• Ion channels coupled to NMDA, kainate and AMPA receptors are the target of pharmacological regulation by a variety of drugs and ions. (nih.gov)
  • While these channels are all nonselectively permeated by Na+ and K+ ions, the NMDA receptor-channel complex contains a number of pharmacological sites distinct from those found on the others. (nih.gov)
  • In addition, there is electrophysiological evidence that input from the contralateral vestibular nerve via the contralateral VN is partially mediated by N -methyl- d -aspartate (NMDA) receptors. (springer.com)
  • Input to the VN from the spinal cord may also be partially mediated by NMDA receptors. (springer.com)
  • A number of recent studies in the area of vestibular plasticity have reported that antagonists for the NMDA receptor subtype disrupt the behavioral recovery that occurs following unilateral deafferentation of the vestibular nerve fibers (vestibular compensation). (springer.com)
  • Alford S. and Williams T. L. (1989) Endogenous activation of glycine and NMDA receptors in lamprey spinal cord during fictive locomotion. (springer.com)
  • Collingridge G. L. and Bliss T. V. P. (1987) NMDA receptors-their role in long term potentiation. (springer.com)
  • The binding of 3H-AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) to quisqualate receptors, 3H-kainic acid (KA) to kainate receptors, and 3H-glutamate to N-methyl-D-aspartate (NMDA) receptors as determined by quantitative autoradiography. (jneurosci.org)
  • This was associated with a 60% decrease in AMPA binding and a 25% decrease in glutamate binding to NMDA receptors. (jneurosci.org)
  • In a rat model of morphine tolerance, we examined the hypotheses that thermal hyperalgesia to radiant heat develops in association with the development of morphine tolerance and that both the development and expression of thermal hyperalgesia in morphine-tolerant rats are mediated by central NMDA and non-NMDA receptors and subsequent protein kinase C (PKC) activation. (jneurosci.org)
  • a non-NMDA receptor antagonist), or GM1 ganglioside (an intracellular PKC inhibitor) treatment was given to examine the effects of these agents on the development and expression of thermal hyperalgesia in morphine- tolerant rats. (jneurosci.org)
  • The data indicate that thermal hyperalgesia develops in association with the development of morphine tolerance and that the coactivation of central NMDA and non-NMDA receptors is crucial for both the development and expression of thermal hyperalgesia in morphine-tolerant rats. (jneurosci.org)
  • A fast excitatory postsynaptic current (EPSC) is mediated by non-NMDA receptors and a slow EPSC is mediated by NMDA receptors. (royalsocietypublishing.org)
  • Other smaller EPSCS mediated by NMDA and non-NMDA receptors, and a strychnine-sensitive synaptic current, are also present. (royalsocietypublishing.org)
  • Given the specialization of the calyx of Held, it seems that the NMDA-receptor ion channel complex is not primarily serving to potentiate a subthreshold input, but may be involved in the development and maintenance of this exuberant somatic synapse. (royalsocietypublishing.org)
  • Intrathecal administration of 7-chlorokynurenate (7CK, 0.25-2.5 mu g), a functional antagonist at the glycine site of the NMDA receptor, did not alter the first phase of the formalin response. (ucl.ac.uk)
  • The role of (+/-)-alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA)-kainate and N-methyl-D-aspartate (NMDA) receptors in the rostral ventrolateral medulla (RVLM) and caudal ventrolateral medulla (CVLM) on the central respiratory drive (CRD)-related activity of splanchnic sympathetic nerve activity (SNA) was examined in rats. (semanticscholar.org)
  • The resolved X-ray crystal structures of the glutamate-binding domain (S1/S2 domains) of the GluR2 and NR1 glutamate receptor subunits were used to model the homologous regions of the N -methyl- d -aspartate (NMDA) receptor's NR2 subunits. (aspetjournals.org)
  • Consistent with these predictions, cis -PPDA displays a 35-fold higher affinity for NR2B-containing NMDA receptors than trans -PPDA. (aspetjournals.org)
  • Of these residues, mutational analysis and modeling suggest that A414, R712, and G713 (NR2B numbering) may be especially useful for developing NR2C- and NR2D-selective NMDA receptor antagonists and that residues A414 and T428 may determine subunit variations in agonist affinity. (aspetjournals.org)
