Abstract：
:We investigated the effects of the platelet activating factor (PAF) receptor antagonists, SM-12502 ((+)-cis-3,5-dimethyl-2-(pyridyl)- thiazolidin-4-one hydrochloride), WEB-2086 (3-(4-(2-chlorphenyl)-9-methyl-6H-thieno(3,2-f)-(1,2,4)triazolo(4, 3- a)(1,4)diazepin-2-yl)-1-(4-morpholinyl)-1-propanone) and RP-48740 (3-(3-pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole-7-carboxamide) on the PAF-mediated activation of rat neutrophils. These antagonists inhibited PAF-induced degranulation and chemotaxis in neutrophils at a dose that correlated well with PAF-induced platelet aggregation based on the statistical analyses. N-formyl-L-methionyl-L-leucyl-L- phenylalanin (fMLP)-induced cellular responses were also inhibited by the PAF receptor antagonists, but their inhibitory potencies did not correlate with those for PAF-induced platelet aggregation. In addition, the doses required for inhibition were higher than those required against PAF-induced responses (i.e. IC50 ratio of WEB-2086, SM-12502 and RP-48740 in fMLP-induced/PAF-induced degranulation was 40.0, 2.8 and 5.6, respectively). PAF receptor antagonists inhibited inositol 1,4,5-triphosphate production and the release of Ca2+ from the intracellular store site after stimulation with PAF. In the fMLP-induced responses, PAF receptor antagonists did not inhibit IP3 production and Ca2+ release, but did inhibit transmembrane Ca2+ influx. These results suggest the presence of distinct PAF receptor subtype, to which exogenously added PAF binds, while endogenously produced PAF binds to the other. Intracellular PAF, which was produced by fMLP-stimulation, may play an important role in the late phase of signal transduction, and may participate in the transmembrane Ca2+ influx.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Koike H,Imanishi N,Natsume Y,Morooka Sdoi
10.1016/0922-4106(94)90037-xsubject
Has Abstractpub_date
1994-11-15 00:00:00pages
299-309issue
3eissn
0014-2999issn
1879-0712journal_volume
269pub_type
杂志文章abstract：:The Nuclear factor (erythroid 2-derived)-like 2 (Nrf2) plays a key role in inflammation which is implicated in the pathophysiology of depression. The Nrf2 activators have antidepressant effects in animal models of depression. The present study was undertaken to examine whether TBE-31 [(±)-(4bS,8aR,10aS)-10a-ethynyl-4b...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.10.037
更新日期：2016-12-15 00:00:00
abstract：:The glutamate receptor agonists, kainate and N-methyl-D-aspartate (NMDA) result in the elevation of intracellular calcium levels ([Ca2+]i) in primary cultures of cerebellar granule neurons. Several tricyclic antidepressants (TCAs), amitriptyline (0.5-1 microM), desipramine (1 microM) and doxepine (1 microM) partially ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90579-s
更新日期：1992-08-14 00:00:00
abstract：:The effects of intraperitoneal injections of two opioid antagonists on plasma corticosterone levels in stressed mice was investigated. The effects of the mu-opioid receptor antagonist naloxone was dependent on the dose used. Low doses (0.5 and 1 mg/kg) potentiated the elevation of plasma corticosterone observed in sal...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90042-6
更新日期：1984-05-18 00:00:00
abstract：:Dinitrosyl iron complexes (DNIC) with glutathione exert a cytotoxic effect on endometrioid tumours in rats with surgically induced experimental endometriosis. Intraperitoneal treatment of rats (Group 1) with DNIC (12.5μmoles/kg, daily, for 12 days), beginning with day 4 after the surgical operation (implantation of tw...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.002
更新日期：2014-03-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90753-3
更新日期：1986-07-15 00:00:00
abstract：:N-Phthaloyl gamma-aminobutyric acid, a new gamma-aminobutyric acid derivative synthesized in this laboratory, has been found to possess anticonvulsant, antinociceptive and antistress activities. Effects of this derivative on gastric lesions induced by aspirin and ethanol were studied in rats. N-Phthaloyl gamma-aminobu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90298-i
更新日期：1992-08-25 00:00:00
abstract：:The actions of dequalinium have been investigated in cultured rat sympathetic neurones. It produced a rapid and reversible inhibition of the slow apamin-sensitive component of the afterhyperpolarization (AHP) which follows a single action potential in these cells. The IC50 for this effect was 1.1 microM and in voltage...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90596-7
更新日期：1994-02-03 00:00:00
abstract：:The effects of ZD0947, a novel ATP-sensitive K+ channel (KATP channel) opener, on the activity of reconstituted KATP channels were investigated using cell-attached recordings. KATP channels were studied in HEK 293 cells by co-expression of inwardly rectifying-6 family K+ channel subunits (Kir6.x: Kir6.1 and Kir6.2) wi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.09.038
更新日期：2016-11-15 00:00:00
abstract：:Neuropathic pain is a type of chronic pain following central or peripheral nervous system lesions that cause allodynia (pain initiated by a non-painful stimulus) and hyperalgesia (increased pain sensation following a painful stimulus). The first objective of the study was to evaluate the pharmacokinetics of eugenol, t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.01.044
更新日期：2007-05-07 00:00:00
abstract：:Brain microvessel endothelial cell monolayers have been shown to be a suitable blood-brain barrier in vitro system to study adrenergic regulation of permeability. We tested adrenergic drugs on bovine brain microvessel endothelial cell monolayer permeability to a biomembrane impermeant molecule, sodium fluorescein. End...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90092-2
更新日期：1994-10-14 00:00:00
abstract：:The anti-ulcer activity of calcitonin gene-related peptide (CGRP) was inhibited, in a dose-dependent manner, by pretreatment with NG-nitro-L-arginine methyl ester, an inhibitor of nitric oxide synthase. Our results suggest that endogenous nitric oxide is involved in the anti-ulcer activity of CGRP. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90252-6
更新日期：1994-04-21 00:00:00
