Quantitative autoradiographic analysis of the new radioligand [(3)H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid ([(3)H]NCS-382) at gamma-hydroxybutyric acid (GHB) binding sites in rat brain.

Abstract:

:(2E)-(5-Hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid (NCS-382) is an antagonist for gamma-hydroxybutyric acid (GHB) at GHB receptor sites. Advantages of using [(3)H]NCS-382 over [(3)H]GHB in radioligand binding studies are that unlike GHB, NCS-382 does not appear to bind to, activate, or interfere with the functioning of GABA(B) or GABA(A) receptors, either directly or indirectly. Herein we establish a protocol for use of [(3)H]NCS-382 by quantitative autoradiography. GHB was used to define non-specific binding, since it displaced [(3)H]NCS-382 to an extent equivalent to NCS-382. Among many areas of brain examined, two regions in which high specific binding of [(3)H]NCS-382 occurred were the hippocampus and cerebral cortex. Areas such as the striatum and nucleus accumbens exhibited intermediate levels of specific binding. No or very low binding was observed in other areas such as the cerebellum and dorsal raphe nucleus. The distribution of GHB binding sites as defined by [(3)H]NCS-382 suggests that GHB may play a role in neuromodulation or neurotransmission in frontal brain areas.

journal_name

Brain Res

journal_title

Brain research

authors

Gould GG,Mehta AK,Frazer A,Ticku MK

doi

10.1016/s0006-8993(03)02865-8

subject

Has Abstract

pub_date

2003-07-25 00:00:00

pages

51-6

issue

1-2

eissn

0006-8993

issn

1872-6240

pii

S0006899303028658

journal_volume

979

pub_type

杂志文章
  • Neurotensin receptor localization by light microscopic autoradiography in rat brain.

    abstract::Neurotensin is a putative peptide neurotransmitter in the mammalian brain. The light microscopic localization of the neurotensin receptor has been carried out by the autoradiographic localization of [3H]neurotensin binding sites in slide-mounted tissue sections. Large variations in receptor distribution were found, ev...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(81)90532-1

    authors: Young WS 3rd,Kuhar MJ

    更新日期:1981-02-16 00:00:00

  • Thirteen-month inhibition of aldose reductase by zenarestat prevents morphological abnormalities in the dorsal root ganglia of streptozotocin-induced diabetic rats.

    abstract::The dorsal root ganglia (DRG) have been identified as the target tissue in diabetic somatosensory neuropathy. It has been reported that, in the chronically diabetic state, DRG sensory neurons may undergo morphological changes. In this study, we examined the effect of zenarestat, an aldose reductase inhibitor, on the m...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2008.10.018

    authors: Shimoshige Y,Minoura K,Matsuoka N,Takakura S,Mutoh S,Kamijo M

    更新日期:2009-01-09 00:00:00

  • Effects of PKC and PKA phosphorylation on desensitization of nicotinic acetylcholine receptors.

    abstract::The present study was designed to assess the effect of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA) on desensitization of Torpedo acetylcholine (ACh) receptors by analyzing summated macroscopic currents in an outside-out patch-clamp configuration. Normal ACh receptors desensitized with a fast (6 ms) ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/s0006-8993(98)00836-1

    authors: Nishizaki T,Sumikawa K

    更新日期:1998-11-23 00:00:00

  • Imipramine inhibits intrathecal substance P-induced behavior and blocks spinal cord substance P receptors in mice.

    abstract::The mechanism of the antinociceptive effect of the tricyclic antidepressant imipramine was investigated in mice. Intrathecal (i.t.) administration of imipramine produced dose-dependent antinociception in the tail-pinch and tail-flick tests with ED50 values (95% confidence limit) of 27.5 (17.0-43.9) and 20.2 (12.6-32.2...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(92)90344-9

    authors: Iwashita T,Shimizu T

    更新日期:1992-05-22 00:00:00

  • Dynamic single unit simulation of a realistic cerebellar network model. II. Purkinje cell activity within the basic circuit and modified by inhibitory systems.

    abstract::In continuation of earlier computer simulation studies 15 of the feedback inhibition exercised by the Golgi cells of the cerebellum, an attempt is made at modeling the behavior of Purkinje and basket cells under somewhat more complex functional circumstances. The simulation study is based on a realistic network model ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(74)90531-9

    authors: Pellionisz A,Szentàgothai J

    更新日期:1974-03-15 00:00:00

  • Sex-dependent and region-specific changes in TrkB signaling in BDNF heterozygous mice.

