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Pharmacological Modification of a Cerebroplegia Solution
Published in Richard A. Jonas, Jane W. Newburger, Joseph J. Volpe, John W. Kirklin, Brain Injury and Pediatric Cardiac Surgery, 2019
Richard A. Jonas, Aoki Mitsuru
NBQX is a non-NMDA, or AMPA (a-amino-3-hydroxy-5-methyl-4-isoxazole) receptor antagonist. AMPA receptor activation results in depolarization of the cell membrane and an increase in sodium and potassium flux, and it can produce excitotoxic neuronal injury in the immature brain. In studies using mature rodents, NBQX has been demonstrated to reduce ischemic neuronal injury.10 However these studies were performed at normothermia and did not include the added insults of cardiopulmonary bypass, anticoagulation, and hemodilution.
Glutathione and Glutathione Derivatives: Possible Modulators of Ionotropic Glutamate Receptors
Published in Christopher A. Shaw, Glutathione in the Nervous System, 2018
Réka Janáky, Vince Varga, Zsolt Jenei, Pirjo Saransaari, Simo S. Oja
The slight enhancing effect (20 ± 4 percent, mean ± SD, n = 12) of NMDA observed in 0.1 mM Mg2+ medium in the presence of 50 μM glycine is not discernible in standard Krebs–Ringer–Hepes solution (Table 4). This block is relieved in the presence of GSH, but not GSSG (Janáky et al., unpublished results). The release evoked by 1 mM kainate is enhanced by GSSG (Table 5), but only during the late stimulation phase by GSH. It is inhibited by CNQX and DNQX, NBQX being without effect (Janáky et al. 1997). The release evoked by 0.5 mM AMPA is enhanced by GSSG, GSH being ineffective (Table 5). t-ACPD fails to influence the release of dopamine in all conditions (Janáky et al. 1997).
Neurotransmitters and pharmacology
Published in Mark J. Ashley, David A. Hovda, Traumatic Brain Injury, 2017
Ronald A. Browning, Richard W. Clough
AMPA receptors can be blocked selectively by the quinoxaline diones, such as 6-nitro-7-sulphamobenzo-quinoxaline 2, 3-dione (NBQX), which are only used in studies involving experimental animals. However, currently there is one AMPA receptor antagonist (i.e., perampanel) available for the treatment of epilepsy.155Perampanel is an allosteric inhibitor of the glutamate-gated sodium channel and is thus a noncompetitive antagonist of the AMPA receptor. There are no selective antagonists at the kainate receptor except, perhaps, the experimental drug LY294486.
NBQX attenuates relapse of nicotine seeking but not nicotine and methamphetamine self-administration in rats
Published in The World Journal of Biological Psychiatry, 2021
Jana Ruda-Kucerova, Petra Amchova, Filip Siska, Yousef Tizabi
Notably, there is a large spectrum of AMPA/kainate allosteric modulators or antagonists where their selectivity and pharmacodynamic profiles differ substantially from each other (Lees 2000; Gass and Olive 2008). Even the class of quinoxalinediones ligands has a variable mechanism of action. Thus, DNQX and CNQX also possess weak partial agonists at both AMPA and kainate receptors and may antagonise the NMDA receptor’s glycine site (Kessler et al. 1989). NBQX, on the other hand, seems to be most selective for AMPA receptors, with 30- to 60-fold greater selectivity over kainate receptors (Lees 2000). There is a study showing that CNQX but not NBQX can suppress amphetamine-induced conditioned place preference, which may be explained by the NMDA antagonistic effect of CNQX (Mead and Stephens 1999). Hence, the presumed selectivity of the ligands has to be carefully verified. For example, it may be that the NMDA antagonism is truly responsible for numerous anti-addiction effects of the compounds (Jones et al. 2018). Nonetheless, a role of kainate antagonism against alcohol drinking was also recently suggested (Van Nest et al. 2017). Similarly, the investigation of selective AMPA receptor modulators in drug addiction is worth exploring as a recent study has demonstrated potential antidepressant effects of such ligands in an animal model (Gordillo-Salas et al. 2020).
Effects of low-dose alcohol exposure in adolescence on subsequent alcohol drinking in adulthood in a rat model of depression
Published in The World Journal of Biological Psychiatry, 2021
Filip Siska, Petra Amchova, Daniela Kuruczova, Yousef Tizabi, Jana Ruda-Kucerova
The overall effect of NBQX was assessed using a simple paired samples t-test (Yandell 1997). Difference between the NBQX effect in the OBX/SHAM and EE/EN conditions was tested using two-way ANOVA with interaction.