当前位置： SCI文献检索 > JOURNAL OF NEUROCHEMISTRY期刊下所有文献 > A trifluoromethylphenyl piperazine derivative with high affinity for 5-hydroxytryptamine-1A sites in rat brain.

A trifluoromethylphenyl piperazine derivative with high affinity for 5-hydroxytryptamine-1A sites in rat brain.

Abstract：

:The inhibition of [3H]5-hydroxytryptamine [( 3H]5-HT) binding in rat brain by 1-[2-(3-bromoacetamidophenyl)ethyl]-4-(3-trifluoromethylphenyl) piperazine (BrAcTFMPP) and that by spiperone were compared. Spiperone inhibition of [3H]5-HT binding in cortex was consistent with displacement from two sites with dissociation constants (KD) of 24 nM (5-HT-1A site) and 19 microM (5-HT-1B site) for spiperone. BrAcTFMPP also discriminated two subpopulations of [3H]5-HT binding sites with dissociation constants of 0.5 nM and 146 nM for the compound. The proportion of high-affinity sites for each compound represented about 35% of the specific [3H]5-HT binding. In the presence of 1 microM spiperone, a concentration that saturates the 5-HT-1A sites while having a minimal effect on 5-HT-1B sites, BrAcTFMPP displaced [3H]5-HT from a single site with a KD for BrAcTFMPP of 145 nM. The inhibition of [3H]5-HT binding by spiperone in the presence of 30 nM BrAcTFMPP was best fit by a single-site model with a KD of 21 microM for spiperone. In corpus striatum, 5-HT-1A sites, as defined with spiperone, represented 15% of the specific [3H]5-HT binding and 30 nM BrAcTFMPP also blocked about 15% of the binding. A significant difference between spiperone and BrAcTFMPP was their affinity for 5-HT-2 receptors. BrAcTFMPP (KD = 41 nM) had an 80-fold lower affinity for these sites than spiperone (KD = 0.5 nM). Thus, BrAcTFMPP and spiperone discriminate the same two subpopulations of [3H]5-HT binding sites and BrAcTFMPP displays a high affinity and a selectivity for 5-HT-1A sites versus both 5-HT-1B and 5-HT-2 sites.

journal_name

J Neurochem

journal_title

Journal of neurochemistry

authors

Ransom RW,Asarch KB,Shih JC

doi

10.1111/j.1471-4159.1985.tb12897.x

subject

Has Abstract

pub_date

1985-03-01 00:00:00

pages

875-80

issue

3

eissn

0022-3042

issn

1471-4159

journal_volume

44

pub_type

杂志文章

相关文献

JOURNAL OF NEUROCHEMISTRY文献大全
  • Mutagenesis of rat dopamine beta-hydroxylase: examination in cell-free system.

    abstract：:Dopamine beta-hydroxylase (DBH; EC 1.14.17.1) exists as membrane-bound and soluble forms in neurosecretory vesicles. The features of DBH required for glycosylation and incorporation into membranes were studied in a cell-free system. Translation of full-length DBH with microsomal membranes generated two glycosylated pr...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.1995.64010025.x

    authors： Feng Z,Sabban EL

    更新日期：1995-01-01 00:00:00

  • Stapling of the botulinum type A protease to growth factors and neuropeptides allows selective targeting of neuroendocrine cells.

    abstract：:Precise cellular targeting of macromolecular cargos has important biotechnological and medical implications. Using a recently established 'protein stapling' method, we linked the proteolytic domain of botulinum neurotoxin type A (BoNT/A) to a selection of ligands to target neuroendocrine tumor cells. The botulinum pro...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.12284

    authors： Arsenault J,Ferrari E,Niranjan D,Cuijpers SA,Gu C,Vallis Y,O'Brien J,Davletov B

    更新日期：2013-07-01 00:00:00

  • A novel presenilin-2 splice variant in human Alzheimer's disease brain tissue.

