• affinity
  • 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)
  • 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)
  • It binds at the GLP-1 receptor with greater affinity than GLP-1 (specifically due to the PSS sequence at the beginning of the 9-amino acid tail), is more potent at maintaining plasma insulin levels than GLP-1, and has a half-life of approximately 120 minutes in rodents (Wang et al. (scribd.com)
  • 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)
  • THCV has also high affinity for CB2 receptors and signals as a partial agonist, differing from both CBD and rimonabant. (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)
  • 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)
  • We envisage that the combination of glutamate and alpha-2 adrenergic antagonists could be potent therapies against neuronal damage following stroke and cardiac arrest. (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)
  • 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)
  • 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)
  • In our study, evidence is provided that strychnine, a competitive antagonist at glycine-gated Cl − channels, is also a potent competitive antagonist at native α-7-containing, α-bungarotoxin-sensitive nicotinic acetylcholine receptor (nAChRs). (aspetjournals.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)
  • Blockade
  • Conversely, EtOH enhancement of pcs IPSCs did not alter PPR and was not enhanced by SCH 50911 but was inhibited by blockade of noradrenergic receptors. (aspetjournals.org)
  • And Δ9-tetrahydrocannabivarin (THCV), a naturally occurring cannabinoid, modulate the effects of THC via direct blockade of cannabinoid CB1 receptors, thus behaving like first-generation CB1 receptor inverse agonists, such as rimonabant. (wikipedia.org)
  • subunit
  • 1 Studies have identified seven noncontinuous "loops" of amino acids that participate in agonist and competitive antagonist binding to the nAChR: loops A-C are on the α subunit (primary component of the binding site), and loops D-G are on the non-α subunit (complementary component of the binding site). (asahq.org)
  • acetylcholine
  • As an antagonist of the α7 nicotinic acetylcholine receptor. (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)
  • Nicotinic α7 acetylcholine receptor-mediated currents are not modulated by the tryptophan metabolite kynurenic acid in adult hippocampal interneurons. (wikipedia.org)
  • It is a type of α-neurotoxin, a neurotoxic protein that is known to bind competitively and in a relatively irreversible manner to the nicotinic acetylcholine receptor found at the neuromuscular junction, causing paralysis, respiratory failure, and death in the victim. (wikipedia.org)
  • It has also been shown to play an antagonistic role in the binding of the α7 nicotinic acetylcholine receptor in the brain, and as such has numerous applications in neuroscience research. (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)
  • spinal cord
  • Recording from identified SPNs in the intermediolateral cell column (IML) of rat spinal cord slices, application of the GABA receptor antagonist bicuculline, but not gabazine, elicited a change in voltage that lasted for the duration of application. (jneurosci.org)
  • 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)
  • peptide
  • To investigate the possibility that glucagon-like peptide-1 (7-36)-amide (GLP-1) receptor agonism may influence axonal structure and function through neuroprotection neurotrophic support, effects of GLP-1 and its long acting analog, Exendin-4 (Ex4) treatment on pyridoxine-induced peripheral neuropathy were examined in rats using behavioral and morphometric techniques. (scribd.com)
  • In the 1980s, several peptide antagonists derived from SP were the first NK1 receptor antagonists. (wikipedia.org)
  • For this reason, pharmaceutical companies concentrated on developing non-peptide NK1 receptor antagonists, and in 1991, three different companies revealed their first results. (wikipedia.org)
  • Since then, non-peptide NK1 receptor antagonists have been researched extensively and many structures and patents have appeared. (wikipedia.org)
  • The 9 amino acid bradykinin peptide elicits many responses including vasodilation, edema, smooth muscle spasm and pain fiber stimulation. (wikipedia.org)
  • BQ-123 is a cyclic peptide consisting of five amino acids. (wikipedia.org)
  • 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)
  • presynaptic
  • EtOH enhancement of local inhibitory postsynaptic currents (IPSCs) was associated with a significant decrease in paired-pulse ratio (PPR) and was significantly potentiated by the GABA B receptor antagonist SCH 50911 [(+)-( S )-5,5-dimethylmorpholinyl-2-acetic acid], consistent with a facilitation of GABA release from presynaptic terminals. (aspetjournals.org)
  • adrenergic
  • Furchgott RF (1972) The classification of adrenoceptors (adrenergic receptors). (springer.com)
  • In contrast, using an alpha 2-adrenergic receptor antagonist, a significant decrease in ischemic damage was found following 10 min of ischemia. (springer.com)
  • 3 For these reasons, multimodal pain control is advocated clinically, using combinations of cyclooxygenase inhibitors, local anesthetics, and other drugs such as α-adrenergic antagonists and gabapentin in conjunction with opioids. (asahq.org)
  • selectively
  • In situ injection of kainic acid: A new method for selectively lesioning neural cell bodies while sparing axons of passage. (springer.com)
  • Rimonabant blocks the CB1 receptor selectively and has been shown to decrease food intake and regulate body-weight gain. (wikipedia.org)
  • GABA
  • 1-Hydroxy-3-amino-pyrrolidone-2(HA-966): a new GABA-like compound, with potential use in extrapyramidal diseases" (PDF). (wikipedia.org)
  • schizophrenia
  • 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)
  • 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)