  • antagonists that selectively block different NR2-containing NMDA receptors are likely to have markedly different physiological and therapeutic/adverse effects. (aspetjournals.org)
  • Interestingly, NMDA receptor (NMDAR) activation requires a second "coagonist. (arvojournals.org)
  • Targeting sites within heterodimer interfaces led us to identify a series of robust light-sensitive NMDA receptors of GluN2A and GluN2B subtypes, two major subtypes playing distinct functional roles. (riken.jp)
  • Our works are important for neuropharmacology because the NMDA receptors are promising drug targets for the development of therapeutic compounds to treat neuronal diseases including depression and Alzheimer's. (riken.jp)
  • Notably, recent H9N2 viruses have acquired molecular markers that allow for a transition from "avian-like" to "human-like" terminal sialic acid (SA) receptor recognition via a single amino acid change at position 226 (H3 numbering), from glutamine (Q226) to leucine (L226), within the HA receptor-binding site (RBS). (flu.org.cn)
  • This study shows the flexibility of position 226 of the HA of H9 influenza viruses and the resulting effect of single amino acid changes on the phenotype of variants in vivo and in vitro ImportanceA single amino acid change at position 226 in the hemagglutinin (HA) from glutamine (Q) to leucine (L) has been shown to play a key role in receptor specificity switching in various influenza HA subtypes, including H9. (flu.org.cn)
  • In this report, we compared and contrasted the pharmacology of raloxifene to block or induce E 2 -stimulated increase in TGF-α mRNA in stable transfectants of ER-negative human breast cancer cells with the cDNAs from wild-type, mutant-amino acid (AA) 400 ER and mutant-AA 351 ER. (aacrjournals.org)
  • On the other hand, V247 on TM6.40 plays a critical role in maintaining the receptor in the inactive state, and the substitution of V247 impaired the receptor constraint and stabilized an active conformation. (harvard.edu)
  • Substitution by aspartic acid, lysine or tyrosine totally eliminated androgen binding and the mutated androgen receptors did not have any transcriptional activating potential with either R1881, R5020 or estradiol. (eur.nl)
  • The alpha 2 subunit has a threonine residue, a conservative substitution for serine, at amino acid 52. (garvan.org.au)
  • These data suggest that the mutation of an alanine to serine at amino acid 52 of the alpha subunit is responsible for the difference in ethanol sensitivity seen in homomeric receptors composed of alpha 1 and alpha 2 subunits. (garvan.org.au)
  • A cyclic hexapeptide comprising alternating alpha-aminoxy and alpha-amino acids is a selective chloride ion receptor. (nih.gov)
  • In nonpolar solvents, the cyclic hexapeptide 2, which comprises alternating D-alpha-amino and D-alpha-aminoxy acids, adopts a C3-symmetric conformation with alternating eight (N--O turns)- and seven (gamma turns)-membered-ring hydrogen bonds. (nih.gov)
  • N-Formylation and N-methylation of the alpha-amino group of L-phenylalanine result in extremely decreased responses of the labellar sugar receptor of the fleshfly, whereas the same structural alteration of L-valine hardly affects the response. (rupress.org)
  • The researchers further determined that the genes for T1R1 and T1R3, which make up the new receptor, display individual variation. (scientificamerican.com)
  • Here calcium imaging of isolated TSCs and taste cell clusters from the circumvallate and foliate papillae of C57BL/6J and T1r3 knockout mice was performed to determine if other receptors are involved in the detection of L-amino acids and IMP. (uvm.edu)
  • Although two selective mutants on Leu128, Leu128Ala (L128A) and Leu128Arg (L128R), demonstrated high binding affinity to IL-8, they were not capable of coupling to G proteins and consequently lost the functional response of the receptors. (harvard.edu)
  • This amino acid change is responsible for the increased affinity of the mutant receptor protein for progestagens and estrogens. (eur.nl)
  • All of the electrophysiological studies conducted so far have used in vitro preparations, and it is possible that denervation of the VN during the preparation of an explant or slice causes changes in EAA receptor function. (springer.com)
  • Charles Zuker of the University of California, San Diego and colleagues discovered and tested the receptor, dubbed T1R1+3, in both mice and humans. (scientificamerican.com)
