Abstract:
:Selective blockade of a subset of GABA(A) receptors may be involved in the antipsychotic effects of Clozapine and several other antipsychotic drugs. Seven antipsychotic drugs, and 11 drugs classified as antidepressants that only partially reverse the inhibitory effect of 1 microM GABA on [35S]TBPS binding, do not yield additive reversal when tested pairwise with Clozapine, which also only partially reverses the inhibitory effect of GABA. This suggests that all of these antipsychotic/antidepressant drugs may block a common subset of GABA(A) receptors. DMCM and Ro 5-4864 are also partial reversers of GABA's inhibitory effect, but they yield additive reversals when tested pairwise with the antipsychotic/antidepressant drugs, and also with each other, suggesting that DMCM, Ro 5-4864, and the antipsychotic drugs define three heterogeneous subsets of GABA(A) receptors, with variable overlap, depending on the drug. Several potent ligands for benzodiazepine binding sites can block the GABA inhibitory effects of DMCM and Ro 5-4864, but with different patterns: the ligands generally blocked DMCM less potently, but more completely than Ro 5-4864. Ro 5-4864 was not blocked by Flumazenil or CGS-8216, ligands that potently blocked DMCM. Nine additional antipsychotic/antidepressant drugs, as well as Clozapine, and 7 "classical" GABA(A) receptor blockers, all of which reversed GABA nearly completely, when tested at lower concentrations that only reverse approximately 20-35%, yielded almost complete additivity when tested pairwise with DMCM or Ro 54864. Another convulsant benzodiazepine, KW-1937, a positional isomer of Brotizolam, fully reverses the inhibitory effect of 1 microM GABA. At a lower concentration yielding about 50% reversal, KW-1937 is completely additive with DMCM, but entirely nonadditive with Ro 5-4864. The 50% reversal obtained with KW-1937 was potently blocked by Triazolam, but with a plateau similar to that obtained with Ro 5-4864. The results with KW- 1937 suggest that its 50% reversal largely corresponds to the reversal obtained with Ro 5-4864, and that virtually all of the [35S]TBPS binding sites inhibited by 1 microM GABA are coupled to benzodiazepine binding sites. The fraction of GABA(A) receptors preferentially blocked by all the antipsychotic/antidepressant drugs, roughly 25% of the [35S]TBPS binding sites inhibited with 1 microM GABA, are sensitive to KW-1937, but not to DMCM or to Ro 5-4864.
journal_name
Neurochem Resjournal_title
Neurochemical researchauthors
Squires RF,Saederup Edoi
10.1023/a:1027359422433subject
Has Abstractpub_date
1997-02-01 00:00:00pages
151-62issue
2eissn
0364-3190issn
1573-6903journal_volume
22pub_type
杂志文章abstract::Previous studies have shown that hypoxia induces nitric oxide synthase-mediated generation of nitric oxide free radicals leading to peroxynitrite production. The present study tests the hypothesis that hypoxia results in NO-mediated modification of Na+, K+-ATPase in the fetal brain. Studies were conducted in guinea pi...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1023/a:1012331108641
更新日期:2001-10-01 00:00:00
abstract::BCL-2-associated athanogene-1(BAG-1) is a multifunctional and anti-apoptotic protein that was first identified as a binding partner of BCL-2. But the effects and mechanisms for BAG-1 against hypoxic damage is unclear up to now. Whether BAG-1 could protect the human brain against hypoxic damage through up-regulating 70...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-017-2304-y
更新日期:2017-10-01 00:00:00
abstract::The effect of ageing and the relationships between the catalytic properties of enzymes linked to Krebs' cycle, electron transfer chain, glutamate and aminoacid metabolism of cerebral cortex, a functional area very sensitive to both age and ischemia, were studied on mitochondria of adult and aged rats, after complete i...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-009-0004-y
更新日期:2009-12-01 00:00:00
abstract::We observed a spot on two-dimensional (2-D) gel in the epileptic mutant strain E1 mice with a similar molecular weight but with a different isoelectric point of approximately 0.2, compared with its mother strain ddY mice. The collected protein from the E1 mice was identified as cytosolic NADP+-dependent isocitrate deh...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1023/a:1020981532281
更新日期:1999-03-01 00:00:00
abstract::A prominent feature of brain pathology in Alzheimer's disease is a robust activation of the neuronal lysosomal system and major cellular pathways converging on the lysosome, namely, endocytosis and autophagy. Recent studies that identify a disturbance of the endocytic pathway as one of the earliest known manifestation...
