Abstract:
:Infusion of arachidonic acid through the guinea pig lung or the cat spleen causes a release of thromboxane A2 and prostaglandins, as measured by bioassay. After incubation of human platelets with arachidonate similar metabolites are formed, as demonstrated chromatographically. Infusion of imidazole (50-75 microgram/ml) through the lung or spleen specifically inhibits thromboxane A2 production and diverts the pathway to the prostaglandins, mainly prostaglandin F2alpha. In human platelets imidazole causes a dose-dependent inhibition of thromboxane A2 formation (ID50 5.5 X 10(-4) M). This inhibition is accompanied by a dose-dependent increase in prostaglandin F2alpha. Since thromboxane A2 induces platelet aggregation and is a potent vasoconstrictor, diversion of pathways to prostaglandins with opposite or less potent action might be of relevance in the treatment of cardiovascular diseases.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Nijkamp FP,Moncada S,White HL,Vane JRdoi
10.1016/0014-2999(77)90104-2subject
Has Abstractpub_date
1977-07-15 00:00:00pages
179-86issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(77)90104-2journal_volume
44pub_type
杂志文章abstract::Prostaglandin E2 increases bradykinin-induced spike activity from polymodal nociceptors of the skin and deep tissues in animals, suggesting sensitization of these receptors. To see whether these neurophysiological observations in animals correspond with increased pain intensity in humans, and whether also vascular noc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00575-7
更新日期:1995-12-29 00:00:00
abstract::Post-traumatic stress disorder (PTSD) and phobias belong to the most common anxiety disorders and to the most common psychiatric illnesses in general. In both disorders, aversive memories are thought to play an important role in the pathogenesis and symptomatology. Previously, we have reported that elevated glucocorti...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2007.11.068
更新日期:2008-04-07 00:00:00
abstract::Local anaesthetics block action potentials in the membranes of excitable cells but their effects on non-excitable cells are less well known. Some local anaesthetics are applied directly onto the skin, and for this reason the effect of procaine (p-aminobenzoic acid diethylamino-etyl ester hydrochloride) and tetracaine ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00623-2
更新日期:1998-10-09 00:00:00
abstract::There is some controversy as to whether 5-HT(2C) receptor agonists are anxiogenic or anxiolytic. The effects of the novel 5-HT(2C) receptor agonist, (S)-2-chloro-5-fluoro-indol-1-yl)-1-methyl ethylamine fumarate (RO 60 0175), in three models of anxiety were therefore tested. RO 60 0175 was found to induce hypolocomoti...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00706-2
更新日期:2000-01-10 00:00:00
abstract::Stimulation of [35S]GTPgammaS binding by serotonin (5-hydroxytryptamine, 5-HT) receptor ligands was characterized in rat hippocampal membranes. The optimized assay contained 30-50 microg protein, 300 microM GDP and 0.1 nM [35S]GTPgammaS, incubated at 37 degrees C for 20 min. At 10 microM, the 5-HT1A receptor agonist R...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01547-1
更新日期:1998-02-19 00:00:00
abstract::The potency of the dihydropyridine calcium channel blocker, PN 200-110 was assessed in vitro against contractions induced by potassium (20-55 mM) and histamine (1-300 microM) in rabbit thoracic aorta, coronary, basilar, renal and central ear arteries. PN 200-110 was particularly effective against potassium responses i...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(86)90623-0
更新日期:1986-12-16 00:00:00
abstract::Painless myocardial infarction is a serious complication of diabetes. The present study examined whether cardiac nociception was altered in the streptozotocin-induced diabetic rat model by assessing intrapericardial capsaicin-evoked electromyography (EMG) responses in the spinotrapezius muscle. Somatic sensitivities t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.10.073
更新日期:2011-01-25 00:00:00
abstract::Synaptic pathology is associated with protein accumulation events, and is thought by many to be the best correlate of cognitive impairment in normal aging and different types of dementia including Alzheimer's disease. Numerous studies point to the disruption of microtubule-based transport mechanisms as a contributor t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.01.053
