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  • 1992
  • Burnashev N, Monyer H, Seeburg PH, Sakmann B (1992) Divalent ion permeability of AMPA receptor channels is dominated by the edited form of a single subunit. (springer.com)
  • induces phase shifts in the rhythm of neuronal firing rate in a pattern that mimics that of light, and microinjection of NMDA or non-NMDA antagonists into the SCN region blocks the phase-shifting effects of light in hamsters ( Colwell and Menaker, 1992 ). (jneurosci.org)
  • affinity
  • Consistent with these predictions, cis -PPDA displays a 35-fold higher affinity for NR2B-containing NMDA receptors than trans -PPDA. (aspetjournals.org)
  • In contrast, the NR2B H486F mutation increased the affinity of the typical antagonists CGS-19755 [(2 R *,4 S *)-4-phosphonomethyl-2-piperidine carboxylic acid] and 4-(3-phosphonopropyl) piperidine-2-carboxylic acid. (aspetjournals.org)
  • have reported that racemic methadone possesses affinity for the NMDA receptor in rat cortical membranes, and reduces NMDA-induced depolarization in vitro in rat spinal cord and cortical wedge preparations. (aspetjournals.org)
  • This protein is a type B gastrin receptor, which has a high affinity for both sulfated and nonsulfated CCK analogs and is found principally in the central nervous system and the gastrointestinal tract. (wikipedia.org)
  • Eastman Kodak and Sterling Winthrop discovered steroid series of tachykinin NK1 receptor antagonists that yielded some compounds but lacked sufficient affinity for the NK1 receptor, despite structure-activity relationship (SAR) studies that were performed. (wikipedia.org)
  • binding protein
  • And the discovery 3 and structure determination 4 of a water-soluble analog to the extracellular domain of the receptor, acetylcholine binding protein (AChBP), has led to inferences about structure-function relations of the nAChR. (asahq.org)
  • Noncompetitive
  • In rat brain cortex synaptosomes superfused with Mg 2+ -free solution containing glycine, [ 3 H]noradrenaline ( 3 H-NA) release evoked by NMD A was abolished by omission of glycine or Ca 2+ and inhibited by Mg 2+ , the competitive and noncompetitive NMDA receptor antagonists CGP 37849 and dizocilpine (MK-801), respectively, as well as by ethanol, but was not affected by tetrodotoxin. (springer.com)
  • Lodge D, Johnson KM (1990) Noncompetitive excitatory amino acid receptor antagonists. (springer.com)
  • We propose that an ischemic insult, severe enough to cause prolonged periods of membrane depolarization, induces changes in the membrane properties leading to cycling of calcium ions across the plasmamembrane, which cannot be blocked by noncompetitive NMDA receptor antagonist. (springer.com)
  • As a noncompetitive antagonist at the glycine site of the NMDA receptor. (wikipedia.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)
  • PMID 10541229 Davis SM, Lees KR, Albers GW, Diener HC, Markabi S, Karlsson G, Norris J. Selfotel in acute ischemic stroke : possible neurotoxic effects of an NMDA antagonist. (wikipedia.org)
  • PMID 11172782 Ikonomidou C, Turski L. Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? (wikipedia.org)
  • dopamine
  • Grieder et al (2012) Phasic D1 and tonic D2 dopamine receptor signaling double dissociate the motivational effects of acute nicotine and chronic nicotine withdrawal. (tocris.com)
  • Excitatory amino acid antagonists attenuate the effects of cocaine on extracellular dopamine in the nucleus accumbens. (aspetjournals.org)
  • 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)
  • 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)
  • CCK-B receptors possess a complex regulation of dopamine activity in the brain. (wikipedia.org)
  • CCK-B receptors modulate dopamine release, and influence the development of tolerance to opioids. (wikipedia.org)
  • glycine
  • 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)
  • R-(+)-HA-966 did not induce drug-appropriate responding in animals trained to discriminate phencyclidine (PCP) from saline, suggesting that the glycine receptor ligand R-(+)-HA-966 has a significantly different behavioral profile than drugs affecting the ion channel of the NMDA receptor complex. (wikipedia.org)
