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  • serotonin
  • a) The key features, including the transmembrane topology of nicotinic acetylcholine, γ‐aminobutyric acid (GABA A ), glycine and serotonin (5‐HT 3 ) receptors. (els.net)
  • A significant decrease in binding of 3H-QNB, 3H-Fluinitrazepam and 3H-Ketanserin, known to label cholinergic (muscarinic), benzodiazepine and serotonin (5HT(2A)) receptors respectively was observed at 1h exposure of PC-12 cells to HNE at 25 and 50microM concentrations. (sigmaaldrich.com)
  • Role of serotonin and other neurotransmitter receptors in brain development: basis for developmental pharmacology. (aspetjournals.org)
  • Results Hallucinogens and mefloquine bound stereoselectively and with relatively high affinity (Ki=0.71-341 nM) to serotonin (5-HT)₂ₐ but not 5-HT₁ₐ or 5-HT₂c receptors.Mefloquine but not chloroquine was a partial 5-HT₂ₐ agonist and a full 5-HT₂c agonist, stimulating inositol phosphate accumulation, with similar potency and efficacy as the hallucinogen dimethyltryptamine (DMT). (oregonstate.edu)
  • agonist
  • Furthermore, the analgesic effect of acupuncture can be replicated by direct injection of an adenosine A1 receptor agonist. (chiroaccess.com)
  • Here, using purified oligodendrocyte progenitors and cerebellar slice cultures, we show that norepinephrine and the beta-adrenergic receptor agonist isoproterenol also inhibited the proliferation, but in contrast to glutamate, isoproterenol stimulated progenitor lineage progression, as determined by O4 and O1 antibody staining. (biologists.org)
  • Despite the opposite effects on lineage progression, both isoproterenol and the glutamate receptor agonist kainate caused accumulation of the cyclin-dependent kinase inhibitors p27(Kip1)and p21(CIP1), and G1 arrest. (biologists.org)
  • The 5-HT1A and 5-HT1B receptors exhibited both high- and low-affinity states for agonist, with the majority of the receptors in a low-affinity state. (neurotransmitter.net)
  • A significantly higher affinity for agonist was observed with both receptors in the presence of alphai3 subunits compared with either alphai2 or alphao subunits, while a significantly lower concentration of alpha subunits was required for a maximal affinity shift of 5-HT1A receptors compared with 5-HT1B receptors (EC50 values of 6.4 and 12. (neurotransmitter.net)
  • The 5-HT1D and 5-HT1E receptors exhibited only a single affinity state for agonist. (neurotransmitter.net)
  • Addition of purified G protein subunits to membranes containing 5-HT1D receptors caused a small increase in affinity for agonist that was only partially reversed by guanine nucleotides while the addition of purified G protein subunits to membranes containing 5-HT1E receptors had no affect on agonist binding. (neurotransmitter.net)
  • hippocampus
  • Two main aims of this work were: (1) to assess whether chronic hyperammonemia increases inflammatory factors in the hippocampus and if this is associated with microglia and/or astrocytes activation and (2) to assess whether hyperammonemia-induced neuroinflammation in the hippocampus is associated with altered membrane expression of glutamate and GABA receptors and spatial learning impairment. (biomedcentral.com)
  • A third aim was to assess whether treatment with sulforaphane enhances endogenous the anti-inflammatory system, reduces neuroinflammation in the hippocampus of hyperammonemic rats, and restores spatial learning and if normalization of receptor membrane expression is associated with learning improvement. (biomedcentral.com)
  • All the receptor bindings were decreased in the left amygdala and pyrmidal cell layr of the left hippocampus. (nii.ac.jp)
  • However, the GABA,Benzodiazepine, 5-HT receptors were inversely increased in the fascia dentata of the hippocampus bilaterally. (nii.ac.jp)
  • Thus, CJP likely exerted its significant antianxiety effect by diminishing monoamine neurotransmitters and regulating mRNA expression of MR and GR in the hippocampus of our rat model of anxiety disorder. (hindawi.com)
  • Involvement of P2X7 receptors in the regulation of neurotransmitter release in the rat hippocampus. (ox.ac.uk)
  • antagonist
  • However, mefloquine was a very low potency antagonist at the D₃ receptor and mefloquine but not chloroquine or hallucinogens blocked [³H]5-HT uptake by the 5-HT transporter. (oregonstate.edu)