    abstract::Altered expression of neurotrophins may contribute to the pathogenesis of schizophrenia. Several studies suggest sex steroid hormones may be involved in the regulation of brain-derived neurotrophic factor (BDNF) signaling, as well as the symptoms of schizophrenia. This study aimed to identify sex differences in BDNF-T...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2011.01.060

    authors: Hill RA,van den Buuse M

    更新日期:2011-04-12 00:00:00

  • (+)-6,7-benzomorphan sigma ligands stimulate dopamine synthesis in rat corpus striatum tissue.

    abstract::The benzomorphan sigma ligands, (+)-N-allylnormetazocine (NANM) and (+)-pentazocine, but not (+)-cyclazocine, stereospecifically stimulated dopamine synthesis in minces of rat corpus striatum by 15-23% over basal values at 0.1-1.0 microM. The effect of (+)-NANM and (+)-pentazocine was blocked by the reported sigma ant...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(91)90159-s

    authors: Booth RG,Baldessarini RJ

    更新日期:1991-08-23 00:00:00

  • Simulation of cerebral hemodynamics for preoperative risk assessment.

    abstract:BACKGROUND:An important part of the medical treatment of many cerebrovascular diseases is the occlusion of brain supplying arteries. Until now, the risk of this intervention can only be estimated by invasive diagnostics including the risk of cerebrovascular accidents. METHODS AND RESULTS:As a supporting tool, a comput...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2006.08.021

    authors: Roessler FC,Reith W,Siegel G

    更新日期:2006-11-06 00:00:00

  • Effects of angiotensin II on dopamine and serotonin turnover in the striatum of conscious rats.

    abstract::This study was designed to evaluate the functional significance of angiotensin II (Ang II) receptors identified by previous receptor autoradiography studies to be located presynaptically on terminals of dopaminergic neurones projecting to the striatum. Microdialysis was performed in the striatum of conscious freely mo...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(93)90902-y

    authors: Mendelsohn FA,Jenkins TA,Berkovic SF

    更新日期:1993-06-11 00:00:00

  • Aquaporin-4 immunoreactivity in Müller and amacrine cells of marine teleost fish retina.

    abstract::Aquaporins (AQPs) are membrane proteins that facilitate water transport across biological membranes and are essential for the proper function of neural tissue. Although AQPs have been extensively studied in mammalian retina, their presence in lower vertebrate retina is less frequently characterized. AQP4 expressed in ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2011.11.014

    authors: Hombrebueno JR,Lee EJ,Martínez-Ruiz N,García-Alcázar A,Grzywacz NM,De Juan J

    更新日期:2012-01-13 00:00:00

  • Effects of bicuculline on receptive field center sensitivity of relay cells in the lateral geniculate nucleus.

    abstract::The lateral geniculate nucleus (LGN) receives input from the retina that is spatially organized into a receptive-field center and surround. It maintains this organization in the signal that it sends to the visual cortex. Previous studies have focused on changes in the receptive-field 'surround' that are generated at t...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(89)90728-2

    authors: Norton TT,Holdefer RN,Godwin DW

    更新日期:1989-05-29 00:00:00

  • Long-term effects of early social isolation in Macaca mulatta: changes in dopamine receptor function following apomorphine challenge.

    abstract::The hypothesis that early social isolation results in long-term alterations in dopamine receptor sensitivity was tested using older adult rhesus monkeys. Isolated and control monkeys were challenged with apomorphine (0.1 and 0.3 mg/kg), and the drug effects on spontaneous blink rate, stereotyped behavior, and self-inj...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(90)91089-y

    authors: Lewis MH,Gluck JP,Beauchamp AJ,Keresztury MF,Mailman RB

    更新日期:1990-04-09 00:00:00

  • The effect of elevated potassium on the adult mollusc giant neurone survival and neurite formation in culture.

    abstract::The number of viable neurones calculated as soon as adult mollusc ganglia tissue was digested and over different periods of cultivation, show that elevated K+ prevents degradation of intercellular contacts, preserves neurones against lysis, prolongs the time course of neurone survival in culture and inhibits neurite f...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(82)90044-0

    authors: Kostenko MA,Tretjak NN,Musienko VS

    更新日期:1982-03-18 00:00:00

  • Normal levels of histamine and tele-methylhistamine in mast cell-deficient mouse brain.

    abstract::To determine the contribution by mast cells to the brain content of histamine (HA) and its metabolite tele-methylhistamine (t-MH), the number of mast cells, as well as the levels of HA and t-MH were measured in brain regions of mast cell-deficient (W/Wv) and control (+/+) mice. In agreement with earlier studies, mast ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(84)90897-7

    authors: Hough LB,Khandelwal JK,Goldschmidt RC,Diomande M,Glick SD

    更新日期:1984-01-30 00:00:00

  • Cerebroprotective effects of TAK-937, a novel cannabinoid receptor agonist, in permanent and thrombotic focal cerebral ischemia in rats: therapeutic time window, combination with t-PA and efficacy in aged rats.

