Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

ChemMedChem ◽  
2016 ◽  
Vol 12 (3) ◽  
pp. 197-201 ◽  
Author(s):  
David Orain ◽  
Engin Tasdelen ◽  
Samuel Haessig ◽  
Manuel Koller ◽  
Anne Picard ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Design And Synthesis ◽  
Ampa Receptor Antagonist ◽  
Orally Active

scholarly journals Cover Picture: Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist (ChemMedChem 3/2017)

ChemMedChem ◽  
2017 ◽  
Vol 12 (3) ◽  
pp. 196-196
Author(s):  
David Orain ◽  
Engin Tasdelen ◽  
Samuel Haessig ◽  
Manuel Koller ◽  
Anne Picard ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Design And Synthesis ◽  
Ampa Receptor Antagonist ◽  
Orally Active

scholarly journals Perampanel: A novel, orally active, noncompetitive AMPA-receptor antagonist that reduces seizure activity in rodent models of epilepsy

Epilepsia ◽  
2011 ◽  
Vol 52 (7) ◽  
pp. 1331-1340 ◽  
Author(s):  
Takahisa Hanada ◽  
Yutaka Hashizume ◽  
Naoki Tokuhara ◽  
Osamu Takenaka ◽  
Naohiro Kohmura ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Seizure Activity ◽  
Rodent Models ◽  
Ampa Receptor Antagonist ◽  
Orally Active ◽  
Models Of Epilepsy

Design and synthesis of labeled analogs of PhTX-56, a potent and selective AMPA receptor antagonist

2005 ◽  
Vol 13 (17) ◽  
pp. 5104-5112 ◽  
Author(s):  
Trine F. Andersen ◽  
Stine B. Vogensen ◽  
Lars S. Jensen ◽  
Kolja M. Knapp ◽  
Kristian Strømgaard
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Design And Synthesis ◽  
Ampa Receptor Antagonist

AMPA Receptor Antagonist CFM-2 Decreases Survivin Expression in Cancer Cells

2018 ◽  
Vol 18 (4) ◽  
pp. 591-596 ◽  
Author(s):  
Domingo Sanchez Ruiz ◽  
Hella Luksch ◽  
Marco Sifringer ◽  
Achim Temme ◽  
Christian Staufner ◽  
...  
Keyword(s):  
Cell Survival ◽  
Receptor Antagonist ◽  
Cancer Cells ◽  
Glutamate Receptors ◽  
Cancer Cell ◽  
Ampa Receptor ◽  
Ampa Receptors ◽  
Survivin Expression ◽  
Ampa Receptor Antagonist ◽  
Cancer Cell Survival

Background: Glutamate receptors are widely expressed in different types of cancer cells. α-Amino-3- hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptors are ionotropic glutamate receptors which are coupled to intracellular signaling pathways that influence cancer cell survival, proliferation, and migration. Blockade of AMPA receptors by pharmacologic compounds may potentially constitute an effective tool in anticancer treatment strategies. Method: Here we investigated the impact of the AMPA receptor antagonist CFM-2 on the expression of the protein survivin, which is known to promote cancer cell survival and proliferation. We show that CFM-2 inhibits survivin expression at mRNA and protein levels and decreases the viability of cancer cells. Using a stably transfected cell line which overexpresses survivin, we demonstrate that over-expression of survivin enhances cancer cell viability and attenuates CFM-2–mediated inhibition of cancer cell growth. Result: These findings point towards suppression of survivin expression as a new mechanism contributing to anticancer effects of AMPA antagonists.

Structural Determinants of the γ-8 TARP Dependent AMPA Receptor Antagonist

2017 ◽  
Vol 8 (12) ◽  
pp. 2631-2647 ◽  
Author(s):  
Matthew R. Lee ◽  
Kevin M. Gardinier ◽  
Douglas L. Gernert ◽  
Douglas A. Schober ◽  
Rebecca A. Wright ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Structural Determinants ◽  
Ampa Receptor Antagonist

ChemInform Abstract: Two Intermediates in the Synthesis of Decahydroisoquinolines with NMDA and AMPA Receptor Antagonist Activity.

ChemInform ◽  
2010 ◽  
Vol 33 (1) ◽  
pp. no-no
Author(s):  
J. Zukerman-Schpector ◽  
Mauricio Vega ◽  
I. Caracelli ◽  
Luiz C. Dias ◽  
Anna M. A. P. Fernandes
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Antagonist Activity ◽  
Ampa Receptor Antagonist

Neuroprotective effect of the novel glutamate AMPA receptor antagonist YM872 assessed with in vivo MR imaging of rat MCA occlusion

1998 ◽  
Vol 811 (1-2) ◽  
pp. 63-70 ◽  
Author(s):  
Asta Håberg ◽  
Masayasu Takahashi ◽  
Tokio Yamaguchi ◽  
Mari Hjelstuen ◽  
Olav Haraldseth
Keyword(s):  
Mr Imaging ◽  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Neuroprotective Effect ◽  
The Novel ◽  
Ampa Receptor Antagonist ◽  
Mca Occlusion
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