    abstract：:Mutations in the presenilin-1 (PS-1) and presenilin-2 (PS-2) genes account for the majority of cases of early-onset familial Alzheimer's disease (AD). Alternative splicing forms of the PS-1 and PS-2 gene products have previously been reported in fibroblast and brain tissue from both familial and sporadic AD patients, ...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.1999.0722498.x

    authors： Sato N,Hori O,Yamaguchi A,Lambert JC,Chartier-Harlin MC,Robinson PA,Delacourte A,Schmidt AM,Furuyama T,Imaizumi K,Tohyama M,Takagi T

    更新日期：1999-06-01 00:00:00

  • Choline acetyltransferase activity and total protein content in selected optic areas of the rat after complete light-deprivation during CNS development.

    abstract：:Choline acetyltransferase (acetyl-CoA: choline O-acetyltransferase, I.U.B. 2.3.1.6) activity and total protein content in visual and extra-visual areas were compared in normal Long-Evans rats and in rats subjected to complete light-deprivation for 21 days from birth. The enzyme activity and the protein content in the ...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.1968.tb10323.x

    authors： Maletta GJ,Timiras PS

    更新日期：1968-08-01 00:00:00

  • Identification of the plasma membrane proteolipid protein as a constituent of brain coated vesicles and synaptic plasma membrane.

    abstract：:We have analyzed brain coated vesicles and synaptic plasma membrane for the presence of the plasma membrane proteolipid protein. Coated vesicles were isolated from calf brain gray matter with a final purification on Sephacryl S-1000 and reisolated twice by chromatography to ensure homogeneity. Fractions were analyzed ...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.1988.tb01829.x

    authors： Sapirstein VS,Nolan C,Stern R,Ciocci M,Masur SK

    更新日期：1988-09-01 00:00:00

  • Splicing of a regulated exon reveals additional complexity in the axonal microtubule-associated protein tau.

    abstract：:Tau is a microtubule-associated protein whose transcript undergoes complex regulated splicing in the mammalian nervous system. Exon 6 of the gene is an alternatively spliced cassette whose expression pattern and splicing regulation had not been previously analyzed in the human. The expression profile of exon 6 is comp...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.1998.70041346.x

    authors： Wei ML,Andreadis A

    更新日期：1998-04-01 00:00:00

  • Functional expression of rat ABCG2 on the luminal side of brain capillaries and its enhancement by astrocyte-derived soluble factor(s).

    abstract：:The purpose of the present study was to clarify the expression, transport properties and regulation of ATP-binding cassette G2 (ABCG2) transporter at the rat blood-brain barrier (BBB). The rat homologue of ABCG2 (rABCG2) was cloned from rat brain capillary fraction. In rABCG2-transfected HEK293 cells, rABCG2 was detec...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.2004.02537.x

    authors： Hori S,Ohtsuki S,Tachikawa M,Kimura N,Kondo T,Watanabe M,Nakashima E,Terasaki T

    更新日期：2004-08-01 00:00:00

  • Arachidonic acid increases choline acetyltransferase activity in spinal cord neurons through a protein kinase C-mediated mechanism.

    abstract：:Arachidonic acid (AA) plays an important role as a signaling factor in the CNS. Therefore, exposure to AA may affect cholinergic neurons in the spinal cord. To test this hypothesis, mRNA expression and activity of choline acetyltransferase (ChAT) was measured in cultured spinal cord neurons treated with increasing con...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.2004.02535.x

    authors： Chalimoniuk M,King-Pospisil K,Pedersen WA,Malecki A,Wylegala E,Mattson MP,Hennig B,Toborek M

    更新日期：2004-08-01 00:00:00

  • Parallel up-regulation of catecholamine biosynthetic enzymes by dexamethasone in PC12 cells.

    abstract：:We sought to investigate whether dexamethasone produces a coordinated, time-dependent effect on all enzymes in the catecholamine biosynthetic pathway in PC12 cells. The levels of mRNAs of tyrosine hydroxylase (TH), aromatic L-amino acid decarboxylase (AADC), and dopamine beta-hydroxylase (DBH) were examined at 0, 6, 1...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.1993.tb03241.x

    authors： Kim KT,Park DH,Joh TH

    更新日期：1993-03-01 00:00:00

  • Characterization of amyloid beta peptides from brain extracts of transgenic mice overexpressing the London mutant of human amyloid precursor protein.

