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  • potent
  • S-(−)-HA-966 has been described as a "γ-hydroxybutyric acid (GHB)-like agent" and a "potent y-butyrolactone-like sedative", but it shows no affinity for the GABAB receptor (GABABR). (wikipedia.org)
  • SB-271046 was found to be potent and selective in vitro and had good oral bioavailability in vivo, but had poor penetration across the blood-brain barrier, so further SAR work was then conducted, which led to improved 5-HT6 antagonists such as SB-357,134 and SB-399,885. (wikipedia.org)
  • Kynurenic
  • Kynurenic acid (KYNA or KYN) is a product of the normal metabolism of amino acid L-tryptophan. (wikipedia.org)
  • It has been shown that kynurenic acid possesses neuroactive activity. (wikipedia.org)
  • As a result, kynurenic acid has been considered for use in therapy in certain neurobiological disorders. (wikipedia.org)
  • Conversely, increased levels of kynurenic acid have also been linked to certain pathological conditions. (wikipedia.org)
  • Kynurenic acid was discovered in 1853 by the German chemist Justus von Liebig in dog urine, which it was apparently named after. (wikipedia.org)
  • However, recently (2011) direct recording of α7 nicotinic acetylcholine receptor currents in adult (noncultured) hippocampal interneurons by the Cooper laboratory validated a 2009 study that failed to find any blocking effect of kynurenic acid across a wide range of concentrations, thus suggesting that in noncultured, intact preparations from adult animals there is no effect of kynurenic acid on α7 nicotinic acetylcholine receptor currents. (wikipedia.org)
  • High levels of kynurenic acid have been identified in patients suffering from tick-borne encephalitis, schizophrenia and HIV-related illnesses. (wikipedia.org)
  • A kynurenic acid hypothesis of schizophrenia was proposed in 2007, based on its action on midbrain dopamine activity and NMDArs, thus linking dopamine hypothesis of schizophrenia with the glutamate hypothesis of the disease. (wikipedia.org)
  • High levels of kynurenic acid have been identified in human urine in certain metabolic disorders, such as marked pyridoxine deficiency and deficiency/absence of kynureninase. (wikipedia.org)
  • When researchers decreased the levels of kynurenic acid in the brains of mice, their cognition was shown to improve markedly. (wikipedia.org)
  • Kynurenic acid shows neuroprotective properties. (wikipedia.org)
  • One controlled study kept mice on a ketogenic diet and measured kynurenic acid concentrations in different parts of the brain. (wikipedia.org)
  • It found that the mice on the ketogenic diet had greater kynurenic acid concentrations in the striatum and hippocampus compared to mice on a normal diet, with no significant difference in the cortex. (wikipedia.org)
  • Nicotinic α7 acetylcholine receptor-mediated currents are not modulated by the tryptophan metabolite kynurenic acid in adult hippocampal interneurons. (wikipedia.org)
  • CNQX
  • The local infusion of 2-amino-5-phosphonovalerate (500 microM), dizocilpine (50 microM) and CNQX (100 microM), started 80 min before cocaine injection, significantly inhibited the cocaine-induced increase in extracellular dopamine. (aspetjournals.org)
  • Simultaneous infusion of the two antagonists (500 microM 2-amino-5-phosphonovalerate and 100 microM CNQX) did not lead to further reductions in the effects of cocaine when compared to either antagonist alone. (aspetjournals.org)
  • PMID
  • PMID 2257491 Grotta J, Clark W, Coull B, Pettigrew LC, Mackay B, Goldstein LB, Meissner I, Murphy D, LaRue L. Safety and tolerability of the glutamate antagonist CGS 19755 (Selfotel) in patients with acute ischemic stroke. (wikipedia.org)
  • effects
  • Elmslie KS, Yoshikami D. (1985) Effects of kynurenate on root potentials evoked by synaptic activity and amino acids in the frog spinal cord. (wikipedia.org)
  • synapses
  • We observe that changing the number of vesicular transporters expressed at hippocampal excitatory synapses results in enhanced evoked and miniature responses and verify biophysically that these changes correspond to an increase in the amount of glutamate released per vesicle into the synaptic cleft. (jneurosci.org)
  • In recent years, it is on grounds of its quinoxline-dione structure, glutamate antagonism of him excitatory, afferent synapses of the cochlear inner hair cells and its neuroprotective properties that caroverine has been investigated as a new drug in the pharmacological treatment of tinnitus. (wikipedia.org)
  • inhibitory
  • In addition, we find that this modulation of synaptic strength by vesicular transporter expression is endogenously regulated, both across development to coincide with a maturational increase in vesicle cycling and quantal amplitude and by excitatory and inhibitory receptor activation in mature neurons to provide an activity-dependent scaling of quantal size via a presynaptic mechanism. (jneurosci.org)
