3 dione 6 cyano 7 nitroquinoxaline 2


Summary: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.

Top Publications

  1. Famous K, Kumaresan V, Sadri Vakili G, Schmidt H, Mierke D, Cha J, et al. Phosphorylation-dependent trafficking of GluR2-containing AMPA receptors in the nucleus accumbens plays a critical role in the reinstatement of cocaine seeking. J Neurosci. 2008;28:11061-70 pubmed publisher
    ..The present results also demonstrate that the reinstatement of cocaine seeking is associated with increases in the phosphorylation-dependent trafficking of GluR2-containing AMPA receptors in the nucleus accumbens. ..
  2. Kimura N. Fictive lung ventilation in the isolated brainstem preparation of the aquatic frog, Xenopus laevis. Adv Exp Med Biol. 2010;669:9-12 pubmed publisher
    ..These results suggest that Xenopus is capable of oscillating buccal rhythm within the brainstem. ..
  3. Bozzo L, Chatton J. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 2010;1316:27-34 pubmed publisher
    ..Thus, TFB-TBOA, with its high potency and its apparent lack of neuronal effects, appears to be one of the most useful pharmacological tools available so far for studying glial glutamate transporters. ..
  4. Okamoto R, Enomoto A, Koizumi H, Tanaka S, Ishihama K, Kogo M. Long-term potentiation of intrinsic excitability in trigeminal motoneurons. Brain Res. 2010;1312:32-40 pubmed publisher
    ..These findings indicate that TMNs exhibit LTP of intrinsic excitability. ..
  5. Chen Y, Balasubramanyan S, Lai A, Todd K, Smith P. Effects of sciatic nerve axotomy on excitatory synaptic transmission in rat substantia gelatinosa. J Neurophysiol. 2009;102:3203-15 pubmed publisher
    ..This would explain how synaptic excitation of tonic cells decreases despite the fact that axotomy increases spontaneous activity in primary afferent neurons. ..
  6. Li Y, Krupa B, Kang J, Bolshakov V, Liu G. Glycine site of NMDA receptor serves as a spatiotemporal detector of synaptic activity patterns. J Neurophysiol. 2009;102:578-89 pubmed publisher
    ..These results suggest that the NMDA receptor glycine site may serve as a detector of the spatiotemporal characteristics of presynaptic activity patterns. ..
  7. Suto N, Ecke L, Wise R. Control of within-binge cocaine-seeking by dopamine and glutamate in the core of nucleus accumbens. Psychopharmacology (Berl). 2009;205:431-9 pubmed publisher
  8. Kealy J, Commins S. Antagonism of glutamate receptors in the CA1 to perirhinal cortex projection prevents long-term potentiation and attenuates levels of brain-derived neurotrophic factor. Brain Res. 2009;1265:53-64 pubmed publisher
    ..This molecular and electrophysiological data suggests that LTP in the CA1-perirhinal cortex projection may require activation of postsynaptic AMPA/kainate receptors in order to sustain LTP. ..
  9. Megalou E, Brandon C, Frost W. Evidence that the swim afferent neurons of tritonia diomedea are glutamatergic. Biol Bull. 2009;216:103-12 pubmed
    ..These findings support glutamate as a transmitter used by the S-cells, and will facilitate studies using this model system to explore a variety of issues related to the neural basis of behavior. ..

More Information


  1. Pancani T, Phelps J, Searcy J, Kilgore M, Chen K, Porter N, et al. Distinct modulation of voltage-gated and ligand-gated Ca2+ currents by PPAR-gamma agonists in cultured hippocampal neurons. J Neurochem. 2009;109:1800-11 pubmed publisher
  2. Roberto M, Cruz M, Gilpin N, Sabino V, Schweitzer P, Bajo M, et al. Corticotropin releasing factor-induced amygdala gamma-aminobutyric Acid release plays a key role in alcohol dependence. Biol Psychiatry. 2010;67:831-9 pubmed publisher
    ..These combined findings suggest a key role for specific presynaptic CRF-GABA interactions in CeA in the development and maintenance of ethanol dependence. ..
  3. Packer O, Verweij J, Li P, Schnapf J, Dacey D. Blue-yellow opponency in primate S cone photoreceptors. J Neurosci. 2010;30:568-72 pubmed publisher
    ..The outward current evoked by yellow light is caused by feedback from horizontal cells that are driven by surrounding L and M cones. Stimulation of the surround modulates calcium conductance in the center S cone. ..