    abstract：:Alzheimer's disease (AD) is marked by the presence of neurofibrillary tangles and amyloid plaques in the brain of patients. To study plaque formation, we report on further quantitative and qualitative analysis of human and mouse amyloid beta peptides (Abeta) from brain extracts of transgenic mice overexpressing the Lo...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.2003.01556.x

    authors： Pype S,Moechars D,Dillen L,Mercken M

    更新日期：2003-02-01 00:00:00

  • Repair gene O6 -methylguanine-DNA methyltransferase is controlled by SP1 and up-regulated by glucocorticoids, but not by temozolomide and radiation.

    abstract：:Therapy of malignant glioma relies on treatment with the O6 -methylating agent temozolomide (TMZ) concomitant with ionizing radiation followed by adjuvant TMZ. For the treatment of recurrences, DNA chloroethylating drugs are also used. The main killing lesion induced by these drugs is O6 -alkylguanine. Since this dama...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.14262

    authors： Aasland D,Reich TR,Tomicic MT,Switzeny OJ,Kaina B,Christmann M

    更新日期：2018-01-01 00:00:00

  • Mortality, oxidative stress and tau accumulation during ageing in parkin null mice.

    abstract：:Young parkin null (pk-/-) mice have subtle abnormalities of behaviour, dopamine (DA) neurotransmission and free radical production, but no massive loss of DA neurons. We investigated whether these findings are maintained while ageing. Pk-/- mice have reduced life span and age-related reduced exploratory behaviour, abn...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.2007.04762.x

    authors： Rodríguez-Navarro JA,Casarejos MJ,Menéndez J,Solano RM,Rodal I,Gómez A,Yébenes JG,Mena MA

    更新日期：2007-10-01 00:00:00

  • Combined treatment with the histone deacetylase inhibitor LBH589 and a splice-switch antisense oligonucleotide enhances SMN2 splicing and SMN expression in Spinal Muscular Atrophy cells.

    abstract：:Spinal muscular atrophy (SMA) is a motor neuron disease caused by loss of function mutations in the Survival Motor Neuron 1 (SMN1) gene and reduced expression of the SMN protein, leading to spinal motor neuron death, muscle weakness and atrophy. Although humans harbour the highly homologous SMN2 gene, its defective sp...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.14935

    authors： Pagliarini V,Guerra M,Di Rosa V,Compagnucci C,Sette C

    更新日期：2020-04-01 00:00:00

  • Temporal profile and cell subtype distribution of activated caspase-3 following experimental traumatic brain injury.

    abstract：:This study investigated the temporal expression and cell subtype distribution of activated caspase-3 following cortical impact-induced traumatic brain injury in rats. The animals were killed and examined for protein expression of the proteolytically active subunit of caspase-3, p18, at intervals from 6 h to 14 days af...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.2000.0751264.x

    authors： Beer R,Franz G,Srinivasan A,Hayes RL,Pike BR,Newcomb JK,Zhao X,Schmutzhard E,Poewe W,Kampfl A

    更新日期：2000-09-01 00:00:00

  • A validated quantitative method for the assessment of neuroprotective barrier impairment in neurodegenerative disease models.

    abstract：:The blood-brain barrier (BBB) and blood-spinal cord barrier (BSCB) are highly specialized structures that limit molecule entry from the blood and maintain homeostasis within the central nervous system (CNS). BBB and BSCB breakdown are associated with multiple neurodegenerative diseases. Given the key role of neuroprot...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.15119

    authors： Kumar V,Lee JD,Coulson EJ,Woodruff TM

    更新日期：2020-07-06 00:00:00

  • Brain beta-spectrin phosphorylation: phosphate analysis and identification of threonine-347 as a heparin-sensitive protein kinase phosphorylation site.

    abstract：:Phosphorylation of brain spectrin was studied by a combination of in vivo and in vitro approaches. Chemical analysis of phosphate groups on electrophoretically purified mouse brain beta-spectrin yielded a stoichiometry of 3.2 +/- 0.18 mol of PO4/mol of beta-spectrin. The spectrin isolated by chromatographic methods fr...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.1998.71052220.x

    authors： Sihag RK

    更新日期：1998-11-01 00:00:00

  • Low activity of angiotensin-converting enzyme in cerebral microvessels of young spontaneously hypertensive rats.