  • PPADS, the non-selective P2-receptor antagonist (3-30 microm), Brilliant blue G (1-100 nm) the P2X7 -selective antagonist and Zn2+ (0.1-30 microm) inhibited, whereas lack of Mg2+ potentiated the response by ATP. (ox.ac.uk)
  • ligands
  • Fluorescent receptor ligands provide a sensitive means of identifying and localizing various cellular receptors, ion channels and ion carriers. (thermofisher.com)
  • Additional fluorescently labeled receptor ligands (including low-density lipoproteins, epidermal growth factors, transferrin and fibrinogen conjugates and chemotactic peptides) are described in Probes for Following Receptor Binding and Phagocytosis-Section 16.1 , along with other probes for studying receptor-mediated endocytosis. (thermofisher.com)
  • More detailed analysis shows that two amino acid differences in the sixth transmembrane domain (Ile333 and Ser334 in the 5-HT1D beta receptor, corresponding to Lys310 and Glu311 in the 5-HT1E receptor) are largely responsible for the differential affinities of some, but not all, ligands for the 5-HT1D beta and 5-HT1E receptors. (neurotransmitter.net)
  • It is likely that these two amino acids subtly determine the overall three-dimensional structure of the receptor rather than interact directly with individual ligands. (neurotransmitter.net)
  • stimulation
  • Electrophysiological studies have indicated that some of the transplant receptors respond to physiological and pharmacological stimulation, suggesting that they are functional. (hindawi.com)
  • It has now become clear, however, that the heart rate and HRV are also determined by intrinsic properties of the pacemaker cells that comprise sinoatrial node, and that these properties respond to autonomic receptor stimulation in a non-linear mode. (omicsonline.org)
  • transporter
  • We characterized associations between central nervous system (CNS) adverse events and brain neurotransmitter transporter/receptor genomics among participants randomized to efavirenz-containing regimens in AIDS Clinical Trials Group studies in the USA. (ovid.com)
  • Efavirenz-related CNS adverse events were not associated with predicted neurotransmitter transporter/receptor gene expression levels in brain or with polymorphisms in these genes. (ovid.com)
  • Variable susceptibility to efavirenz-related CNS adverse events may not be explained by brain neurotransmitter transporter/receptor genomics. (ovid.com)
  • rats
  • In order to provide data on the degree to which various central neurotransmitter receptors are occupied in vivo, we performed ex vivo receptor occupancy studies with risperidone in comparison with clozapine and haloperidol in rats and guinea pigs. (nih.gov)
  • This reduces neuroinflammation, normalizes membrane expression of glutamate and GABA receptors, and restores spatial learning in hyperammonemic rats. (biomedcentral.com)
  • Regulation
  • Probes for Signal Transduction-Chapter 17 focuses on reagents for investigating events-such as calcium regulation, kinase, phosphatase and phospholipase activation, and lipid trafficking-that occur downstream from the receptor-ligand interaction ( Figure 16.2.1 ). (thermofisher.com)
  • Receptors function as agents of up- or down-regulation, depending upon the molecules that they bind to. (chiroaccess.com)
  • Biophysics, pharmacology, and regulation of glutamate receptors. (pitt.edu)
  • kainate
  • ATP (3-30 microm) and BzATP (0.6-6 microm) elicited concentration-dependent [14 C]glutamate efflux, and blockade of the kainate receptor-mediated transmission by CNQX (10-100 microm) and gadolinium (100 microm), decreased ATP evoked [3 H]GABA efflux. (ox.ac.uk)
  • localization
  • 1992 ) Beta-adrenergic receptors: astrocytic localization in the adult visual cortex and their relation to catecholamine axon terminals as revealed by electron microscopic immunocytochemistry. (biologists.org)
  • The text provides clearly structured information on the biosynthesis and degradation, localization, receptors, signal transduction pathways, and biological effects in the central nervous system, with all substances uniformly treated for an easy comparison of data. (mexmat.ru)
  • behavior
  • The G protein coupling behavior of four human 5-hydroxytryptamine receptor subtypes (5-HT1A, 5-HT1B, 5-HT1D, and 5-HT1E) has been studied in membranes from Sf9 cells expressing the individual receptors. (neurotransmitter.net)