  • Their action can be excitatory, increasing conductance, causing more glutamate to be released from the presynaptic cell, but they also increase inhibitory postsynaptic potentials, or IPSPs. (wikipedia.org)
  • citation needed] In general, spasticity develops when an imbalance occurs in the excitatory and inhibitory input to α motor neurons caused by damage to the spinal cord and/or central nervous system. (wikipedia.org)
  • glycine
  • The chemicals 2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV) and eglumegad activate only group II mGluRs, while 2-amino-4-phosphonobutyrate (L-AP4) activates only group III mGluRs. (wikipedia.org)
  • The glycine/N-methyl-D-aspartate receptor antagonist activity is specific to the R-(+) enantiomer, whereas the sedative and ataxic effects are specific to the S-(-) enantiomer. (wikipedia.org)
  • efficacy
  • Together, these findings underscore that vesicular transporter expression is used endogenously to directly regulate the extent of glutamate release, providing a concise presynaptic mechanism for controlling the quantal efficacy of excitatory transmission during synaptic refinement and plasticity. (jneurosci.org)
  • GABA
  • Pubmed ID: 11961124 Acid(B) funzionale gamma-amminobutirrico (recettori GABA(B)) montare da due subunità, GABA(B(1)) e GABA(B(2). (jove.com)
  • 1-Hydroxy-3-amino-pyrrolidone-2(HA-966): a new GABA-like compound, with potential use in extrapyramidal diseases" (PDF). (wikipedia.org)
  • neurons
  • The present work thus aims to more fully characterize the manner by which VGLUT1 expression is able to influence synaptic function and to elucidate whether neurons actually make use of this machinery endogenously, to presynaptically modulate the function of excitatory signaling. (jneurosci.org)
  • potent
  • S-(−)-HA-966 has been described as a "γ-hydroxybutyric acid (GHB)-like agent" and a "potent y-butyrolactone-like sedative", but it shows no affinity for the GABAB receptor (GABABR). (wikipedia.org)
  • sequence
  • While Arc mRNA is subject to degradation by NMD, the translated protein contains a PEST sequence at amino acids 351-392, indicating proteasome-dependent degradation. (wikipedia.org)
  • miniature
  • These animals proved viable and exhibit no gross malformations in neuronal architecture, but express higher levels of the GluR1 subunit and increased miniature excitatory postsynaptic currents (mEPSCs) in addition to displaying deficiencies in long-term memory. (wikipedia.org)
  • Pharmacology
  • Importanza Del Recettore Gamma-amminobutirrico Acid(B) C-termini Per Accoppiamento G-proteina Molecular Pharmacology. (jove.com)
  • protein
  • This discovery helped to establish the nature of the coding relationship that links information stored in genomic nucleic acid with protein expression in the living cell. (wikipedia.org)
  • activity
  • Caroverine, an N-methyl-D-aspartate and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist together with antioxidant activity, has been shown to protect the inner ear from excitotoxicity and to be effective in the treatment of tinnitus, sudden hearing loss and speech discrimination disorders in presbyacusis. (wikipedia.org)
  • structure
  • The amino acid structure of agelenin is Gly-Gly-Cys-Leu-Pro-His-Asn-Arg-Phe-Cys-Asn-Ala-Leu-Ser-Gly-Pro-Arg-Cys-Cys-Ser-Gly-Leu-Lis-Cys-Lis-Glu-Leu-Ser-Ile-Trp-Asp-Ser-Arg-Cys-Leu. (wikipedia.org)
  • produce
  • They showed that by using mRNA to insert multiple uracil repeats into the genome of the bacterium E. coli, they could cause the bacterium to produce a polypeptide consisting solely of repeated phenylalanine amino acids. (wikipedia.org)
  • group
  • In current clamp, blocking L-type Ca channels with the specific blocker nifedipine greatly reduced prolonged poststimulus firing and occluded the effect of adding group I mGluR antagonists. (jneurosci.org)
  • The results demonstrated that the firing rate after high-frequency synaptic stimulation was indeed reduced by blockade by group I mGluR antagonists. (jneurosci.org)
  • essential
  • Nevertheless, glutamate is formally classified as a non-essential amino acid, because it can be synthesized from alpha-Ketoglutaric acid, which is produced as part of the citric acid cycle by a series of reactions whose starting point is citrate. (wikipedia.org)
  • This essential amino acid is classified as neutral, and nonpolar because of the inert and hydrophobic nature of the benzyl side chain. (wikipedia.org)
  • As an essential amino acid, phenylalanine is not synthesized de novo in humans and other animals, who must ingest phenylalanine or phenylalanine-containing proteins. (wikipedia.org)
  • block
  • DACH-platin micelle NC-4016 is prepared through the formation of a polymer-metal complex between DACH-platin and the polyethylene glycol-poly (glutamic acid) block copolymer, PEG-P(Glu). (newyorkoncology.com)