  4. Kasai N, Ramanujan C, Fujimoto I, Shimada A, Ryan J, Torimitsu K. AFM observation of single, functioning ionotropic glutamate receptors reconstituted in lipid bilayers. Biochim Biophys Acta. 2010;1800:655-61 pubmed publisher
    ..This knowledge may be useful for neuroscience as well as in pharmaceutical applications. ..
  5. Li D, Chen S, Pan H. Adenosine inhibits paraventricular pre-sympathetic neurons through ATP-dependent potassium channels. J Neurochem. 2010;113:530-42 pubmed publisher
    ..Collectively, our findings suggest that adenosine inhibits the excitability of PVN pre-sympathetic neurons through A(1) receptor-mediated opening of K(ATP) channels. ..
  6. Hickmott P. Synapses of horizontal connections in adult rat somatosensory cortex have different properties depending on the source of their axons. Cereb Cortex. 2010;20:591-601 pubmed publisher
    ..These data suggest that individual excitatory synapses from connections that cross a border (CB) have smaller amplitudes than those that come from within a representation (NCB), and suggest a postsynaptic locus for the difference. ..
  7. Hinckley C, Wiesner E, Mentis G, Titus D, Ziskind Conhaim L. Sensory modulation of locomotor-like membrane oscillations in Hb9-expressing interneurons. J Neurophysiol. 2010;103:3407-23 pubmed publisher
  8. Cammalleri M, Martini D, Timperio A, Bagnoli P. Functional effects of somatostatin receptor 1 activation on synaptic transmission in the mouse hippocampus. J Neurochem. 2009;111:1466-77 pubmed publisher
    ..We conclude that SRIF control of excitatory transmission through an action at sst(1) may represent an important contribution to the regulation of hippocampal activity. ..
  9. Sheroziya M, Von Bohlen Und Halbach O, Unsicker K, Egorov A. Spontaneous bursting activity in the developing entorhinal cortex. J Neurosci. 2009;29:12131-44 pubmed publisher
    ..We conclude that prolonged intrinsic bursting activity is a characteristic feature of developing medial EC layer III neurons that might be involved in neuronal and network maturation. ..
  10. Ziskind Conhaim L, Mentis G, Wiesner E, Titus D. Synaptic integration of rhythmogenic neurons in the locomotor circuitry: the case of Hb9 interneurons. Ann N Y Acad Sci. 2010;1198:72-84 pubmed publisher
    ..Our findings suggest that the rhythmogenic Hb9 INs are integral components of the sensorimotor circuitry that regulate locomotor-like activity in the spinal cord. ..
  11. Zhao X, Liu M, Yuan D, Wang Y, He Y, Wang D, et al. Nociception-induced spatial and temporal plasticity of synaptic connection and function in the hippocampal formation of rats: a multi-electrode array recording. Mol Pain. 2009;5:55 pubmed publisher
    ..In addition, the multi-synaptic model established in the present investigation may open a new avenue for future studies of pain-related brain dysfunctions at the higher level of the neuromatrix. ..
  12. Sánchez Mejorada E, Sánchez Mondragon G, Pineda J, Gonzalez M, Barral J. N-type calcium channels mediate a GABA(B) presynaptic modulation in the corticostriatal synapse in turtle's paleostriatum augmentatum. Synapse. 2009;63:855-62 pubmed publisher
    ..These data suggest that N and P/Q channels participate in the neurotransmitter release, whereas only N-type Ca2+ channels are involved in the presynaptic modulation of GABA(B) in the corticostriatal synapse of the turtle. ..
  13. Bodnar I, Bánky Z, Zelena D, Halász B. Glutamate receptor antagonist infused into the hypothalamic suprachiasmatic nuclei interferes with the diurnal fluctuations in plasma prolactin and corticosterone levels and injected into the mesencephalic dorsal raphe nucleus attenuates the suckling. Brain Res Bull. 2009;80:9-16 pubmed publisher
  14. Khakpay R, Semnanian S, Javan M, Janahmadi M. The effect of intra-locus coeruleus injection of 17beta-estradiol on inflammatory pain modulation in male rat. Behav Brain Res. 2010;214:409-16 pubmed publisher
    ..05). It may be concluded that the analgesic effect of 17beta-estradiol in formalin-induced inflammatory pain is mediated through interaction with membrane-bound receptors, probably the NMDA receptors. ..
  15. Xing J, Li D, Li J. Role of GABA receptors in nitric oxide inhibition of dorsolateral periaqueductal gray neurons. Neuropharmacology. 2008;54:734-44 pubmed publisher
    ..Overall, NO suppresses neuronal activity of the dl-PAG via a potentiation of GABAergic synaptic inputs and via GABA(A) receptors. ..