  • where glycine receptors are rare ( Frostholm and Rotter, 1985 ), strongly support the notion that some of the toxic effects of this alkaloid can be accounted for by its action on receptors other than the glycine receptors in the CNS. (aspetjournals.org)
  • Kynurenic acid acts in the brain as a glycine-site NMDAr antagonist, key in glutamatergic neurotransmission system, which is thought to be involved in the pathophysiology and pathogenesis of schizophrenia. (wikipedia.org)
  • Subtypes
  • For instance, studies of the interactions of epibatidine, α-conotoxin-ImI and amantadine with neuronal nAChRs have suggested that different subtypes of these receptors are likely to be involved in analgesia, convulsions and Parkinson's disease. (aspetjournals.org)
  • extracellular
  • NK1 receptor, as well as the other tachykinin receptors, is made of seven hydrophobic transmembrane (TM) domains with three extracellular and three intracellular loops, an amino-terminus and a cytoplasmic carboxy-terminus. (wikipedia.org)
  • It is activated by proteolytic cleavage of its extracellular amino terminus. (wikipedia.org)
  • neuronal
  • Göthert M, Thielecke G (1976) Inhibition by ethanol of noradrenaline output from peripheral sympathetic nerves: possible interaction of ethanol with neuronal receptors. (springer.com)
  • Several investigations have demonstrated protection against neuronal damage following global and focal ischemia, using antagonist against the N-methyl-d-aspartate (NMDA) receptor. (springer.com)
  • Block, G.A., Pulsinelli, W.A. (1987) Excitatory amino acid receptor antagonists: Failure to prevent ischemic neuronal damage. (springer.com)
  • Studies directed at determining the ability of centrally acting compounds to interact with native neuronal nAChRs have been helpful in improving the understanding of the functions of these receptors in the CNS. (aspetjournals.org)
  • antagonism
  • d- Methadone at an intrathecal dose of 250 μg shifted the ED 50 value for NMDA-induced nociceptive behaviors more than 3-fold to the right, which indicates an antagonism of these NMDA receptor-mediated effects. (aspetjournals.org)
  • Bäckström and Hyytiä (2006) Ionotropic and metabotropic glutamate receptor antagonism attenuates cue-induced cocaine seeking. (tocris.com)
  • inhibit
  • CB1 receptors are coupled through Gi/o proteins and inhibit adenylyl cyclase and activate mitogen-activated protein (MAP) kinase. (wikipedia.org)
  • In addition, CB1 receptors inhibit presynaptic N- and P/Q-type calcium channels and activate inwardly rectifying potassium channels. (wikipedia.org)
  • The observation that a single molecule of the toxin suffices to inhibit channel opening is in agreement with experimental data on the amount of toxin per receptor. (wikipedia.org)
  • 1989
  • Banay-Schwartz M, Lajtha A, Palkovits M (1989) Changes with ageing in the levels of amino acids in rat CNS structural elements. (springer.com)
  • Fink K, Göthert M, Molderings G, Schlicker E (1989) N-Methyl-D-aspartate (NMDA) receptor-mediated stimulation of noradrenaline release, but not of other neurotransmitters, in the rat brain cortex: receptor location, characterization and desensitization. (springer.com)
  • Application of non-NMDA antagonists blocks excitatory postsynaptic potentials in SCN cells after stimulation of the optic nerves ( Cahill and Menaker, 1989 ). (jneurosci.org)
  • nucleotide sequence
  • The present invention refers to muteins of the C5a anaphylatoxin (C5a) which are C5a receptor antagonists, to nucleic acid molecules comprising a nucleotide sequence encoding such muteins of C5a anaphylatoxin, to host cells containing a nucleic acid molecule comprising a nucleotide sequence encoding such muteins of the C5a anaphylatoxin as well as to a pharmaceutical composition comprising a mutein of the C5a anaphylatoxin acting as a C5a receptor antagonists. (freepatentsonline.com)
  • vivo
  • To determine whether d- methadone has functional, in vivo NMDA receptor antagonist activity, the antinociceptive effects of d- methadone were evaluated in the rat tail-flick and formalin tests. (aspetjournals.org)
  • Thus, d- methadone, although it has little opioid activity, may be antinociceptive if it possesses in vivo NMDA receptor antagonist activity and may contribute to the analgesic effects of racemic methadone. (aspetjournals.org)