    abstract：:Angiotensin-converting enzyme (ACE) activity was measured in microvessels prepared from cerebral cortices of 4-week-old spontaneously hypertensive rats (SHR). The Vmax value of the ACE activity in the cerebral microvessels of SHR was lower than that of Wistar Kyoto controls of the same age by 25% without difference in...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.1985.tb08761.x

    authors： Kobayashi H,Wada A,Izumi F,Take K,Magnoni MS

    更新日期：1985-04-01 00:00:00

  • Frame-shifted amyloid precursor protein found in Alzheimer's disease and Down's syndrome increases levels of secreted amyloid beta40.

    abstract：:Frame-shifted amyloid precursor protein (APP(+1)), which has a truncated out-of-frame C-terminus, accumulates in the neuropathological hallmarks of patients with Alzheimer's disease pathology. To study a possible involvement of APP(+1) in the pathogenesis of Alzheimer's disease, we expressed APP695 and APP(+1) in the ...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.2004.02528.x

    authors： van Dijk R,Fischer DF,Sluijs JA,Sonnemans MA,Hobo B,Mercken L,Mann DM,Hol EM,van Leeuwen FW

    更新日期：2004-08-01 00:00:00

  • Essential role for integrin linked kinase in Akt-mediated integrin survival signaling in hippocampal neurons.

    abstract：:Activation of integrin receptors in neurons can promote cell survival and synaptic plasticity, but the underlying signal transduction pathway(s) is unknown. We report that integrin signaling prevents apoptosis of embryonic hippocampal neurons by a mechanism involving integrin-linked kinase (ILK) that activates Akt kin...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.2003.01579.x

    authors： Gary DS,Milhavet O,Camandola S,Mattson MP

    更新日期：2003-02-01 00:00:00

  • High-field proton magnetic resonance spectroscopy of a swine model for axonal injury.

    abstract：:A miniature swine model for diffuse brain injury has recently been developed that replicates the inertial loading conditions associated with rotational acceleration during automotive accidents. The swine model induces diffuse axonal pathology without macroscopic injury such as contusions and hematomas, thus affording ...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.1998.70052038.x

    authors： Cecil KM,Lenkinski RE,Meaney DF,McIntosh TK,Smith DH

    更新日期：1998-05-01 00:00:00

  • Alternative polyadenylation and miR-34 family members regulate tau expression.

    abstract：:Tau pathologically aggregates in Alzheimer's disease, and evidence suggests that reducing tau expression may be safe and beneficial for the prevention or treatment of this disease. We sought to examine the role of the 3'-untranslated region (3'-UTR) of human tau mRNA in regulating tau expression. Tau expresses two 3'-...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.12437

    authors： Dickson JR,Kruse C,Montagna DR,Finsen B,Wolfe MS

    更新日期：2013-12-01 00:00:00

  • Neuroactive steroid levels in plasma and cerebrospinal fluid of male multiple sclerosis patients.

    abstract：:Neuroactive steroid family includes molecules synthesized in peripheral glands (i.e., hormonal steroids) and directly in the nervous system (i.e., neurosteroids) which are key regulators of the nervous function. As already reported in clinical and experimental studies, neurodegenerative diseases affect the levels of n...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.12745

    authors： Caruso D,Melis M,Fenu G,Giatti S,Romano S,Grimoldi M,Crippa D,Marrosu MG,Cavaletti G,Melcangi RC

    更新日期：2014-08-01 00:00:00

  • Therapeutic approaches in Parkinson's disease and related disorders.

    abstract：:The lack of effective therapies for neurodegenerative disorders is one of the most relevant challenges of this century, considering that, as the global population ages, the incidence of these type of diseases is quickly on the rise. Among these disorders, synucleinopathies, which are characterized by the abnormal accu...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章,评审

    doi：10.1111/jnc.13529

    authors： Valera E,Masliah E

    更新日期：2016-10-01 00:00:00

  • Glutamate receptor subunit expression in primary neuronal and secondary glial cultures.

