. Hou ◽  
Dennis J. Hoover ◽  
Longfei Xie ◽  
...  
Keyword(s):  
Ampa Receptor ◽  
Ampa Receptor Potentiators

AMPA Receptor Potentiators for the Treatment of CNS Disorders

2004 ◽  
Vol 3 (3) ◽  
pp. 181-194 ◽  
Author(s):  
Michael O'Neill ◽  
David Bleakman ◽  
Dennis Zimmerman ◽  
Eric Nisenbaum
Keyword(s):  
Ampa Receptor ◽  
Cns Disorders ◽  
Ampa Receptor Potentiators

Ring-Fused Thiadiazines as Core Structures for the Development of Potent AMPA Receptor Potentiators

2010 ◽  
Vol 17 (30) ◽  
pp. 3575-3582 ◽  
Author(s):  
B. Pirotte ◽  
P. Francotte ◽  
E. Goffin ◽  
P. Fraikin ◽  
L. Danober ◽  
...  
Keyword(s):  
Ampa Receptor ◽  
Ampa Receptor Potentiators

scholarly journals Reply to "A Comment on 'Discovery and Characterization of AMPA Receptor Modulators Selective for TARP- 8"

2016 ◽  
Vol 358 (3) ◽  
pp. 527-527
Author(s):  
M. P. Maher ◽  
M. K. Ameriks ◽  
B. M. Savall ◽  
N. I. Carruthers ◽  
T. W. Lovenberg
Keyword(s):  
Ampa Receptor ◽  
Receptor Modulators

scholarly journals Identification and characterization of RNA aptamers: A long aptamer blocks the AMPA receptor and a short aptamer blocks both AMPA and kainate receptors

2017 ◽  
Vol 292 (18) ◽  
pp. 7338-7347 ◽  
Author(s):  
William J. Jaremko ◽  
Zhen Huang ◽  
Wei Wen ◽  
Andrew Wu ◽  
Nicholas Karl ◽  
...  
Keyword(s):  
Ampa Receptor ◽  
Neurological Diseases ◽  
Rna Aptamers ◽  
Kainate Receptors ◽  
Single Receptor ◽  
Cell Recording ◽  
Exponential Enrichment ◽  
High Degree

AMPA and kainate receptors, along with NMDA receptors, represent different subtypes of glutamate ion channels. AMPA and kainate receptors share a high degree of sequence and structural similarities, and excessive activity of these receptors has been implicated in neurological diseases such as epilepsy. Therefore, blocking detrimental activity of both receptor types could be therapeutically beneficial. Here, we report the use of an in vitro evolution approach involving systematic evolution of ligands by exponential enrichment with a single AMPA receptor target (i.e. GluA1/2R) to isolate RNA aptamers that can potentially inhibit both AMPA and kainate receptors. A full-length or 101-nucleotide (nt) aptamer selectively inhibited GluA1/2R with a KI of ∼5 μm, along with GluA1 and GluA2 AMPA receptor subunits. Of note, its shorter version (55 nt) inhibited both AMPA and kainate receptors. In particular, this shorter aptamer blocked equally potently the activity of both the GluK1 and GluK2 kainate receptors. Using homologous binding and whole-cell recording assays, we found that an RNA aptamer most likely binds to the receptor's regulatory site and inhibits it noncompetitively. Our results suggest the potential of using a single receptor target to develop RNA aptamers with dual activity for effectively blocking both AMPA and kainate receptors.

Synthesis and pharmacological characterization of l-trans-4-tetrazolylproline (ly300020): A novel systemically-active ampa receptor agonist

1993 ◽  
Vol 3 (1) ◽  
pp. 95-98 ◽  
Author(s):  
James A. Monn ◽  
Matthew J. Valli ◽  
Rebecca A. True ◽  
Darryl D. Schoepp ◽  
J.David Leander ◽  
...  
Keyword(s):  
Ampa Receptor ◽  
Receptor Agonist ◽  
Pharmacological Characterization

Mapping the functional effects of the AMPA receptor potentiators LY450108 and LY451395 with 14C 2-deoxyglucose autoradiography

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S410-S410
Author(s):  
Jill H Fowler ◽  
Michael J O'Neill ◽  
David Bleakman ◽  
James McCulloch
Keyword(s):  
Ampa Receptor ◽  
Ampa Receptor Potentiators
Sign in / Sign up

Export Citation Format

Share Document