    abstract::Some occluded arteries of acute ischemic stroke (AIS) patients are not recanalized, even if thrombolytic therapy is performed. Considering such clinical settings, we examined the potential cerebroprotective efficacy of TAK-937, a novel cannabinoid receptor agonist, in young adult and aged rats with a permanent middle ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2013.06.014

    authors: Murakami K,Suzuki M,Suzuki N,Hamajo K,Tsukamoto T,Shimojo M

    更新日期:2013-08-14 00:00:00

  • Sex differences in the dendritic branching of dentate granule cells following differential experience.

    abstract::Male and female hooded rats were raised from weaning in either a complex or an isolated environment in two separate replications. After one month, the brains were Golgi-Cox stained and dendritic fields of dentate gyrus granule cells were quantified. There was a sex difference in response to the environment. Females ra...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(85)90125-8

    authors: Juraska JM,Fitch JM,Henderson C,Rivers N

    更新日期:1985-04-29 00:00:00

  • Vitamin B₁₂ dependent changes in mouse spinal cord expression of vitamin B₁₂ related proteins and the epidermal growth factor system.

    abstract::Chronic vitamin B12 (cobalamin) deficiency in the mammalian central nervous system causes degenerative damage, especially in the spinal cord. Previous studies have shown that cobalamin status alters spinal cord expression of epidermal growth factor (EGF) and its receptor in rats. Employing a mouse model of cobalamin-d...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2013.01.050

    authors: Mutti E,Lildballe DL,Kristensen L,Birn H,Nexo E

    更新日期:2013-03-29 00:00:00

  • Effect of noxious somesthetic stimulation on the activity of neurons of the nucleus centralis of the amygdala.

    abstract::Neurons (n = 107) were recorded, in anaesthetized rats, with extracellular micropipettes, in the nucleus centralis of the amygdala (Ce). The activity of a large majority (77%) was exclusively or preferentially affected by noxious stimuli applied in any area of the body. The rest of the neurons was not activated by any...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(90)91512-f

    authors: Bernard JF,Huang GF,Besson JM

    更新日期:1990-07-23 00:00:00

  • Ultrastructural localization of inhibin beta- and somatostatin-28-immunoreactivities in the paraventricular and supraoptic nuclei.

    abstract::Recent studies have supported the existence of projections to the paraventricular and supraoptic nuclei of the hypothalamus that arise from non-catecholaminergic neurons in the nucleus of the solitary tract, whose terminal distribution is suggestive of interactions with both parvocellular and magnocellular neurosecret...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(95)00760-n

    authors: Sawchenko PE,Pfeiffer SW

    更新日期:1995-10-02 00:00:00

  • MicroRNA let-7c-5p improves neurological outcomes in a murine model of traumatic brain injury by suppressing neuroinflammation and regulating microglial activation.

    abstract::MicroRNAs (miRNAs) are a class of non-coding small RNAs that regulate the expression of target genes. They derive from pre-miRNAs that are enzymatically processed by dicer to ∼22 nucleotide mature miRNAs. Members of the pre-miRNA lethal-7 (let-7) are known to regulate cell proliferation and apoptosis. Here, we showed ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2018.01.032

    authors: Lv J,Zeng Y,Qian Y,Dong J,Zhang Z,Zhang J

    更新日期:2018-04-15 00:00:00

  • Analysis of fast axoplasmic transport in nerve ligation and adriamycin-induced neuronal perikaryon lesions.

    abstract::Fast axoplasmic transport was examined in experimental nerve ligation and adriamycin-induced neuronal perikaryon lesions. Animals were sacrificed at precisely 3 and 4 h following the injection of [3H]leucine. In single ligated nerves, the 3 and 4 h down-flow rates, which include the time for neuronal processing of lab...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(79)90730-3

    authors: Sahenk Z,Mendell JR

    更新日期:1979-07-27 00:00:00

  • Neuron-specific enolase-like immunoreactivity in inner hair cells but not outer hair cells in the guinea pig organ of Corti.

    abstract::Neuron-specific enolase (NSE) has been localized only in neurons and cells with characteristics of neurons. The immunocytochemical localization of NSE was examined in guinea pig cochleae to determine if hair cells, which have some neuronal characteristics, would show NSE-like immunoreactive labeling. NSE-like immunore...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(85)91541-0

    authors: Altschuler RA,Reeks KA,Marangos PJ,Fex J

    更新日期:1985-02-18 00:00:00

  • L-type calcium channels modulate glutamate-driven bursting activity in the nucleus accumbens in vivo.

