Abstract：
:[3H]Strychnine binding to rat pons + medulla membranes was used as a measure of glycine receptors or glycine receptor-coupled chloride channels in vitro. A series of compounds structurally related to 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP), which previously were shown to antagonize glycine responses in cat spinal cord, inhibited [3H]strychnine binding in micromolar concentrations. The most potent of these glycine antagonists, 5,6,7,8-tetrahydro-4H-isoxazolo[3,4-d]azepin-3-ol (iso-THAZ), was also the most potent inhibitor of [3H]strychnine binding, with a Ki of 1,400 nM. The Ki value for strychnine was 7.0 nM, whereas the Ki value for the mixed gamma-aminobutyric acid (GABA)/glycine antagonist 3 alpha-hydroxy-16-imino-5 beta-17-aza-androstan-11-one (RU 5135) was only 4.6 nM. Sodium chloride (1,000 mM) enhanced the affinity of strychnine, brucine, isostrychnine, and the nonselective GABA antagonist pitrazepin for [3H]strychnine binding sites, whereas the affinities of glycine, beta-alanine, and taurine were reduced. These sodium chloride shifts, however, were not predictive of antagonist or agonist properties, since the sodium chloride shift for the glycine antagonist iso-THAZ and of the other THIP-related antagonists were similar to those of the glycine-like agonists. The various sodium chloride shifts show that different groups of ligands bind to glycine receptor sites in different ways.
journal_name
J Neurochemjournal_title
Journal of neurochemistryauthors
Braestrup C,Nielsen M,Krogsgaard-Larsen Pdoi
10.1111/j.1471-4159.1986.tb00667.xsubject
Has Abstractpub_date
1986-09-01 00:00:00pages
691-6issue
3eissn
0022-3042issn
1471-4159journal_volume
47pub_type
杂志文章abstract：:Exogenously administered estrogens can enhance the rate of increase of glucose 6-phosphate dehydrogenase activity in rat extensor digitorum longus muscles following denervation. In this communication, we report that the effect of denervation on glucose 6-phosphate dehydrogenase activity is modified by variations in en...
journal_title：Journal of neurochemistry
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doi：10.1111/j.1471-4159.1982.tb06660.x
更新日期：1982-06-01 00:00:00
abstract：:A diverse group of neurodegenerative diseases - including progressive supranuclear palsy (PSP), corticobasal degeneration and Alzheimer's disease among others, collectively referred to as tauopathies - are characterized by progressive, age-dependent intracellular formations of misfolded protein aggregates that play ke...
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journal_title：Journal of neurochemistry
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doi：10.1111/j.1471-4159.1989.tb09220.x
更新日期：1989-05-01 00:00:00
abstract：:Semaphorins are a family of secreted and membrane-associated proteins involved in growth cone guidance during development. Here, we describe the interaction of Semaphorin4F (Sema4F) with the post-synaptic density protein SAP90/PSD-95. Using the yeast two-hybrid system and coprecipitation assays we were able to show an...
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pub_type： 杂志文章
doi：10.1046/j.1471-4159.2001.00447.x
更新日期：2001-08-01 00:00:00
abstract：:We have examined the ability of KW-6002, an adenosine A2a antagonist, to modulate the dyskinetic effects of L-DOPA in 6-hydroxydopamine-lesioned rats. In animals rendered dyskinetic by a previous course of L-DOPA treatment, KW-6002 did not elicit any abnormal involuntary movements on its own, but failed to reduce the ...
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1985.tb08744.x
更新日期：1985-04-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/jnc.15119
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pub_type： 杂志文章
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更新日期：1985-01-01 00:00:00
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pub_type： 杂志文章
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更新日期：2007-12-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1471-4159.2006.04390.x
更新日期：2007-04-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1981.tb01676.x
更新日期：1981-03-01 00:00:00
abstract：:We have introduced a series of point mutations into the human opioid receptor-like (ORL1) receptor and characterized them for their ability to constitutively activate G protein-coupled receptor signalling pathways. Among the 12 mutants generated, mutation at Asn133 (N133W) gave increased basal signalling through three...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.2002.01231.x
更新日期：2002-12-01 00:00:00
abstract：:Exogenously added sialyl cholesterol (SC) induced neuritogenesis and accumulated in the nuclear fraction of a mouse neuroblastoma cell line, Neuro2a, as reported elsewhere. To clarify the significance of nuclear SC, we examined the structure of chromatin and its transcriptional level. The chromatin of SC-treated cells...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1992.tb11350.x
更新日期：1992-04-01 00:00:00
abstract：:Transgenic Huntington's disease (HD) mice, expressing exon 1 of the HD gene with an expanded CAG repeat, are totally resistant to striatal lesion induced by excessive NMDA receptor activation. We now show that striatal lesions induced by the mitochondrial toxin malonate are reduced by 70-80% in transgenic HD mice comp...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.2001.00482.x
更新日期：2001-08-01 00:00:00
abstract：:In view of a cytoprotective effect of elastase inhibitor on chemokine-mediated tissue injury, we examined the neuroprotective effect of ONO-5046, a specific inhibitor of neutrophil elastase, in rats with spinal cord injury. Standardized spinal cord compression markedly increased cytokine-induced neutrophil chemo-attra...
journal_title：Journal of neurochemistry
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doi：10.1046/j.1471-4159.2001.00488.x
更新日期：2001-09-01 00:00:00
abstract：:This study focused on the molecular and pharmacological characterization of muscarinic acetylcholine receptors expressed by progenitors and differentiated oligodendrocytes. We also analyzed the role of muscarinic receptors in regulating downstream signal transduction pathways and the functional significance of recepto...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.2001.00356.x
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1987.tb10020.x
更新日期：1987-10-01 00:00:00
abstract：:Microglia, macrophage-like cells in the CNS, are multifunctional cells; they play an important role in removal of dead cells or their remnants by phagocytosis in the CNS degeneration and are one of important cells in the CNS cytokine network to produce and respond to a variety of cytokines. The functions of microglia ...
journal_title：Journal of neurochemistry
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更新日期：1999-04-01 00:00:00
abstract：:Recent evidence indicates that tyrosine phosphorylation may play important roles in retinal photoreceptor rod outer segments (ROS). We investigated the tyrosine phosphorylation of endogenous proteins in isolated bovine ROS. Several proteins with apparent molecular masses of 31, 39, 60, 83, 90, 97, 120, 140, and 180 kD...
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更新日期：2012-08-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1988.tb01803.x
更新日期：1988-09-01 00:00:00
abstract：:Activation of extracellular signal-regulated protein kinase 1/2 (ERK1/2) are implicated in the pathophysiology of spinal cord injury (SCI). However, the specific functions of individual ERK isoforms in neurodegeneration are largely unknown. We investigated the hypothesis that ERK2 activation may contribute to patholog...
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更新日期：2010-04-01 00:00:00
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doi：10.1111/j.1471-4159.1993.tb13428.x
更新日期：1993-05-01 00:00:00
abstract：:The ATP-dependent glutamate uptake system in synaptic vesicles prepared from mouse cerebellum was characterized, and the levels of glutamate uptake were investigated in the cerebellar mutant mice, staggerer and weaver, whose main defect is the loss of cerebellar granule cells, and the nervous mutant, whose main defect...
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更新日期：2008-08-01 00:00:00
