Therapeutic window of opportunity for the neuroprotective effect of valproate versus the competitive AMPA receptor antagonist NS1209 following status epilepticus in rats

2011 ◽  
Vol 61 (5-6) ◽  
pp. 1033-1047 ◽  
Author(s):  
Melanie Langer ◽  
Claudia Brandt ◽  
Christina Zellinger ◽  
Wolfgang Löscher
Keyword(s):  
Status Epilepticus ◽  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Neuroprotective Effect ◽  
Therapeutic Window ◽  
Window Of Opportunity ◽  
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

scholarly journals Neuroprotective Effect of the AMPA Receptor Antagonist LY-293558 in Focal Cerebral Ischemia in the Cat

1994 ◽  
Vol 14 (3) ◽  
pp. 466-471 ◽  
Author(s):  
R. Bullock ◽  
D. I. Graham ◽  
S. Swanson ◽  
J. McCulloch
Keyword(s):  
Cerebral Ischemia ◽  
Middle Cerebral Artery ◽  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Cerebral Artery ◽  
Focal Cerebral Ischemia ◽  
Neuroprotective Effect ◽  
Ischemic Damage ◽  
Physiological Variables ◽  
Ampa Receptor Antagonist

The effects of the glutamate α-amino-3-hydroxy 5-methyl-4-isoxazole propionate (AMPA) receptor antagonist LY-293558 in reducing ischemic brain damage have been assessed in halothane-anesthetized cats. Focal cerebral ischemia was produced by permanent occlusion of one middle cerebral artery, and the animals were killed 6 h later. The amount of early irreversible ischemic damage was assessed at 16 predetermined stereotactic planes by an observer blinded to treatment paradigm employed. Treatment with LY-293558 (15 mg/kg i.v., plus infusion of 7 mg/kg/h) initiated 30 min prior to middle cerebral artery occlusion reduced significantly (p < 0.02) the volume of ischemic damage (from 3,423 ± 212 mm3 of the cerebral hemisphere in vehicle-treated cats to 2,822 ± 569 mm3 in LY-293558-treated cats). The present data demonstrate that an AMPA receptor antagonist can reduce focal ischemic damage in a gyrencephalic species in which key physiological variables have been controlled and monitored throughout the postischemic period. These data provide additional support for the clinical evaluation of AMPA receptor antagonists in focal cerebral ischemia in humans.

scholarly journals The Neuroprotective Effect of the Novel AMPA Receptor Antagonist PD152247 (PNQX) in Temporary Focal Ischemia in the Rat

Stroke ◽  
1999 ◽  
Vol 30 (7) ◽  
pp. 1472-1477 ◽  
Author(s):  
Gerald P. Schielke ◽  
Nancy C. Kupina ◽  
Peter A. Boxer ◽  
Christopher F. Bigge ◽  
Devin F. Welty
Keyword(s):  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Neuroprotective Effect ◽  
Focal Ischemia ◽  
The Novel ◽  
Ampa Receptor Antagonist

scholarly journals Treatment of early and late kainic acid-induced status epilepticus with the noncompetitive AMPA receptor antagonist GYKI 52466

Epilepsia ◽  
2010 ◽  
Vol 51 (1) ◽  
pp. 108-117 ◽  
Author(s):  
Brita Fritsch ◽  
Jeffrey J. Stott ◽  
Joy Joelle Donofrio ◽  
Michael A. Rogawski
Keyword(s):  
Status Epilepticus ◽  
Receptor Antagonist ◽  
Kainic Acid ◽  
Ampa Receptor ◽  
Gyki 52466 ◽  
Ampa Receptor Antagonist

scholarly journals Effects of the AMPA-Receptor Antagonist, NBQX, on Neuron Loss in Dentate Hilus of the Hippocampal Formation after 8, 10, or 12 Min of Cerebral Ischemia in the Rat

1997 ◽  
Vol 17 (2) ◽  
pp. 147-152 ◽  
Author(s):  
Ping Hu ◽  
Nils Henrik Diemer ◽  
Torben Bruhn ◽  
Flemming Fryd Johansen
Keyword(s):  
Cerebral Ischemia ◽  
Receptor Antagonist ◽  
Ampa Receptor ◽  
Hippocampal Formation ◽  
Neuroprotective Effect ◽  
Pyramidal Cells ◽  
Ca1 Pyramidal Cells ◽  
Ampa Receptor Antagonist ◽  
Hippocampal Ca1 ◽  
Dentate Hilus

The α-amino-3-hydroxy-5-methyl-4-isoxazole (AMPA) receptor antagonist, 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo( F)quinoxaline (NBQX), offers protection to hippocampal CA1 pyramidal cells after short episodes of transient cerebral ischemia. Besides CA1 pyramidal cells, neurons containing somatostatin (SS) and located in the dentate hilus of the hippocampal formation are lost after cerebral ischemia. We studied the protective effects of NBQX on SS neurons in the hilus and on hippocampal CA1 pyramidal cells following 8, 10, or 12 min of four-vessel occlusion ischemia during systemic hypotension. NBQX was administered 3 × 30 mg/kg at 0, 10, and 25 after induction of ischemia or sham, and all rats survived for 7 days. NBQX given to control rats without ischemia had no influence on number or morphology of hilar SS neurons and CA1 pyramidal cells. After 8 min of ischemia, NBQX prevented loss of hilar SS neurons. After 10 and 12 min of ischemia, NBQX had no significant effects on loss of SS neurons in the dentate hilus. However, in all ischemic groups, NBQX significantly reduced loss of CA1 pyramidal cells as compared to control rats. This neuroprotective effect decreased gradually and significantly as the time of ischemia increased. Our results support the observation that SS neurons in hilus are among the most ischemia-vulnerable neurons in the brain. We found that administration of NBQX in generally accepted dosages can protect the rapidly dying SS neurons in hilus from only brief episodes of ischemia.

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.

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