Abstract：
:Neurones isolated from the CA1 region of rat hippocampal slices by the "vibrodissociation" method were voltage-clamped in the whole-cell configuration. The currents through N-methyl-D-aspartate (NMDA) channels were recorded in response to the rapid application (solution exchange time <30 msec) of 100 microM aspartate (ASP) in a Mg2+-free solution in the presence of 3 microM glycine. When added to the ASP solution, bepridil (BPD) caused a concentration-dependent decrease in both peak and stationary currents due to an uncompetitive open-channel blockade of NMDA channels. At -100 mV, the half-blocking concentration (IC50) for the stationary current was 14.01 +/- 0.17 microM (n = 10). The blocking and unblocking time constants were 7.4 +/- 0.3 x 10(3)/M/sec and 0.12 +/- 0.02/sec, respectively. Membrane hyperpolarization enhanced the BPD block. The equilibrium dissociation constant behaved as an exponential function of the membrane potential and increased e-fold every 37 mV.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Sobolevsky A,Koshelev S,Khodorov BIdoi
10.1016/s0028-3908(97)00003-8subject
Has Abstractpub_date
1997-03-01 00:00:00pages
319-24issue
3eissn
0028-3908issn
1873-7064pii
S0028390897000038journal_volume
36pub_type
杂志文章abstract：:Changes in astroglial volume were studied after incubating primary cultures from the cerebral cortex of newborn rats for 5 hr in taurine, glutamate or gamma-aminobutyric acid (GABA), alone or together with monoamine receptor agonists. Control cell volume was 2.2 microliters/mg protein. In the presence of taurine or gl...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(92)90165-l
更新日期：1992-01-01 00:00:00
abstract：:Stimulant drugs produce reward but also activate stress-responsive systems. The corticotropin-releasing factor (CRF) and the related hypothalamus-pituitary-adrenal (HPA) axis stress-responsive systems are activated by stimulant drugs. However, their role in stimulant drug-induced reward remains poorly understood. Here...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2017.01.024
更新日期：2017-05-01 00:00:00
abstract：:Efforts to translate sub-anesthetic ketamine infusions into widespread clinical use have centered around developing medications with comparable neurobiological activity, but with attenuated psychoactive effects so as to minimize the risk of behavioral toxicity and abuse liability. Converging lines of research, however...
journal_title：Neuropharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.neuropharm.2018.01.005
更新日期：2018-11-01 00:00:00
abstract：:Alterations in rapid eye movement sleep (REM) have been suggested as valid translational efficacy markers: activation of the metabotropic glutamate receptor 2 (mGluR2) was shown to increase REM latency and to decrease REM duration. The present paper addresses the effects on vigilance states of the mGluR2 positive allo...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.11.031
更新日期：2016-04-01 00:00:00
abstract：:Improgan is a chemical congener of the H2 antagonist cimetidine which shows the profile of a highly effective analgesic when administered directly into the CNS. Although the improgan receptor is unknown, improgan activates analgesic pathways which are independent of opioids, but may utilize cannabinoid mechanisms. To ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2006.04.003
更新日期：2006-09-01 00:00:00
abstract：:Methylazoxymethanol (MAM)-treated pregnant rat at gestation day (GD) 17 has been shown to be a valuable developmental animal model for schizophrenia. Yet, this model remains to be established in mice. In the present study, we examined behavioral, cytoarchitectural, and neurochemical changes in the offspring of MAM-tre...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2019.02.034
更新日期：2019-05-15 00:00:00
abstract：:The patch-clamp technique was used to study the effects of nystatin on a cloned delayed rectifier potassium channel (Kv1.3) expressed in Chinese hamster ovary (CHO) cells. Kv1.3 currents recorded in the whole-cell configuration, using an intracellular solution containing nystatin, were subjected to a time- and concent...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(96)00094-9
更新日期：1996-01-01 00:00:00
abstract：:Studies described here tested the hypothesis that phosphodiesterase 10A inhibition by a selective antagonist, MP-10, activates the dopamine D2 receptor expressing medium spiny neurons to a greater extent than the D1 receptor expressing neurons. We used regional pattern of c-Fos induction in the neostriatal subregions ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.08.008
更新日期：2015-12-01 00:00:00
