Abstract:
:Glucocorticoids bind to and activate a cytoplasmic glucocorticoid receptor. The activated glucocorticoid receptor translocates into the nucleus and binds to specific response elements in the promoter regions of anti-inflammatory genes such as lipocortin-1 and secretory leukocyte protease inhibitor (SLPI). However, the major anti-inflammatory effects of glucocorticoids appear to be due largely to interaction between the activated glucocorticoid receptor and transcription factors, notably nuclear factor-kappaB (NF-kappaB) and activator protein-1 (AP-1), that mediate the expression of inflammatory genes. NF-kappaB switches on inflammatory genes via a process involving recruitment of transcriptional co-activator proteins and changes in chromatin modifications such as histone acetylation. This process must occur in the correct temporal manner to allow for effective inflammatory gene expression to occur. The interactions between NF-kappaB and the glucocorticoid receptor result in differing effects on histone modifications and chromatin remodelling. Drugs that enhance glucocorticoid receptor nuclear translocation (long acting beta-agonists) and GR-associated histone deacetylases activity (theophylline) have been shown to be effective add-on therapies. In addition, dissociated glucocorticoids that target NF-kappaB preferentially have also been successful in the treatment of allergic disease.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Hayashi R,Wada H,Ito K,Adcock IMdoi
10.1016/j.ejphar.2004.07.011keywords:
subject
Has Abstractpub_date
2004-10-01 00:00:00pages
51-62issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(04)00720-4journal_volume
500pub_type
杂志文章,评审abstract::We have investigated the role of tyrosine kinase in the antiarrhythmic effects of peroxynitrite preconditioning in rat isolated heart by using a tyrosine phosphatase inhibitor, sodium orthovanadate, and tyrosine kinase inhibitors, genistein and tyrphostin. Rat hearts were preconditioned by peroxynitrite administration...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(03)01377-3
更新日期:2003-03-19 00:00:00
abstract::The aim of this study was to assess the role of nitric oxide (NO) in lipid peroxidation following 5 min of bilateral carotid occlusion in the Mongolian gerbil. The study consisted of 4 experimental groups (n = 10). Animals were either sham operated, subjected to bilateral carotid occlusion or administered the NO synth...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00502-c
更新日期:1995-10-16 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90456-g
更新日期:1990-09-21 00:00:00
abstract::In isolated rat aorta, endothelin-1 induced contractions at lower concentrations than endothelin-3. The contractile effects were augmented by removing the endothelium. In contrast, endothelium-1 and endothelin-3 at similar concentrations induced endothelium-dependent relaxation in norepinephrine-stimulated aorta. IRL ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90112-u
更新日期:1993-02-16 00:00:00
abstract::Cocaine and a cocaine analog, WIN 36,065-2, were administered daily for 3 or 4 days. Both compounds developed sensitization to their locomotor stimulatory effects, with similarly shaped dose-response curves. Dosages giving optimal sensitization were 25 mg/kg per day for cocaine and 3 mg/kg for WIN 35,065-2. At 40 mg/k...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90184-6
更新日期:1986-10-14 00:00:00
abstract::Therapeutic angiogenesis is a promising strategy for treating ischemia. The lysophospholipid mediator sphingosine-1-phosphate (S1P) acts on vascular endothelial cells to stimulate migration and tube formation, and plays the critical role in developmental angiogenesis. We developed poly(lactic-co-glycolic-acid) (PLGA)-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.02.038
更新日期:2010-05-25 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90085-6
更新日期:1981-07-17 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90645-9
更新日期:1984-10-01 00:00:00
abstract::Neurotoxins are harmful to nervous system and cause either neuronal cell death or impairment of synaptic activity, which contributes to Parkinson's disease or other neuronal disorders. Hippocampal synaptic plasticity was proposed as a cellular model for memory processing. In this study, we reported a novel effect of n...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2016.11.048
更新日期:2017-01-15 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90364-2
更新日期:1981-04-09 00:00:00
abstract::The N-methyl-D-aspartate (NMDA) receptor-mediated component of the synaptic response of cerebellar granule cells to mossy fibre stimulation was selectively inhibited by the nitric oxide (NO) donor, nitroprusside (nitroferricyanide). The direct depolarisation of granule cells induced by perfusion of NMDA was similarly ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90021-h
更新日期:1991-12-10 00:00:00
abstract::In the presence of thiorphan an 'enkephalinase' inhibitor, bestatin an aminopeptidase inhibitor of bacterial origin potently inhibited the hydrolysis of [3H][Leu5]enkephalin by slices from rat striatum with an IC50 value of about 0.2 microM whereas puromycin was approximately 1000 times less potent on this preparation...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90181-4
更新日期:1983-01-21 00:00:00
abstract::An 125I-iodinated ryanodine analog, modified by attaching an iodo-Cbz-beta-alanyl group to the C10eq hydroxy of ryanodine (iodo-carbobenzyloxy-beta-alanyl-ryanodine), binds to cardiac sarcoplasmic reticulum Ca2+ release channels with equal affinity as [3H]ryanodine. In the present study, both iodo-Cbz-beta-alanyl-ryan...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90061-2