  • neuron
  • Rather, the focus will be on chemical interneuronal communication involving the release of a neurotransmitter from one neuron, which alters the activity of the receiving neuron. (thefreelibrary.com)
  • intracellular
  • R PLC = Receptors promoting the hydrolysis of phosphatidylinositol 4,5-diphosphate (PIP 2 ) to inositol 1,4,5-triphosphate (IP 3 ), which increases intracellular Ca 2+ , and diacylglycerol (DAG), which activates protein kinase C (PKC). (thermofisher.com)
  • membrane
  • c) The arrangement of the subunits and the channel pore of the nicotinic acetylcholine receptor as viewed perpendicular to the plane of the membrane. (els.net)
  • d) The nicotinic acetylcholine (ACh) receptor in the membrane together with the acetylcholine‐binding site (drawn to scale). (els.net)
  • b) The G protein‐coupled receptor as viewed through the plane of the membrane. (els.net)
  • Thus when expressed in an identical membrane environment these four closely related 5-HT1 receptor subtypes exhibit different G protein coupling behaviors. (neurotransmitter.net)
  • Binding
  • Using saturation‐binding curves and Scatchard transformation, the affinity of the radioligand for the receptor can be determined. (els.net)
  • The decrease in the binding with DA-D2 receptors continued till 8h. (sigmaaldrich.com)
  • Two of these receptors, the 5-HT1D beta and the 5-HT1E receptors, are approximately 60% identical in the transmembrane domains that presumably form the ligand binding site yet have very different pharmacological properties. (neurotransmitter.net)
  • Binding of tryptamine analogs at h5-HT1E receptors: a structure-affinity investigation. (neurotransmitter.net)
  • protein
  • Most are G protein-coupled receptors, which span across the cell's surface more than once. (reference.com)
  • Pertinent features of G protein‐coupled neurotransmitter receptors. (els.net)
  • a) The key features, including the transmembrane topology of metabotropic G protein‐coupled receptors. (els.net)
  • That entity is the receptor, which is simply defined as any structure (a protein molecule) which receives and responds to an environmental stimulus. (chiroaccess.com)
  • Human 5-HT1 receptor subtypes exhibit distinct G protein coupling behaviors in membranes from Sf9 cells. (neurotransmitter.net)
  • Addition of purified G protein subunits to membranes expressing either 5-HT1A or 5-HT1B receptors shifted the majority of the receptors to a high-affinity state in the absence, but not in the presence, of guanine nucleotides. (neurotransmitter.net)
  • vitro
  • Conclusions Mefloquine, but not chloroquine, shares an in vitro receptor interaction profile with some hallucinogens and this neurochemistry may be relevant to the adverse neuropsychiatric effects associated with mefloquine use by a small percentage of patients. (oregonstate.edu)
  • C-IAP.In vitro multiple tracer autoradio graphy on these adjacent sections was performed using ^3H-MK801, ^3H-QNB,^3H-Muscimol, ^3H-Ro15-1788, ^3H-5-HT.The receptor bindings were measured with image analyzer. (nii.ac.jp)
  • transmembrane
  • Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. (neurotransmitter.net)
  • Analysis of the pharmacological properties of a series of chimeric 5-HT1D beta/5-HT1E receptors indicates that sequences in the sixth and seventh transmembrane domains are responsible for the differential affinity of 5-carboxamidotryptamine for these two receptors. (neurotransmitter.net)
  • respectively
  • 80%) was achieved before H1, D2, alpha 1 and alpha 2 receptors became occupied (ED50 = 0.45, 0.66, 0.75 and 3.7 mg/kg, respectively). (nih.gov)
  • Haloperidol occupied D2 and alpha 1 receptors at low doses (ED50 = 0.13 and 0.42 mg/kg, respectively) and 5-HT2 receptors at a higher dose (ED50 = 2.6 mg/kg). (nih.gov)
  • release
  • Neurotransmitter is used here in its most general sense , including not only messengers that act to regulate ion channels , but also those which act on second messenger systems and those which may act at a distance from their release sites . (biology-online.org)
  • On one hand, we found that hsp90 is necessary for the efficient neurotransmitter release at the presynaptic terminal. (jneurosci.org)