abstract：:We have used a focal stimulation method to study neurotransmission at synapses onto hippocampal pyramidal neurons in cultures derived from neonatal rats. Single functional boutons were visualized by activity-dependent preloading with the fluorescent dye FM1-43, then focally stimulated by localized application of eleva...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(95)00143-t
更新日期：1995-11-01 00:00:00
abstract：:Tuberous Sclerosis Complex (TSC) is a multisystem genetic disorder caused by mutation in either Tsc1 or Tsc2 genes that leads to the hyper activation of the mTOR pathway, a key signalling pathway for synaptic plasticity. TSC is characterized by benign tumors arising in different organs and severe neuropsychiatric symp...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.11.003
更新日期：2013-04-01 00:00:00
abstract：:Many studies in preclinical animal models have described fear-reducing effects of the neuropeptide oxytocin in the central nucleus of the amygdala. However, recent studies have refined the role of oxytocin in the central amygdala, which may extend to the selection of an active defensive coping style in the face of imm...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2020.108130
更新日期：2020-08-15 00:00:00
abstract：:The effects of nefiracetam on GABA-induced chloride currents were studied with rat dorsal root ganglion neurons in primary culture using the whole-cell patch-clamp technique. The dose-response curve for GABA-induced currents was shifted by 16 microM to lower concentrations by 10 microM nefiracetam while the maximal re...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(96)00074-3
更新日期：1996-01-01 00:00:00
abstract：:We generated transgenic (Thy1alpha6) mice in which the GABA(A) receptor alpha6 subunit, whose expression is usually confined to granule cells of cerebellum and cochlear nuclei, is ectopically expressed under the control of the pan-neuronal Thy-1.2 promoter. Strong Thy1alpha6 subunit expression occurs, for example, in ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(02)00151-x
更新日期：2002-09-01 00:00:00
abstract：:Repeated stress exposure can lead to the development of anxiety and mood disorders. An emerging biological substrate of depression and associated pathology is the nucleus accumbens (NAc), which through interactions with limbic, cognitive and motor circuits can regulate a variety of stress responses. Within these circu...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2017.07.008
更新日期：2017-10-01 00:00:00
abstract：:The effects of the anxiolytic benzodiazepine flurazepam and the anxiogenic beta-carboline N-methyl-beta-carboline-3-carboxylate (FG 7142) were measured in unanaesthetised rats. Changes in motor activity, using a Doppler-shift microwave device, and in the extracellular concentration of ascorbate in the striatum and nuc...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(89)90087-7
更新日期：1989-05-01 00:00:00
abstract：:Alcohol damages the developing brain and can lead to fetal alcohol syndrome. One of alcohol's most important neuropathologic effects is neuronal death. As neurons mature, they become less vulnerable to alcohol-induced death because they acquire a protective signaling pathway, mediated by nitric oxide (NO). This pathwa...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2008.12.006
更新日期：2009-03-01 00:00:00
abstract：:Neurons in thalamic midline and paraventricular nuclei (PVT) display a unique slow afterhyperpolarizing potential (sAHP) following the low threshold spike (LTS) generated by activation of their low voltage Ca(2+) channels. We evaluated the conductances underlying this sAHP using whole-cell patch-clamp recordings in ra...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2014.06.023
更新日期：2014-11-01 00:00:00
abstract：:The risk of Alzheimer's disease (AD) is higher in patients with type 2 diabetes mellitus (T2DM). Previous studies in high-fat diet-induced AD animal models have shown that brain insulin resistance in these animals leads to the accumulation of amyloid beta (Aβ) and the reduction in GSK-3β phosphorylation, which promote...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2016.10.029
更新日期：2017-02-01 00:00:00
abstract：:(+)-2-Methyl-4-carboxyphenylglycine (LY367385), a potent and selective antagonist of mGlu1a metabotropic glutamate receptors, was neuroprotective in the following in vitro and in vivo models of excitotoxic death: (i) mixed cultures of murine cortical cells transiently exposed to N-methyl-D-aspartate (NMDA); (ii) rats ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(98)00159-2
更新日期：1999-02-01 00:00:00
