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：:An important feature of cocaine addiction in humans is the emergence of negative affect (e.g., dysphoria, irritability, anhedonia), postulated to play a key role in craving and relapse. Indeed, the DSM-IV recognizes that social, occupational and/or recreational activities become reduced as a consequence of repeated dr...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2013.04.025
更新日期：2014-01-01 00:00:00
abstract：:The effect of chronic (4 weeks) treatment of rats with the antidepressant drugs desipramine, maprotiline, chlorimipramine, zimelidine or iprindol on the sensitivity of presynaptic alpha 2- and postsynaptic beta-adrenoceptors in neocortical slices was investigated. Acute (1 day) treatment with the antidepressants did n...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(84)80002-7
更新日期：1984-02-01 00:00:00
abstract：:Up to 80% of cancer patients are affected by the cancer anorexia-cachexia syndrome (CACS), which leads to excessive body weight loss, reduced treatment success and increased lethality. The area postrema/nucleus of the solitary tract (AP/NTS) region emerged as a central nervous key structure in this multi-factorial pro...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2020.108289
更新日期：2020-12-01 00:00:00
abstract：:A genetic component is associated with the development of many forms of epilepsy. Recently, mutations in the GABAA receptor have been linked to several inherited epilepsies. One of these mutations is a non-conservative change of alanine to aspartate in the third transmembrane domain of the alpha1 subunit. To determine...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2003.11.015
更新日期：2004-04-01 00:00:00
abstract：:The modulation of insect behavior for the purpose of controlling the spread of infectious diseases has been the task of a few insect repellents for which the mechanistic modes of action on odorant receptors (ORs) are unclear. Here, we study the effects of the repellents DEET and IR3535, and a novel OR co-receptor (Orc...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.01.004
更新日期：2012-04-01 00:00:00
abstract：:There is no in situ evidence hitherto for a modulation by ATP of the glutamatergic excitatory transmission onto medium spiny neurons (MSNs) in the rat striatum. In order to resolve this question, we used the patch-clamp technique in brain slice preparations to record excitatory postsynaptic currents (EPSCs) evoked by ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2011.12.001
更新日期：2012-03-01 00:00:00
abstract：:Vasopressin V1a receptors in the rat brain have been studied for their role in modulating aggression and anxiety. In the current study blood-oxygen-level-dependent (BOLD) functional MRI was used to test whether V1a receptors modulate neural processing in the maternal brain when dams are exposed to a male intruder. Pri...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2009.06.023
更新日期：2010-01-01 00:00:00
abstract：:We investigated the effect of 5-HT6 receptor subtype activation on glutamatergic transmission by means of whole-cell patch-clamp electrophysiological recordings from medium spiny neurons of the striatum and layer V pyramidal neurons of the prefrontal cortex. To this aim, we took advantage of a novel ligand, ST1936, sh...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2011.05.004
更新日期：2011-09-01 00:00:00
abstract：:N-Methyl-D-aspartate (NMDA) receptors are important CNS target sites of alcohols, but the site and mechanism of action of alcohols on NMDA receptors remains unclear. In CHO-K1 cells transfected with NR1/NR2B NMDA receptor subunits, ethanol inhibited NMDA-activated current with an IC(50) of 138 mM. Truncation of the in...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(00)00067-8
更新日期：2000-07-24 00:00:00
abstract：:The neuronal nicotinic acetylcholine receptor alpha7 (nAChR alpha7) may be involved in cognitive deficits in Schizophrenia and Alzheimer's disease. A fast pharmacological characterization of homomeric alpha7 receptors is mostly hampered by their low functional expression levels in heterologous expression systems. In t...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2004.10.003
更新日期：2005-02-01 00:00:00
abstract：:Long-term memory formation is known to be critically dependent upon de novo gene expression in the brain. As a consequence, pharmacological enhancement of the transcriptional processes mediating long-term memory formation provides a potential therapeutic strategy for cognitive disorders involving aberrant neuroplastic...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.06.043
更新日期：2013-01-01 00:00:00
abstract：:Hypoxic-ischemic encephalopathy (HI) accounts for the majority of developmental, motor and cognitive deficits in children, leading to life-long neurological impairments. Since the plasmamembrane sodium/calcium exchanger (NCX) plays a fundamental role in maintaining ionic homeostasis during adult brain ischemia, in the...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2018.03.017
更新日期：2018-06-01 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：:Autophagy is an intracellular degradation pathway with dynamic interactions for eliminating damaged organelles and protein aggregates by lysosomal digestion. The EGFP-conjugated microtubule-associated protein 1 light chain 3 (EGFP-LC3) serves to monitor autophagic process. Extracellular β-amyloid peptide accumulation ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.02.003
更新日期：2015-06-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(87)90130-4
更新日期：1987-12-01 00:00:00
abstract：:The loci coeruleus of freely moving cats were perfused bilaterally with acetylcholine at a dose of 0.001 microgram/microliter per min, while the animals were recorded polygraphically. The controls consisted of experiments in which no perfusions were done, and experiments in which the loci coeruleus were perfused bilat...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(82)90174-5