  • In humans, T1R1+3 is more sensitive to the chemical glutamate than to any other amino acid. (scientificamerican.com)
  • Regarding coexpression of l -AA receptors, the mGluRs and T1R1 were similarly coexpressed with CaSR (10-12% of cells) whereas GPRC6a was coexpressed least (7% of cells). (springer.com)
  • Maria A. Panaro, Margherita Sisto, Carlo I. Mitolo, Antonia Cianciulli and Vincenzo Mitolo, " Mutation, Selection and the Amino Acid Hydropathic Character: A Study on Receptor Genes Involved in Immune and Non-Immune Functions", Endocrine, Metabolic & Immune Disorders - Drug Targets (2009) 9: 47. (eurekaselect.com)
  • No differences were found in ethanol sensitivity between alpha 2 and the mutant alpha 1(A52S) receptors. (garvan.org.au)
  • The general anesthetic propofol was also tested in homomeric alpha 1, alpha 2, or the mutant alpha 1(A52S) receptors. (garvan.org.au)
  • Toll-like receptor (TLR) signaling plays a central role in the pathophysiology of many acute and chronic human inflammatory diseases, and pharmacological regulation of TLR responses is anticipated to be beneficial in many of these inflammatory conditions. (sigmaaldrich.com)
  • Ratiometric imaging with Fura-2 was used to study calcium responses to IMP and four L-amino acids (monopotassium L-glutamate, L-serine, L-arginine, and L-glutamine) with and without IMP. (uvm.edu)
  • Our data indicate that synergistic and non-synergistic responses to L-amino acids and IMP are mediated by multiple receptors or possibly a receptor complex. (uvm.edu)
  • A theoretical analysis demonstrated that random mutations in the first nt preserve hydrophobicity in 73 % of triplets coding for hydrophobic amino acids (aa) and hydrophilicity in 77 % of triplets coding for hydrophilic aa, while random mutations in the second nt preserve hydrophobicity in 18 % of triplets coding for hydrophobic aa and hydrophilicity in 53 % of triplets coding for hydrophilic aa. (eurekaselect.com)
  • Acar I, Cetinkaya A, Lay I, Ileri-Gurel E (2018) The role of calcium sensing receptors in GLP-1 and PYY secretion after acute intraduodenal administration of L-tryptophan in rats. (springer.com)
  • Now scientists have identified a taste receptor that may play a part in making sure we consume enough of it. (scientificamerican.com)
  • Avau B, Rotondo A, Thijs T, Andrews CN, Janssen P, Tack J, Depoortere I (2015) Targeting extra-oral bitter taste receptors modulates gastrointestinal motility with effects on satiation. (springer.com)
  • Taste receptors in the taste sensory cells that detect food molecules are the key players in selecting dietary nutrients. (uvm.edu)
  • Their effectiveness depends mainly on the place of the constituent amino acids rather than on their composition, indicating the decisive role that certain aliphatic amino acids in the C-terminal position play in stimulation. (rupress.org)
  • Here, we show that murine mucosal homogenates and STC-1 cells, a murine enteroendocrine cell line, express mRNA for all l -AA receptors. (springer.com)
  • In some mRNA sequences, namely those of formyl peptide receptors and chemokine CXC receptors 4, it has been observed that the second nucleotide (nt) of the coding triplets is significantly more highly conserved than the first nt and the correlation between the conservation indexes of the first two nt is positive and significantly higher than the "basic" correlation usually found between adjacent nt. (eurekaselect.com)
  • By using cell-cell fusion and pseudotype virion infection assays, we found that HERV-W Env efficiently uses both hASCT2 and the related transporter hASCT1 (gene name, SLC1A4) as receptors. (asm.org)
  • These results suggest a substantial difference in the stereospecificities and functional group specificities of the furnase (F) and aliphatic carboxylate (T) sites in the sugar receptor. (rupress.org)
  • The results of these experiments showed that the response patterns elicited by L-amino acids varied significantly across TSCs. (uvm.edu)
  • The results reveal that amino acids other than L226 and Q226 are well tolerated and that some amino acids allow for the recognition of both avian and human influenza receptors in the absence of other changes. (flu.org.cn)
  • The recognition of ASCT1 and ASCT2 despite this divergence of their sequences strongly suggests that the use of both receptors has been highly advantageous for survival and evolution of the HERV-W family of retroviruses. (asm.org)