Abstract:
:Microspectrofluorimetric measurements of excitatory amino acid-evoked rises in intracellular free calcium concentration ([Ca2+]i), electrophysiological measurements of currents through single NMDA receptor-operated ion channels and estimates of cellular viability following NMDA challenge were employed to examine the interactions of (-)- and (+)-beta-cyclazocine with the NMDA receptor-channel complex in cultured rat hippocampal neurons. Rises in [Ca2+]i evoked by NMDA, but not those evoked by kainate, AMPA or 50 mM K+, were reduced by (-)-beta-cyclazocine in a concentration- and use-dependent manner with an estimated IC50 value of 272 nM. In outside-out patches, (-)-beta-cyclazocine did not change the magnitudes of unitary NMDA-evoked currents but diminished both the frequency of channel openings and their mean open time. The IC50 for (-)-beta-cyclazocine against NMDA channel open state probability was estimated at 84 nM. The actions of (-)-beta-cyclazocine were consistent with a voltage-dependent open channel block of the NMDA channel with a blocking rate constant of 7.03.10(7) M-1.s-1 at -40 mV. Neurons exposed to a high concentration of NMDA in vitro were protected from death by 1 and 10 microM (-)-beta-cyclazocine. In all of the above assays, (+)-beta-cyclazocine was considerably less potent an NMDA antagonist and neuroprotective agent than (-)-beta-cyclazocine; the IC50 for (+)-beta-cyclazocine against channel open state probability was estimated at 14 microM. The results demonstrate that (-)-beta-cyclazocine is a potent and selective inhibitor of NMDA-evoked responses in cultured rat hippocampal neurons and an effective neuroprotective agent in vitro.
journal_name
Brain Resjournal_title
Brain researchauthors
Sawyer DC,McLarnon JG,Church Jdoi
10.1016/0006-8993(95)00771-hsubject
Has Abstractpub_date
1995-11-06 00:00:00pages
30-8issue
1-2eissn
0006-8993issn
1872-6240pii
0006-8993(95)00771-Hjournal_volume
698pub_type
杂志文章相关文献
BRAIN RESEARCH文献大全abstract::We have examined the effects of isotonic hypovolemia on the expression of the neuronal nitric oxide synthase (nNOS) gene in the paraventricular (PVN) and supraoptic nuclei (SON) of the rat, using in situ hybridization histochemistry with a 35S-labelled oligodeoxynucleotide probe complementary to nNOS mRNA. Intraperito...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(97)01531-x
更新日期:1998-04-20 00:00:00
abstract::Up to today, the neuronal bases of activating and establishing a memory trace are not well understood. Several findings point towards the idea that the activation of an engram is mirrored in induced oscillatory bursts in the gamma frequency range (> 20 Hz; induced gamma band responses; iGBRs). In the present study, we...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/j.brainres.2006.04.069
更新日期:2006-06-30 00:00:00
abstract::Microinjections of the substance P (SP) antagonist (D-pro2,D-phe7,D-trp9)-SP, or the gamma-aminobutyric acid (GABA) agonist, muscimol, into the entopeduncular nucleus reduced muscle tone in genetically spastic rats in a dose- and time-dependent manner. Similar injections into the ventral thalamus, zona incerta or amyg...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(90)90564-r
更新日期:1990-02-19 00:00:00
abstract::To determine the contribution of presynaptic cholinergic mechanisms to the increased sensitivity of a genetically selected line of Sprague-Dawley rats (Flinders S-line) to the anticholinesterase, diisopropyl fluorophosphate (DFP), rats were sacrificed by focused microwave irradiation of the head 1 min after a pulse in...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(84)91044-8
更新日期:1984-03-05 00:00:00
abstract::Microglial cyclo-oxygenase (COX) expression is considered to be important in the pathogenesis of Alzheimer's disease (AD) and, therefore, constitutes a key target for therapeutic intervention. We investigated the influence of AD plaque associated factors on COX-1 and COX-2 expression and activity in adult human microg...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(02)03164-5
更新日期:2002-10-04 00:00:00
abstract::Previous data suggest a relationship between the loss of response to levodopa in Parkinson's disease (PD) patients with the co-occurrence of dementia, but the role of alterations in the dopamine system has not been explored. We measured the extent of striatal DA loss and changes in striatal DA D(2) and D(3) receptors ...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(02)03396-6
更新日期:2002-11-15 00:00:00
abstract::The microdialysis technique was utilized to study the effects of N-methyl-D-aspartate (NMDA) receptor ligands on the in vivo release of endogenous glutamate (Glu) and aspartate (Asp) from the rat striatum. Addition of NMDA (250 and 500 microM) to the dialysis perfusion solution resulted in a striking dose-dependent in...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(92)91195-k