abstract：:Adenosine 5'-triphosphate-sensitive potassium channel (KATP channel) activator, minoxidil sulfate (MS), can selectively increase the permeability of the blood-tumor barrier (BTB); however, the mechanism by which this occurs is still under investigation. Using a rat brain glioma (C6) model, we first examined the expres...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.08.004
更新日期：2013-12-01 00:00:00
abstract：:Alcohol use disorder (AUD) is a serious public health problem that results in tremendous social, legal and medical costs to society. Unlike other addictive drugs, there is no specific molecular target for ethanol (EtOH). Here, we report a novel molecular target that mediates EtOH effects at concentrations below those ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2019.01.021
更新日期：2019-05-01 00:00:00
abstract：:Mutations in LRRK2 (leucine-rich repeat kinase 2) are found associated with both sporadic and familial Parkinson's disease (PD). Pathogenic mutations are localized to the catalytic domains of LRRK2, including kinase and GTPase domains. Altered catalytic activity correlates with neurotoxicity, indicating that targeting...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2014.05.020
更新日期：2014-10-01 00:00:00
abstract：:In the present study, we investigated the effect of ACPT-I [(1S, 3R,4S)-1-aminocyclopentane-1,2,4-tricarboxylic acid], a blood-brain-barrier permeable agonist of group III mGlu receptor, against oxygen-glucose deprivation (OGD)-evoked neuronal cell death in primary neuronal cell cultures and in the model of transient ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.11.025
更新日期：2016-03-01 00:00:00
abstract：:Urocortin 3 (Ucn3) is an anorexigenic neuropeptide with high affinity for the type 2 corticotropin-releasing factor receptor (CRF₂-R). How the expression of hypothalamic Ucn3 is regulated by fasting and refeeding in genetically obese (fa/fa) Zucker rats is not known. Obese Zucker rats develop early hyperphagia associa...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2011.12.023
更新日期：2012-07-01 00:00:00
abstract：:Most current pharmacologic antidepressant treatments target monoaminergic systems confronts some problems such as low rate of remission and high risk for relapse indicating new therapeutic strategy is urgently need. Evidences showed that impairments in mitochondrial function were associated with the pathogenesis of mo...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2016.02.031
更新日期：2016-06-01 00:00:00
abstract：:Discovered and crystallized over sixty years ago, serotonin's important functions in the brain and body were identified over the ensuing years by neurochemical, physiological and pharmacological investigations. This 2008 M. Rapport Memorial Serotonin Review focuses on some of the most recent discoveries involving sero...
journal_title：Neuropharmacology
pub_type： 历史文章,杂志文章,评审
doi：10.1016/j.neuropharm.2008.08.034
更新日期：2008-11-01 00:00:00
abstract：:The metabotropic glutamate receptor 2 (mGlu2) plays an important role in the presynaptic control of glutamate release and several mGlu2 positive allosteric modulators (PAMs) have been under assessment for their potential as antipsychotics. The binding mode of mGlu2 PAMs is better characterized in functional terms whil...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2016.08.040
更新日期：2017-03-15 00:00:00
abstract：:Neurotrophins jointly exert various functions in the nervous system, including neuronal differentiation, survival, and regulation of synaptic plasticity. However, the functional interactions of neurotrophins or mechanisms through which neurotrophins regulate each other are still not clear. In the present study, brain-...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(02)00043-6
更新日期：2002-06-01 00:00:00
abstract：:Parkinson's disease (PD) is a neurodegenerative disease characterized by the progressive loss of dopaminergic neurons in the substantia nigra, leading to motor symptoms. Despite the remarkable improvements in the management of PD in recent decades, many patients remain significantly disabled. Metformin is a primary me...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2020.108173
更新日期：2020-09-15 00:00:00
abstract：:The purpose of the present studies was to investigate the behavioral and convulsant effects produced by the group I metabotropic glutamate receptor agonist (S)-3,5-dihydroxyphenylglycine (DHPG). Administered i.c.v. to mice, (S)-3,5-DHPG produced a behavioral syndrome consisting of scratching and/or facial grooming, tr...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2005.01.017
更新日期：2005-05-01 00:00:00