    abstract::The majority of adult nucleus accumbens medium spiny neurons exhibit a bistable membrane potential that fluctuates between a relatively hyperpolarized (Down) state (average=-76 mV) and a less hyperpolarized (Up) state (average=-60 mV) near firing threshold. During in vivo extracellular recordings from nucleus accumben...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/s0006-8993(00)02868-7

    authors: Cooper DC,White FJ

    更新日期:2000-10-13 00:00:00

  • Recovery of regenerating goldfish retinal ganglion cells is slowed in the absence of the topographically correct synaptic target.

    abstract::When the axons of goldfish retinal ganglion cells are severed the cell bodies undergo a series of changes as the axons regenerate. These changes begin to reverse when the axons start to innervate the tectum and by 3 months after the lesion the cell bodies have nearly returned to normal. When the axons projecting to th...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(87)90824-9

    authors: Burmeister DW,Dunn-Meynell AA

    更新日期:1987-10-13 00:00:00

  • Peripheral nerve injury alters the expression of NF-κB in the rat's hippocampus.

    abstract::The hippocampus plays an important role in learning and memory and possibly contributes to the formation of pain-related memory and emotional responses. However, there is currently little data linking the hippocampus to neuropathic pain. It has been reported that NF-κB is an important regulatory factor in memory conso...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2011.01.006

    authors: Chou CW,Wong GT,Lim G,McCabe MF,Wang S,Irwin MG,Mao J

    更新日期:2011-03-10 00:00:00

  • Neurodegeneration in autoimmune MRL-lpr mice as revealed by Fluoro Jade B staining.

    abstract::As in many humans suffering from lupus erythematosus, the development of systemic autoimmunity and inflammation in Fas-deficient MRL-lpr mice is accompanied by CNS dysfunction of unknown etiology. Experimental studies revealed infiltration of lymphoid cells into the choroid plexus, reduced neuronal complexity, retarde...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/s0006-8993(02)03980-x

    authors: Ballok DA,Millward JM,Sakic B

    更新日期:2003-02-28 00:00:00

  • Selective impairment of declarative memory following stimulation of dentate gyrus granule cells: a naloxone-sensitive effect.

    abstract::Albino rats received 10 s of sub-seizure electrical stimulation applied to the dentate gyrus granule cells immediately after acquisition of information on trial 1 of a 2-trial radial maze spatial memory task. Granule cell stimulation selectively reduced the probability of accessing information held in declarative memo...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(84)90166-5

    authors: Collier TJ,Routtenberg A

    更新日期:1984-09-24 00:00:00

  • Enkephalin-like immunoreactivity levels increase in the motor nucleus after an intramedullar axotomy of motoneurons in the adult cat spinal cord.

    abstract::Neuropeptide- and serotonin-like immunoreactivities were studied in the lumbar spinal cord of the cat after a longitudinal incision in the ventral funiculus. This lesion, which accomplishes a central axotomy of motoneurons, was accompanied by increased level of Met-enkephalin-like immunoreactivity in nerve endings in ...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(90)90157-7

    authors: Lindå H,Cullheim S,Risling M,Arvidsson U,Mossberg K,Ulfhake B,Terenius L,Hökfelt T

    更新日期:1990-11-26 00:00:00

  • Antidiabetic sulfonylureas: localization of binding sites in the brain and effects on the hyperpolarization induced by anoxia in hippocampal slices.

    abstract::The distribution of antidiabetic sulfonylurea [( 3H]glibenclamide) binding sites is heterogeneous in rat brain. Pyramidal and extrapyramidal motor system contain the highest densities of sites, particularly in the substantia nigra and in the globus pallidus. Only low levels are present in the hypothalamic nuclei and t...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/0006-8993(89)91288-2

    authors: Mourre C,Ben Ari Y,Bernardi H,Fosset M,Lazdunski M

    更新日期:1989-05-01 00:00:00

  • Chronic treatment with fibrates elevates superoxide dismutase in adult mouse brain microvessels.

    abstract::Fibrates are activators of peroxisome proliferator-activated receptor (PPAR) α. Pretreatment with fibrates has been shown to protect brain against ischemia in mice. We hypothesized that fibrates elevate superoxide dismutase (SOD) levels in the brain microvessels (BMVs). BMVs were isolated from male C57BL/6 and PPARα n...

    journal_title:Brain research

    pub_type: 杂志文章

    doi:10.1016/j.brainres.2010.08.075

    authors: Wang G,Liu X,Guo Q,Namura S

    更新日期:2010-11-04 00:00:00