更新日期:1992-07-10 00:00:00
abstract::These studies examined the microsomal brain metabolism of phencyclidine (PCP) in male and female Sprague-Dawley rats. Several monohydroxylated metabolites of PCP were detected including cis- and trans-1-(1-phenyl-4-hydroxycyclohexyl)piperidine (c-PPC and t-PPC) and 1-(1-phenylcyclohexyl)-4-hydroxypiperidine (PCHP). Th...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(97)00203-5
更新日期:1997-05-09 00:00:00
abstract::Factors underlying paired-pulse facilitation (PPF) were studied by intracellular and field recordings of CA1 neurons in the hippocampal slice in vitro, following stimulation of the Schaffer collaterals apical dendritic afferents. Similar magnitudes of PPF were found using the slopes or peaks of the excitatory postsyna...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(94)90209-7
更新日期:1994-07-04 00:00:00
abstract::Abnormally hyperphosphorylated tau is the major protein component of neurofibrillary tangles, the characteristic lesion of Alzheimer's disease (AD). Protein phosphatases (PP) type 1 (PP-1), type 2A (PP-2A) and type 2B (PP-2B) appear to be involved in the regulation of tau phosphorylation. The incidence of neurofibrill...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(96)00904-3
更新日期:1996-11-25 00:00:00
abstract::Adult male rats, intact (N) or with complete (CHD), anterior (AHD), or posterior (PHD) hypothalamic deafferentations were bilaterally adrenalectomized. At 3, 6, 12 and 20 days post-adrenalectomy they were decapitated and trunk blood was collected for ACTH determinations. In N rats, ACTH markedly elevated up to 850 pg/...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(84)90127-6
更新日期:1984-11-26 00:00:00
abstract::We examined the effect of the molarless condition on the dendritic spines of hippocampal pyramidal cells in SAMP8 mice in comparison to its effect on learning ability in a maze test. The molarless condition caused a decrease in the number of the spines of CA1 pyramidal cells only in the aged mice showing a reduced lea...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/j.brainres.2005.07.038
更新日期:2005-09-28 00:00:00
abstract::Double immunocytochemistry using peroxidase-antiperoxidase and protein A-gold was performed to determine whether neuropeptide Y (NPY) immunoreactive neurons receive synaptic inputs from catecholaminergic axon terminals in the rat neostriatum. Tyrosine hydroxylase-immunoreactive axons were found to be in synaptic conta...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(88)90484-2
更新日期:1988-08-23 00:00:00
abstract::Lesions to the ventromedial hypothalamus (VMH) inhibit receptive sexual behavior in the whiptail lizard, Cnemidophorus uniparens, an all-female species. All lesions to the VMH that effectively abolished receptivity specifically damaged the dorsal lateral VMH, an area containing high concentrations of estrogen receptor...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(95)00191-r
更新日期:1995-05-22 00:00:00
abstract::The bag cell neurons of Aplysia are capable of generating an afterdischarge, which, in vivo, triggers egg-laying behavior. Pharmacologic elevation of cyclic AMP levels in isolated bag cell neurons has been shown to initiate repetitive firming similar to that seen during an afterdischarge, and to decrease outward curre...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(90)91733-w
更新日期:1990-11-05 00:00:00
abstract::The response properties of neurons in the region of striate cortex subserving central retina (0 degrees-2 degrees) and in a region of representation of parafoveal retina (4 degrees-7 degrees) were studied in unanesthetized paralyzed macaque monkeys. Neurons sensitive to the orientation of the stimulus in the visual fi...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(75)90240-1
更新日期:1975-12-12 00:00:00
abstract::Several studies have examined the activity of neurons in hypothalamic tissue slices. The present experiments studied relationships between neuronal activity (firing rate and thermosensitivity) and tissue survival as a function of time and slice thickness. Rat hypothalamic tissue slices were sectioned at different thic...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(97)00671-9
更新日期:1997-11-28 00:00:00
abstract::We cloned the genes for the mouse homologue of the neuromedin B receptor (NMB-R) and the bombesin receptor subtype 3 (BRS-3). Both receptor genes consist of three exons with well-conserved intron-exon borders. Although the NMB-R gene spans more than 10 kb, the BRS-3 gene spans only about 4 kb. Comparison of the mouse ...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(97)00380-6
更新日期:1997-07-11 00:00:00
abstract::Recently, Somberg, in a preliminary report (1983), noted that electrical stimulation of the area postrema causes an increase in coronary vascular resistance. The increase in resistance was mediate by an increase in sympathetic activity as it was counteracted by alpha-adrenergic receptor blockade. The purpose of our st...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(88)91269-3