更新日期:1994-08-16 00:00:00
abstract::Our purpose was to verify if alcohol causes alterations on translocation of Ca(2+) and tension induced by KCl or noradrenaline in vas deferens of periadolescent Wistar rats. A single dose of alcohol (i.p. 3.0g/kg) or saline as control, was given 4h before sacrifice. Longitudinal strips of prostatic portion were mounte...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.04.009
更新日期:2014-07-15 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.12.028
更新日期:2011-04-25 00:00:00
abstract::Administration of endothelin to inactin-anesthetized rats resulted in a significant renal vasoconstriction as evidenced by a reduction in both renal plasma flow and glomerular filtration rate. Infusion of the novel nonpeptide endothelin ETA/ETB receptor antagonist, (+/-)-SB 209670, [(1RS-2SR,3RS)-3-(2-carboxymethoxy-4...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00591-9
更新日期:1995-12-29 00:00:00
abstract::Anandamide (AEA), an endogenous cannabinoid and vanilloid receptor ligand, possesses anti-inflammatory properties. Transport of AEA through cytoplasm is facilitated by heat shock protein (HSP) Hsp70, which enhances the rate of cellular AEA uptake, possibly via direct interactions. In lungs, increased HSP expression is...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.06.045
更新日期:2011-10-01 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90553-t
更新日期:1993-08-10 00:00:00
abstract::The recovery of the muscarinic cholinergic receptor (mAChR) from its down-regulation by long-term exposure to ACh was investigated. This was done to obtain information about regulation of the mAChR. Exposure of guinea-pig vas deferens to 30 microM ACh for 24 h decreased the amount of mAChR to 30% of the initial level,...
journal_title:European journal of pharmacology
pub_type: 杂志文章
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.06.057
更新日期:2011-10-01 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.10.096
更新日期:2011-02-25 00:00:00
abstract::Administration of methyl-beta-carboline-3-carboxamide (FG 7142, 15 mg/kg i.p.) to rats has previously been shown to cause a selective increase in the levels of 3,4-dihydroxy-phenylacetic acid (DOPAC) in the prefrontal cortex and ventral tegmental area (VTA) via an interaction with benzodiazepine receptors. On withdraw...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90221-4
更新日期:1987-06-04 00:00:00
abstract::Corticotropin-releasing factor (CRF) is a neurohormone that mediates stress, anxiety, and affects serotonergic activity. Studies have shown that CRF has dose-dependent opposing effects on serotonergic activity. This effect has been hypothesized to be differentially mediated by CRF(1) and CRF(2) receptors in the dorsal...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.09.024
更新日期:2008-01-14 00:00:00
abstract::The role of tuberoinfundibular and periventricular-hypophysial dopaminergic neurons in mediating rimcazole-induced decreases in plasma concentrations of prolactin and alpha-melanocyte stimulating hormone was assessed. Dopaminergic neuronal activity was estimated by measuring concentrations of 3,4-dihydroxyphenylacetic...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00841-1
更新日期:1996-03-28 00:00:00
abstract::[3H]MDL 105,519 (((E)-3-(2-phenyl-2-carboxyethenyl)-4,6-dichloro-1[3H]-indole-2-ca rboxylic acid) is a novel radioligand which binds with high affinity, Kd = 2.5 nM, to the glycine site of adult rodent forebrain, N-methyl-D-aspartate subtype of glutamate receptors. As with other glycine site antagonists, the major det...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00431-2
更新日期:1998-07-17 00:00:00
abstract::[3H]Idazoxan is a labelled ligand that is frequently used to study alpha 2-adrenoceptors in the central nervous system. In pig kidney membranes, [3H]idazoxan labelled high-affinity binding sites (Kd = 1.5 nM) that were not alpha 2-adrenoceptors and which recognized clonidine with low affinity. This new class of bindin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90503-7
更新日期:1989-01-31 00:00:00
abstract::The novel CCK antagonist L364,718 was tested on caerulein- and morphine-induced antinociception in rat using the paw pressure test. Caerulein-induced antinociception (ED50 = 30 micrograms/kg) was significantly inhibited by L354,718 (200 micrograms/kg i.p.) which on its own did not affect paw pressure threshold. In con...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90849-7
更新日期:1988-07-26 00:00:00
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journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.02.012
更新日期:2019-06-15 00:00:00
abstract::The spasmolytic activity of synthetic alpha-human atrial natriuretic peptide (alpha-hANP) and its related peptides was determined in vitro using the chick rectum and the rat aorta. Natriuretic activity was also measured in the anesthetized rat, alpha-hANP-(7-28), with the NH2-terminal hexapeptide truncated, had greate...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90632-2
更新日期:1988-02-16 00:00:00
abstract::Atropine-induced locomotor stimulation was investigated in the developing rat pretreated with 6-hydroxydopa at birth. The locomotor stimulation by atropine was first observed on day 20 and gradually increased with age. The treatment with 6-hydroxydopa potentiated atropine-induced locomotor stimulation on days later th...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(78)90149-8
更新日期:1978-08-15 00:00:00