    abstract：:We report on the expression of ionotropic glutamate receptor subunits in primary neuronal cultures from rat cortex, hippocampus and cerebellum and of metabotropic glutamate (mGlu) receptor subtypes in these neuronal cultures as well as in cortical astroglial cultures. We found that the NMDA receptor (NR) subunits NR1,...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.2001.00369.x

    authors： Janssens N,Lesage AS

    更新日期：2001-06-01 00:00:00

  • Neuroprotection of immortalized hippocampal neurones by brain-derived neurotrophic factor and Raf-1 protein kinase: role of extracellular signal-regulated protein kinase and phosphatidylinositol 3-kinase.

    abstract：:We have investigated the molecular mechanisms of neurotrophin-mediated cell survival in HT22 cells, a murine cell line of hippocampal origin, expressing the brain-derived neurotrophic factor (BDNF) receptor TrkB as well as the TrkB.T1 splice variant. Stimulation with BDNF protected HT22-TrkB cells, but not HT22-TrkB.T...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.2003.02255.x

    authors： Rössler OG,Giehl KM,Thiel G

    更新日期：2004-03-01 00:00:00

  • Alteration of alpha-tocopherol content in the developing and aging peripheral nervous system: persistence of high correlations with total and specific (n-6) polyunsaturated fatty acids.

    abstract：:In contrast to brain, the sciatic nerve concentration of vitamin E in rats increased rapidly during the postnatal period (approximately fivefold between days 1 and 8), then decreased dramatically (about twofold between days 8 and 30), and further decreased slowly between days 30 and 60 and remained constant up to 2 ye...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.1990.tb04917.x

    authors： Clément M,Bourre JM

    更新日期：1990-06-01 00:00:00

  • Mitigation of peroxynitrite-mediated nitric oxide (NO) toxicity as a mechanism of induced adaptive NO resistance in the CNS.

    abstract：:During CNS injury and diseases, nitric oxide (NO) is released at a high flux rate leading to formation of peroxynitrite (ONOO(*)) and other reactive nitrogenous species, which nitrate tyrosines of proteins to form 3-nitrotyrosine (3NY), leading to cell death. Previously, we have found that motor neurons exposed to low...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/j.1471-4159.2009.05884.x

    authors： Bishop A,Gooch R,Eguchi A,Jeffrey S,Smallwood L,Anderson J,Estevez AG

    更新日期：2009-04-01 00:00:00

  • The subunit composition of a GABAA/benzodiazepine receptor from rat cerebellum.

    abstract：:The pentameric subunit composition of a large population (36%) of the cerebellar granule cell GABAA receptors that show diazepam (or clonazepam)-insensitive [3H]Ro 15-4513 binding has been determined by immunoprecipitation with subunit-specific antibodies. These receptors have alpha 6, alpha 1, gamma 2S, gamma 2L, and...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.1994.63010371.x

    authors： Khan ZU,Gutierrez A,De Blas AL

    更新日期：1994-07-01 00:00:00

  • Inhibition of glucosylceramide synthase stimulates autophagy flux in neurons.

    abstract：:Aggregate-prone mutant proteins, such as α-synuclein and huntingtin, play a prominent role in the pathogenesis of various neurodegenerative disorders; thus, it has been hypothesized that reducing the aggregate-prone proteins may be a beneficial therapeutic strategy for these neurodegenerative disorders. Here, we ident...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1111/jnc.12672

    authors： Shen W,Henry AG,Paumier KL,Li L,Mou K,Dunlop J,Berger Z,Hirst WD

    更新日期：2014-06-01 00:00:00

  • Urotensin-II regulates intracellular calcium in dissociated rat spinal cord neurons.

    abstract：:Urotensin-II (U-II), a peptide with multiple vascular effects, is detected in cholinergic neurons of the rat brainstem and spinal cord. Here, the effects of U-II on [Ca2+]i was examined in dissociated rat spinal cord neurons by fura 2 microfluorimetry. The neurons investigated were choline acetyltransferase-positive a...

    journal_title：Journal of neurochemistry

    pub_type： 杂志文章

    doi：10.1046/j.1471-4159.2002.01196.x

    authors： Filipeanu CM,Brailoiu E,Le Dun S,Dun NJ

    更新日期：2002-11-01 00:00:00