abstract：:A mixture of dexamphetamine and chlordiazepoxide induces hyperactivity in both mice and rats. This type of hyperactivity has been proposed as an animal model of mania. Magnesium valproate itself had little influence on the activity of normal mice and rats. Acute pretreatment of mice with magnesium valproate (75-300 mg...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90266-k
更新日期：1993-06-24 00:00:00
abstract：:Three agents with K+ channel blocking activity, procaine, 4-aminopyridine (4-AP) and tetraethylammonium (TEA), were tested for inhibition of vasorelaxation and 86Rb+ efflux induced by cromakalim (BRL 34915), pinacidil and nicorandil in rabbit isolated mesenteric artery. The potency order for inhibition of vasorelaxati...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90728-5
更新日期：1988-08-02 00:00:00
abstract：:The action of organic solvents on the biochemical and biophysical properties of protein kinase C (PKC) was measured in a defined lipid vesicle system. Chloroform, benzyl alcohol and ethanol all partially activated PKC. They had no effect on the Ca(2+)- or anionic phospholipid-, phosphatidylserine-dependence. Their abi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90114-w
更新日期：1991-04-25 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00623-1
更新日期：1996-11-14 00:00:00
abstract：:Recent studies suggested the involvement of the endocannabinoid pathway on insulin secretion in RINm5F cells or rat islets. Animal and clinical studies have reported beneficial effects of the selective cannabinoid 1 receptor antagonist rimonabant on glucose homeostasis. The aim of this study was to investigate the in ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.05.024
更新日期：2009-08-15 00:00:00
abstract：:Histopathological parameters are essential for deciding on adjuvant treatment following breast cancer surgery. We assessed the impact of inter-observer variability on treatment strategy in patients operated for clinically node negative, non-palpable breast carcinomas. In the context of a multicenter randomised control...
journal_title：European journal of pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ejphar.2012.12.033
更新日期：2013-10-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90522-1
更新日期：1980-12-05 00:00:00
abstract：:Fructose-2,6-bisphosphate is a potent activator of 6-phosphofructo-1-kinase, a key enzyme in glycolysis. We previously revealed that sulfonylureas stimulate fructose-2,6-bisphosphate production in the rat liver by activating 6-phosphofructo-2-kinase. In the present study, we show that CS-045, a new antidiabetic agent,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1994-03-21 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：2019-01-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90238-5
更新日期：1988-01-12 00:00:00
abstract：:Glycine displaces [3H]CGP-39653 ([3H]D,L-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid) binding to the glutamate recognition site with both high and low affinity. We reported previously that chronic treatment with antidepressants reduced the proportion of high to low affinity sites, or, even eliminated the high af...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01589-6
更新日期：1998-01-26 00:00:00
abstract：:The functional role of metabotropic glutamate (mGlu) receptors in the rat dentate gyrus was investigated. By using extracellular recording techniques in slices, it was found that the depression induced by the mGlu receptor agonist (1S,3R)-1-amino-cyclopentane-1,3-dicarboxylate (ACPD) was mediated through the mGlu grou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00560-9
更新日期：1995-12-29 00:00:00
abstract：:This study evaluated the coronary dopamine receptors by using the dopamine D1 receptor agonist fenoldopam, dopamine D2 receptor agonist propylbutyldopamine, and their selective antagonists SCH23390 and domperidone. Left circumflex coronary flow (CF), coronary perfusion pressure at constant flow, left ventricular hemod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94126-i
更新日期：1990-11-06 00:00:00
abstract：:We tested if discontinuation of cocaine self-administration can lead to the development of depressive-like symptoms in the forced swim test expressed as changes in immobility, swimming and climbing behaviors in rats. A "yoked" procedure in which rats were run simultaneously in groups of three, with two rats received t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.10.049
更新日期：2010-02-10 00:00:00
abstract：:[D-Met2,Pro5]enkephalinamide (DMPEA) strongly activated cardioinhibitory vagal efferents and elicited bradycardia when perfused through the cerebroventricular system of anaesthetized dogs. These effects were concentration-dependent but plateaued at an intraventricular concentration of 200 micrograms/ml. At this maxima...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90216-x
更新日期：1985-04-02 00:00:00
abstract：:The effects of N- and L-type voltage operated calcium channel (VOCC) antagonists were examined on the bronchoconstriction induced by vagal stimulation in artificially respired guinea-pigs. Vagal stimulation produced a reproducible and consistent bronchoconstrictor response which corresponded to an increase in pulmonar...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90589-v
更新日期：1992-08-14 00:00:00
abstract：:The effect of treatment with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) on juvenile (6-8 months), young adult (2-4 years) and aged (8-10 years) common marmosets were compared. Juvenile marmosets were more resistant to the actions of MPTP and required a greater cumulative dose over a longer period to induce th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90800-w
更新日期：1993-01-12 00:00:00
abstract：:The effect of papaverine on the positive inotropic response to isopreqaline and to calcium was studied on the rabbit isolated papillary muscle; theophylline and the calcium antagonistic D600 were used for comparison. The dose-response curve for isoprenaline was shifted to the left by papaverine (3 times 10- minus 6 to...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90102-8
更新日期：1975-02-01 00:00:00
abstract：:Alzheimer's disease is the most frequent cause of dementia. Family and twin studies have suggested that genetic factors play a role in Alzheimer's disease development. Some Alzheimer's disease cases show an autosomal dominant inheritance pattern and thus allow the discovery of major disease genes. However, most Alzhei...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(00)00903-1
更新日期：2001-01-19 00:00:00