  16. Kim S, Ryan T. CDK5 serves as a major control point in neurotransmitter release. Neuron. 2010;67:797-809 pubmed publisher
    ..These studies thus pinpoint CDK5 as a major control point for modulation of neurotransmitter release in mammalian neurons. ..
  17. Apland J, Aroniadou Anderjaska V, Braga M. Soman induces ictogenesis in the amygdala and interictal activity in the hippocampus that are blocked by a GluR5 kainate receptor antagonist in vitro. Neuroscience. 2009;159:380-9 pubmed publisher
  18. Nakamura M, Choi K, Choi S, Do C, Jun J, Kwon H, et al. Presynaptic kainate receptors increase GABAergic neurotransmission in rat periaqueductal gray neurons. Eur J Pharmacol. 2010;635:72-8 pubmed publisher
    ..Presynaptic kainate receptors on GABAergic nerve terminals appear to modulate GABAergic transmission, and in doing so may play an important role in the regulation of PAG neuron excitability. ..
  19. Marosi M, Nagy D, Farkas T, Kis Z, Rozsa E, Robotka H, et al. A novel kynurenic acid analogue: a comparison with kynurenic acid. An in vitro electrophysiological study. J Neural Transm (Vienna). 2010;117:183-8 pubmed publisher
    ..The new analogue may therefore be considered a promising candidate for clinical studies. ..
  20. Jung S, Kim J, Kwon O, Jung J, An K, Jeong A, et al. Input-specific synaptic plasticity in the amygdala is regulated by neuroligin-1 via postsynaptic NMDA receptors. Proc Natl Acad Sci U S A. 2010;107:4710-5 pubmed publisher
    ..These findings suggest that neuroligin-1 can modulate, in a pathway-specific manner, synaptic plasticity in the amygdala circuits of adult animals, likely by regulating the abundance of postsynaptic NMDA receptors. ..
  21. Gruber A, Powell E, O DONNELL P. Cortically activated interneurons shape spatial aspects of cortico-accumbens processing. J Neurophysiol. 2009;101:1876-82 pubmed publisher
    ..The data indicate a high order of information processing within striatal circuits that should be considered in models of basal ganglia function and disease. ..
  22. Jin Y, Cahill E, Fernandes L, Wang X, Chen W, Smith S, et al. Optical tracking of phenotypically diverse individual synapses on solitary tract nucleus neurons. Brain Res. 2010;1312:54-66 pubmed publisher
  23. Panuccio G, Curia G, Colosimo A, Cruccu G, Avoli M. Epileptiform synchronization in the cingulate cortex. Epilepsia. 2009;50:521-36 pubmed publisher
    ..In addition, mu-opioid receptors appear to modulate both excitatory and inhibitory mechanisms, thus influencing epileptiform synchronization in the ACC. ..
  24. Kukley M, Nishiyama A, Dietrich D. The fate of synaptic input to NG2 glial cells: neurons specifically downregulate transmitter release onto differentiating oligodendroglial cells. J Neurosci. 2010;30:8320-31 pubmed publisher
  25. Guzmán Lenis M, Navarro X, Casas C. Drug screening of neuroprotective agents on an organotypic-based model of spinal cord excitotoxic damage. Restor Neurol Neurosci. 2009;27:335-49 pubmed publisher
    ..The in vitro model used may serve to initiate comparative analyses of new compounds to narrow the choice for future neuroprotective agents to be tested in vivo. ..
  26. Fu L, van den Pol A. Kisspeptin directly excites anorexigenic proopiomelanocortin neurons but inhibits orexigenic neuropeptide Y cells by an indirect synaptic mechanism. J Neurosci. 2010;30:10205-19 pubmed publisher
    ..POMC cells may hypothetically serve as a conditional relay station downstream of kisspeptin and GnIH to signal the availability of energy resources relevant to reproduction...
  27. Fuenzalida M, Fernandez de Sevilla D, Couve A, Buño W. Role of AMPA and NMDA receptors and back-propagating action potentials in spike timing-dependent plasticity. J Neurophysiol. 2010;103:47-54 pubmed publisher
    ..However, a transient depolarization of another origin that unblocks NMDA receptors and a BAP may also trigger LTP. ..