journal_title:Neurochemical research
pub_type: 杂志文章,评审
doi:10.1023/a:1007675508413
更新日期:2000-10-01 00:00:00
abstract::Docosahexaenoic acid (DHA) is verified to have neuroprotective effects on traumatic brain injury (TBI) rats by activating Nrf2 signaling pathway, but the role of NOX2 in this effect has not been illuminated. So this study explored the role of NOX2 in TBI models treated with DHA, aiming to complete the mechanism of DHA...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-020-03078-z
更新日期:2020-08-01 00:00:00
abstract::The release of the inhibitory neurotransmitter GABA is generally enhanced under potentially cell-damaging conditions. The properties and regulation of preloaded [3H]GABA release from mouse hippocampal slices were now studied in free radical-containing medium in a superfusion system. Free radical production was induced...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-007-9439-1
更新日期:2008-03-01 00:00:00
abstract::The present work describes the kinetics of enkephalin hydrolysis by plasma enzymes and the fragmentation pattern of both the parent peptide and of the first hydrolysis by-products. The degradation kinetics were followed by positive identification of the hydrolysis fragments by chromatographic methods, by amino acid an...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00964980
更新日期:1985-10-01 00:00:00
abstract::Metabolic modeling of dynamic (13)C labeling curves during infusion of (13)C-labeled substrates allows quantitative measurements of metabolic rates in vivo. However metabolic modeling studies performed in the brain to date have only modeled time courses of total isotopic enrichment at individual carbon positions (posi...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-012-0782-5
更新日期:2012-11-01 00:00:00
abstract::Although nitric oxide (NO) plays key signaling roles in the nervous systems, excess NO leads to cell death. In this study, the involvement of p38 mitogen-activated protein kinase (p38 MAPK) and apoptosis signal-regulating kinase-1 (ASK1) in NO-induced cell death was investigated in PC12 cells. NO donor transiently act...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1023/a:1010917129951
更新日期:2001-05-01 00:00:00
abstract::The MAO inhibitor phenelzine (PLZ) at a dose of 25 mg/kg does not affect the behavior of rats. In contrast, the equivalent dose of a deuterated analog (alpha, alpha, beta, beta-tetradeutero-PLZ, d4PLZ) elicits a biphasic behavioral syndrome in rats. In an attempt to correlate changes in cerebral monoamines with behavi...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00973322
更新日期:1988-02-01 00:00:00
abstract::Using the immunoblot technique, we found that an incubation of purified human myelin in 10 mM Tris-HCl buffer at pH 7.5 resulted in the conversion of the myelin-associated glycoprotein (MAG) to a smaller derivative (dMAG). Exogenously added 5 mM CaCl2 accelerated the conversion of MAG. In buffer containing more than 1...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00964509
更新日期:1984-05-01 00:00:00
abstract::Acidosis (pH 6.0) led to significant decrease in high-affinity choline uptake by rat brain synaptosomes. The effects persisted following pH readjustment (7.4) of the incubation medium, consisting of decrease in both Km and Vmax of the affinity system. pH readjustment coincided with synaptosomal leakage of lactate dehy...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00969699
更新日期:1995-07-01 00:00:00
abstract::Emerging data suggests that mitochondrial dysfunction is prominently involved in Alzheimer disease (AD) progression. Sirtuin-3 (Sirt3) is a member of the sirtuin family of nicotinamide adenine dinucleotide dependent deacetylases that regulates a variety of mitochondrial functions and suppresses mitochondria-related ph...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-015-1630-1
更新日期:2015-08-01 00:00:00
abstract::SENP3 (SUMO-specific proteases 3), a member of the small ubiquitin-like modifier specific protease family, was identified as a molecule that deconjugates SUMOylation of modified protein substrates and functions as an isopeptidase by disrupting SUMO homeostasis to facilitate cancer development and progression. However,...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-012-0869-z
更新日期:2012-12-01 00:00:00
abstract::The effects of a number of drugs that deplete catecholamines or block their receptors were investigated on the levels of free amino acids and glutamate decarboxylase activity in rat striatum and substantia nigra, in an attempt to clarify the possible links between catecholamine and amino acid transmitter function. Whi...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00966009
更新日期:1977-10-01 00:00:00
abstract::Fecal incontinence and constipation still remain the major complications after procedures for anorectal malformations (ARMs). Previous studies have demonstrated a decrease of neural cell in lumbosacral spinal cord of ARMs patients and rat models. However, the underlying mechanism remains elusive. In this study, the ne...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-017-2354-1
更新日期:2017-11-01 00:00:00
abstract::Acupuncture and moxibustion are traditional medical treatments that have come to play important roles in complementary and alternative medicines. Moxibustion also has a long history as a folk remedy in Japan, particularly due to the technical simplicity and selective efficacy on certain types of disease and distress. ...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-005-8839-3
更新日期:2005-12-01 00:00:00
abstract::Recent evidence suggests that young rodents submitted to high fructose (FRU) diet develop metabolic, and cognitive dysfunctions. However, it remains unclear whether these detrimental effects of FRU intake can also be observed in middle-aged mice. Nine months-old C57BL/6 female mice were fed with water (Control) or 10%...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-020-03135-7
更新日期:2020-12-01 00:00:00
abstract::This review presents data on metabotropic uridine nucleotide receptor subtypes (P2UR) activated by UTP, sometimes also by UDP and/or ATP. Some chemical details of receptor subtypes and ligand interactions are described. Ligand-activated P2UR subtypes may couple to different second messengers, yet little is known about...