更新日期:1988-05-17 00:00:00
abstract::Prolonged exposure of opioid receptors to agonists leads to their regulation by the classical process of clathrin-dependent internalization, followed by their intracellular degradation (down regulation). We have previously shown that the opioid agonist etorphine induced an additional process of down regulation of mu-o...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/j.brainres.2011.02.040
更新日期:2011-04-22 00:00:00
abstract::The basic characteristics of the electroencephalograms (EEGs) of the entorhinal cortex (EC) were compared to those of the olfactory bulb (OB) and prepiriform cortex (PPC) in the awake cat, using methods that take into account linear (coherence functions) and non-linear relationships (mutual information). The frequency...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(88)91264-4
更新日期:1988-05-17 00:00:00
abstract::The present study was undertaken to disclose temporal changes in the distribution of Fos-like immunoreactive (-IR) neurons in the trigeminal subnucleus caudalis (SpVc), one of the important relay nuclei for processing the nociceptive information from the oro-facial regions, following induction of experimental tooth mo...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(98)01323-7
更新日期:1999-02-20 00:00:00
abstract::Caspases, a family of cysteine proteases, are widely activated in neurons and glia in the injured brain, a response thought to induce apoptosis. However, caspase activation in astrocytes following injury is not strongly associated with apoptosis. The present study investigates the potential role of caspase activation ...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/j.brainres.2012.02.056
更新日期:2012-04-23 00:00:00
abstract::β-Amyloid peptide (Aβ) plays a central role in the pathogenesis of Alzheimer׳s disease, but in lower amounts it is found in normal brains where it participates in physiological processes and probably regulates synaptic plasticity. This study investigated the effects of physiologically relevant concentrations of Aβ (1 ...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/j.brainres.2014.02.031
更新日期:2014-04-16 00:00:00
abstract::The study makes an attempt to find out the action of norepinephrine (NE) and phenoxybenzamine (PB), applied at medial preoptic area (mPOA), in altering the sleep-awake responses, in free moving rats, which has not yet been reported. Effects of application of NE during day and PB during night, at mPOA, on sleep-awake r...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(84)90125-2
更新日期:1984-11-26 00:00:00
abstract::The present study was designed to investigate the role of activation of Kca+2 channels and cAMP in opioid-induced pial artery dilation in newborn pigs equipped with closed cranial windows. Methionine enkephalin, an endogenous mu agonist, elicited dilation that was modestly attenuated by the Kca+2 channel antagonist, i...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/s0006-8993(96)01284-x
更新日期:1997-02-07 00:00:00
abstract::To test the hypothesis that neurons in the hypothalamic paraventricular nucleus (PVN) may be under both direct and indirect regulation by alpha melanocyte-stimulating hormone (alpha-MSH)-synthesizing neurons of the arcuate nucleus, we determined whether the retrogradely transported marker substance, cholera toxin beta...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/j.brainres.2005.09.023
更新日期:2005-12-07 00:00:00
abstract::Neovascularization within syngeneic rat fetal neocortical grafts transplanted into a previously prepared cavity in the cerebral cortex was studied 1 to 3 months after transplantation, utilizing scanning electron microscopy of vascular corrosion casts. The grafts were easily identified and the outer surface of the graf...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(95)00304-9
更新日期:1995-05-29 00:00:00
abstract::In adult cats, we have investigated how nerve cross-union between slow and fast muscle affects twitch contraction and half-relaxation times in the presence and absence of motor disuse, produced by complete decerebellation. Cerebellectomy abolished the slowing of cross-innervated fast muscle and diminished the amount o...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(82)90480-2
更新日期:1982-02-18 00:00:00
abstract::A possible role for neuropeptides in affective disorders is suggested by many investigators. Somatostatin-like immunoreactivity (SS-LI) and neuropeptide Y-like immunoreactivity (NPY-LI) concentrations are demonstrated to be reduced in cerebrospinal fluid from depressed patients. We have shown that long-term treatment ...
journal_title:Brain research
pub_type: 杂志文章
doi:10.1016/0006-8993(92)90850-9
更新日期:1992-12-18 00:00:00