更新日期：1982-11-01 00:00:00
abstract：:Postsynaptic induction of long-term potentiation (LTP) at cortical and thalamic afferent synapses onto lateral amygdala (LA) projection neurons not only involves NMDA receptor activation, but also depends on L-type voltage-dependent calcium channels (L-VDCCs). Here we show, using whole cell recordings and two-photon C...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2006.07.010
更新日期：2007-01-01 00:00:00
abstract：:In view of the involvement of noradrenaline (NA) in the regulation of adrenocortical secretion, its role in the rise of plasma corticosterone following neural stimuli was evaluated in rats. The injection of the catecholamine neurotoxin 6-hydroxydopamine (6-OHDA) into the ventral noradrenergic bundle in the brain stem,...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(88)90161-x
更新日期：1988-02-01 00:00:00
abstract：:This study analyzed and compared the effects of EGCG treatment on the expression of NTFs and NTF receptors expression in the sciatic nerve and the L3-L6 spinal cord segments at the early phase of regeneration following sciatic nerve crush injury. Analysis of BDNF, GDNF and NT3 neurotropic factors and Trk-B, Trk-C and ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.10.029
更新日期：2016-03-01 00:00:00
abstract：:Serotonin (5-HT) modulates the hypothalamic-pituitary-adrenal (HPA) axis response to stress. We examined the effect of chronic restraint stress (CRS; 20 min/day) as compared to control (CTRL) conditions for 14 days, on: 1) restraint-induced ACTH and corticosterone (CORT) secretion in rats pretreated with vehicle or SB...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.03.013
更新日期：2013-08-01 00:00:00
abstract：RATIONALE:Diabetes mellitus (DM) is a major risk factor for Alzheimer's disease and vascular dementia. Few animal models exist that focus on the metabolic contributions to dementia onset and progression. Thus, there is strong scientific rationale to explore the effects of streptozotocin (STZ), a diabetogenic compound, ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2018.04.021
更新日期：2018-07-15 00:00:00
abstract：:The demonstrated functional interaction of metabotropic glutamate 5 (mGlu₅) receptors with N-methyl-d-aspartate (NMDA) receptors has prompted speculation that their activation may offer a potential treatment for aspects of schizophrenia. Development of selective mGlu₅ agonists has been difficult, but several different...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.07.030
更新日期：2013-01-01 00:00:00
abstract：:Trazodone is one of the most commonly prescribed medicines for treating depression and insomnia. However, the pharmacological mechanism of action underlying trazodone's unique effects is unclear. Despite its nanomolar affinity for 5HT(2A) receptors, histamine(1) receptors and alpha(1) adrenoceptors the drug is given a...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2007.05.011
更新日期：2007-08-01 00:00:00
abstract：:Trace Amine-Associated Receptor 1 (TAAR1) is a G protein-coupled receptor (GPCR) expressed in several mammalian brain areas and activated by "trace amines" (TAs). TAs role is unknown; however, discovery of their receptors provided an opportunity to investigate their functions. In vivo evidence has indicated an inhibit...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2014.02.007
更新日期：2014-06-01 00:00:00
abstract：:Pain is among the most common symptoms in cancer and approximately 90% of patients experience end-stage cancer pain. The management of cancer pain is challenging due to the significant side effects associated with opioids, and novel therapeutic approaches are needed. MMG22 is a bivalent ligand containing MOR agonist a...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2019.107690
更新日期：2019-12-01 00:00:00
abstract：:Fast rhythmic activity in a frequency range between 20 and 40 Hz occurs in vitro in hippocampal area CA3 after activation of muscarinic receptors. Here we show that carbachol-induced rhythmic activity is modulated by serotonin (5-HT). Spectral analysis reveals that 5-HT (0.3-30 microM) decreases power, but not frequen...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2004.10.011
更新日期：2005-03-01 00:00:00
abstract：:Cannabidiol (CBD), a non-euphorigenic compound derived from Cannabis, shows promise for improving recovery following cerebral ischemia and has recently been shown effective for the treatment of childhood seizures caused by Dravet and Lennox-Gastaut syndromes. Given evidence for activity to mitigate effects of CNS insu...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2019.107716
更新日期：2019-11-01 00:00:00
abstract：:Visual cues that become associated with the consumption of psychostimulant drugs energize craving and the intake of the drug by mechanisms of which little is known. In two experiments using in vivo microdialysis in freely moving rats we compared the effects of visual and auditory stimulation with that of cocaine (0, 5...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2006.10.002
更新日期：2007-03-01 00:00:00
abstract：:Following its binding to somatodendritic receptors, the neuropeptide neurotensin (NT) internalizes via a clathrin-mediated process. In the present study, we investigated whether NT also internalizes presynaptically using synaptosomes from rat neostriatum, a region in which NT1 receptors are virtually all presynaptic. ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(02)00054-0
更新日期：2002-06-01 00:00:00
abstract：:In the current study, we investigated the effect of the activation of the alpha-7 nicotinic acetylcholine receptor (α7 nAchR) on dextran sulphate sodium (DSS)-induced colitis and referred mechanical hyperalgesia in mice. Colitis was induced in CD1 male mice through the intake of 4% DSS in tap water for 7 days. Control...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.06.004
更新日期：2012-10-01 00:00:00