  28. Yoshimura H, Sugai T, Honjo M, Kaneyama K, Segami N, Kato N. Application of caffeine reveals input frequency-dependent determination of signal-traveling routes between primary and secondary visual cortices in rats. Neurosci Res. 2010;66:30-6 pubmed publisher
  29. Roux J, Wanaverbecq N, Jean A, Lebrun B, Trouslard J. Depolarization-induced release of endocannabinoids by murine dorsal motor nucleus of the vagus nerve neurons differentially regulates inhibitory and excitatory neurotransmission. Neuropharmacology. 2009;56:1106-15 pubmed publisher
    ..These results show for the first time that DMNV neurons release EC in an activity-dependent manner, which in turn differentially regulates their inhibitory and excitatory synaptic inputs. ..
  30. Ni X, Martin Caraballo M. Differential effect of glutamate receptor blockade on dendritic outgrowth in chicken lumbar motoneurons. Neuropharmacology. 2010;58:593-604 pubmed publisher
  31. Lee K, Porteous R, Campbell R, Luscher B, Herbison A. Knockdown of GABA(A) receptor signaling in GnRH neurons has minimal effects upon fertility. Endocrinology. 2010;151:4428-36 pubmed publisher
  32. Mostofi A, Holtzman T, Grout A, Yeo C, Edgley S. Electrophysiological localization of eyeblink-related microzones in rabbit cerebellar cortex. J Neurosci. 2010;30:8920-34 pubmed publisher
    ..These small eyeblink-related areas provide cerebellar cortical targets for analysis of eyeblink conditioning at a neuronal level but need to be localized with electrophysiological identification in individual animals. ..
  33. Lundius E, Sanchez Alavez M, Ghochani Y, Klaus J, Tabarean I. Histamine influences body temperature by acting at H1 and H3 receptors on distinct populations of preoptic neurons. J Neurosci. 2010;30:4369-81 pubmed publisher
    ..Our data indicate that histamine modulates the core body temperature by acting at two distinct populations of preoptic neurons that express H1 and H3 receptor subtypes, respectively. ..
  34. Gorini C, Jameson H, Mendelowitz D. Serotonergic modulation of the trigeminocardiac reflex neurotransmission to cardiac vagal neurons in the nucleus ambiguus. J Neurophysiol. 2009;102:1443-50 pubmed publisher
  35. Acuna Goycolea C, Obrietan K, van den Pol A. Cannabinoids excite circadian clock neurons. J Neurosci. 2010;30:10061-6 pubmed publisher
    ..These data raise the possibility that the time dissociation described by cannabinoid users may result in part from altered circadian clock function and/or entrainment to environmental time cues. ..
  36. Khaliq Z, Bean B. Pacemaking in dopaminergic ventral tegmental area neurons: depolarizing drive from background and voltage-dependent sodium conductances. J Neurosci. 2010;30:7401-13 pubmed publisher
    ..In addition, we found that non-voltage-dependent background sodium current is much smaller in SNc neurons than VTA neurons. ..
  37. Dhawale A, Hagiwara A, Bhalla U, Murthy V, Albeanu D. Non-redundant odor coding by sister mitral cells revealed by light addressable glomeruli in the mouse. Nat Neurosci. 2010;13:1404-12 pubmed publisher
  38. Chen X, Shu S, Schwartz L, Sun C, Kapur J, Bayliss D. Homeostatic regulation of synaptic excitability: tonic GABA(A) receptor currents replace I(h) in cortical pyramidal neurons of HCN1 knock-out mice. J Neurosci. 2010;30:2611-22 pubmed publisher
  39. Lam F, Ng E. Substance P and glutamate receptor antagonists improve the anti-arthritic actions of dexamethasone in rats. Br J Pharmacol. 2010;159:958-69 pubmed publisher
    ..The efficacy of dexamethasone in reducing arthritic pain and joint swelling can be improved by co-administration of substance P and glutamate receptor antagonists. ..
  40. Magloire V, Streit J. Intrinsic activity and positive feedback in motor circuits in organotypic spinal cord slice cultures. Eur J Neurosci. 2009;30:1487-97 pubmed publisher
    ..Together, these findings suggest that intrinsic firing of motoneurons may contribute to the activation of population bursts through cholinergic positive feedback loops in cultured spinal networks...
  41. Lin H, Mao S, Su C, Gean P. Alterations of excitatory transmission in the lateral amygdala during expression and extinction of fear memory. Int J Neuropsychopharmacol. 2010;13:335-45 pubmed publisher
    ..DCS does not affect inhibitory transmission but reverses the conditioning-induced post-synaptic memory trace when administered before extinction training. ..