journal_title:Neurochemical research
pub_type: 杂志文章,评审
doi:10.1023/a:1022487128766
更新日期:1997-08-01 00:00:00
abstract::Planarians are rapidly developing into very useful research subjects in pharmacology and neuroscience research. Here we report that curare, a cholinergic nicotinic receptor antagonist, alleviates the nicotine-induced planarian seizure-like movements (pSLM) by up to 50 % at equimolar concentrations of nicotine and cura...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-015-1512-6
更新日期:2015-10-01 00:00:00
abstract::The labeling of RNA in young and adult rat brain has been studied by measuring in vitro (tissue slices incubation) the incorporation of labeled uridine into RNA of total tissue and of the various subcellular fractions purified from cerebral hemispheres of 1- and 10-month-old rats. Gel electrophoretic analysis of the n...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00965100
更新日期:1983-04-01 00:00:00
abstract::Studies on primary astrocytes cultured in vitro have shown that process formation involves changes in cytoskeletal proteins and release of tension on the substratum. Actin filament reorganization has previously been found to be the major cytoskeletal change occurring during process formation. These changes are relativ...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1023/a:1022413718447
更新日期:1998-03-01 00:00:00
abstract::Mammalian MTH1 protein, a MutT-related protein, catalyzes the hydrolysis of 8-oxo-7,8-dihydroguanosine triphosphate (8-oxoGTP) to monophosphate, thereby preventing incorporation of 8-oxo-7,8-dihydroguanine (8-oxoguanine) into RNA. In this study, we applied immunohistochemistry to follow the expression of MTH1 and the ...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-011-0484-4
更新日期:2011-08-01 00:00:00
abstract::Regional cerebral glucose utilization (RCGU) and behavior were studied during naloxone-precipitated withdrawal in rats after chronic intravenous (IV) or intracerebroventricular (ICV) administration of sufentanil citrate, a potent, highly selective mu opiate agonist. Changes in RCGU were indistinguishable between the t...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF01006813
更新日期:1994-10-01 00:00:00
abstract::Unrelated cells such as dental follicle precursor cells (DFPCs) and retinal Müller cells (MCs) make spheres after cultivation in serum-replacement medium (SRM). Until today, the relation and molecular processes of sphere formation from different cell types remain undescribed. Thus in this study we compared proteomes o...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-011-0524-0
更新日期:2011-11-01 00:00:00
abstract::An in vitro model of anoxia-induced brain damage was utilized to help elucidate the biochemical basis of cell damage due to reduced oxygen availability. Previous studies suggest that anoxia-induced damage may vary presynaptically, post-synaptically or in the cell body. Thus, the consequences of an anoxic treatment inc...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00972482
更新日期:1988-04-01 00:00:00
abstract::Numerous studies have demonstrated that the Acetyl Coenzyme A-dependent arylamine NAT enzyme exist in many tissues of experimental animals including humans, and that NAT has been shown to be exist in mouse brain tissue. Increased NAT activity levels are associated with increased sensitivity to the mutagenic effects of...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1023/a:1007632326953
更新日期:2000-11-01 00:00:00
abstract::Glutamine synthetase (GS) is the major glutamine-forming enzyme of vertebrates and is accepted to be a marker of astroglial cells. Maturation of astroglial cells is characterized by an increase of GS activity, and the regulation of this enzyme is the topic of many publications. Because of the fundamental role of the G...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/s11064-005-2754-5
更新日期:2005-05-01 00:00:00
abstract::In vitro synthesis of myelin proteolipid protein (PLP) was explored at different ages using rat brain total homogenates, incubated for 30 min with [3H]glycine. Total proteolipids, extracted from the incubated samples, were separated by SDS-PAGE and the radioactivity was measured in the band corresponding to myelin PLP...
journal_title:Neurochemical research
pub_type: 杂志文章
doi:10.1007/BF00973044
更新日期:1984-09-01 00:00:00