  42. Liu L, Zhang R, Liu K, Zhou H, Tang Y, Su J, et al. Tissue kallikrein alleviates glutamate-induced neurotoxicity by activating ERK1. J Neurosci Res. 2009;87:3576-90 pubmed publisher
    ..Thus, TK represents a promising therapeutic strategy for ischemic stroke. ..
  43. Mutolo D, Bongianni F, Cinelli E, Pantaleo T. Role of excitatory amino acids in the mediation of tracheobronchial cough induced by citric acid inhalation in the rabbit. Brain Res Bull. 2009;80:22-9 pubmed publisher
    ..Present data also corroborate the notion that the cVRG is involved in the generation of the whole cough motor pattern, but seems to represent merely an expiratory output system for sneezing. ..
  44. Llano D, Theyel B, Mallik A, Sherman S, Issa N. Rapid and sensitive mapping of long-range connections in vitro using flavoprotein autofluorescence imaging combined with laser photostimulation. J Neurophysiol. 2009;101:3325-40 pubmed publisher
    ..These data suggest that FA is a sensitive tool for exploring and measuring connectivity and, when coupled with glutamate photostimulation, can rapidly map long-range projections in a single animal. ..
  45. Huang F, Abbas A, Li R, Afanasenkau D, Wigström H. Bidirectional synaptic plasticity in response to single or paired pulse activation of NMDA receptors. Neurosci Res. 2010;67:108-16 pubmed publisher
    ..In addition to NMDA-R driven processes, passive relaxation contributes to the synaptic plasticity and in some cases outbalances the active control. ..
  46. Aracri P, Consonni S, Morini R, Perrella M, Rodighiero S, Amadeo A, et al. Tonic modulation of GABA release by nicotinic acetylcholine receptors in layer V of the murine prefrontal cortex. Cereb Cortex. 2010;20:1539-55 pubmed publisher
    ..We conclude that heteromeric nAChRs control GABA release presynaptically, whereas mixed nAChRs regulate both excitation and inhibition of interneurons, the balance depending on the overall glutamatergic drive. ..
  47. Nosyreva E, Kavalali E. Activity-dependent augmentation of spontaneous neurotransmission during endoplasmic reticulum stress. J Neurosci. 2010;30:7358-68 pubmed publisher
  48. Desfeux A, El Ghazi F, Jegou S, Legros H, Marret S, Laudenbach V, et al. Dual effect of glutamate on GABAergic interneuron survival during cerebral cortex development in mice neonates. Cereb Cortex. 2010;20:1092-108 pubmed publisher
    ..These data indicate a dual effect of glutamate on survival of immature and mature GABAergic neurons and suggest that ketamine may induce apoptosis of immature GABAergic neurons. ..
  49. Ahmed M, Siegelbaum S. Recruitment of N-Type Ca(2+) channels during LTP enhances low release efficacy of hippocampal CA1 perforant path synapses. Neuron. 2009;63:372-85 pubmed publisher
  50. Hettes S, Gonzaga W, Heyming T, Nguyen J, Perez S, Stanley B. Stimulation of lateral hypothalamic AMPA receptors may induce feeding in rats. Brain Res. 2010;1346:112-20 pubmed publisher
  51. Lin H, Mao S, Gean P. Block of gamma-aminobutyric acid-A receptor insertion in the amygdala impairs extinction of conditioned fear. Biol Psychiatry. 2009;66:665-73 pubmed publisher
    ..GABA(A) receptor insertion in the amygdala contributes a significant part to the extinction of fear memory. ..
  52. Sibilla S, Fabbro A, Grandolfo M, D Andrea P, Nistri A, Ballerini L. The patterns of spontaneous Ca2+ signals generated by ventral spinal neurons in vitro show time-dependent refinement. Eur J Neurosci. 2009;29:1543-59 pubmed publisher
    ..It is attractive to assume that periodic oscillations of Ca(2+) confer a summative ability to these cells to shape the plasticity of local circuits through different changes (phasic or tonic) in intracellular Ca(2+). ..
  53. Han S, Park S, Jeon J, Chang K, Ahn D, Oh S, et al. Functional type I vanilloid receptor expression by substantia gelatinosa neurons of trigeminal subnucleus caudalis in mice. Neurosci Lett. 2009;452:228-31 pubmed publisher
    ..These results indicate that a sub-population of SG neurons in the Vc express functional TRPV1 receptors, and that capsaicin can directly activate the TRPV1 receptor on the postsynaptic membrane of SG neurons. ..