更新日期:2007-05-07 00:00:00
abstract::Kinins are known to be potent releasers of histamine. In the present study, the B2 antagonist analogues of bradykinin (BK) and kallidin (KD): [( Thi6,9,D-Phe8]KD, [Thi5,8,D-Phe7]BK) were also found to be potent releasers of histamine from rat mast cells and not to exert any antagonistic effect. Similarly, two B1 recep...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90051-9
更新日期:1988-04-27 00:00:00
abstract::Effects of protein kinase C inhibitors, staurosporine and 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine dihydrochloride and protein tyrosine kinase inhibitors, genistein, tyrphostin and 2,5-dimethylcinnamate on the neutrophil responses stimulated by immunoglobulin G (IgG), complement C5a or platelet-activating factor...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00097-0
更新日期:1996-06-13 00:00:00
abstract::Cultured retina cells released accumulated [3H]GABA (gamma-aminobutyric acid) when stimulated by L-glutamate, N-methyl-D-aspartate (NMDA) and kainate. In the absence of Mg2+, dopamine at 200 microM (IC50 60 microM), inhibited in more than 50% the release of [3H]GABA induced by L-glutamate and NMDA, but not by kainate....
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01522-7
更新日期:1998-02-05 00:00:00
abstract::Glioma is a kind of lethal malignant tumor, and lacks efficient therapies. Combination therapy has been claimed to be a promising approach to combat cancer, due to its increased anti-cancer effects and reduced side effects. This study aimed to investigate the anti-cancer effect and mechanism of combining imatinib with...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.173022
更新日期:2020-05-05 00:00:00
abstract::The effects of itasetron (endo-N-8-methyl-8-azabicyclo-[3.2.1.]-octo-3-yl) -2,3-dihydro-2-oxo-1 H-benzimidazole-1-carboxamide hydrochloride), a 5-HT3 receptor antagonist, on discrete memory abilities of the aged rat were assessed by using the multiple choice avoidance behavioral task. Chronic treatment with itasetron ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00586-9
更新日期:1996-09-12 00:00:00
abstract::Selective serotonin reuptake inhibitors (SSRIs) are widely used as a first-line therapy in postpartum depression. The objective of this study was to determine the mechanism underlying the inhibitory effects of the SSRI, fluvoxamine, on β-casein expression, an indicator of lactation, in MCF-12A human mammary epithelial...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.09.038
更新日期:2015-11-05 00:00:00
abstract::We assessed the intrinsic activity of the purported selective muscarinic M1 receptor agonist SR 95639A (morpholinoethylamino-3-benzocyclohepta-(5,6-c)-pyridazine) in inducing several receptor-mediated signals. Our results indicate that SR 95639A lacks the ability to activate phosphoinositide hydrolysis in rat cerebral...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(92)90126-g
更新日期:1992-10-01 00:00:00
abstract::Morphine and aspartic acid were administered separately and in combination to 80 rats divided into 8 groups. Ten and 20 min following the injections, brain, liver and kidney L-asparaginase activity was determined. Morphine decreased brain and liver L-asparaginase activity and increased that of kidney. Aspartic acid co...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90244-9
更新日期:1979-12-20 00:00:00
abstract::The alpha(2)-adrenoceptor agonist, clonidine, modulates colorectal sensorimotor functions in humans and, given intrathecally, has analgesic effects in the colorectal distension (CRD) model in rats. We tested the effects of systemic clonidine on the visceral pain-related viscerosomatic and autonomic cardiovascular resp...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.06.056
更新日期:2008-09-04 00:00:00
abstract::The effects of GABA and diazepam on the spontaneous and potassium-evoked release of 3H-5-HT from rat hippocampal synaptosomes, preloaded by incubation with 3H-5-HT, have been investigated. Both GABA and diazepam independently increased the spontaneous release of 5-HT whereas they blocked the calcium-dependent, potassi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(80)90054-0
更新日期:1980-11-07 00:00:00
abstract::The influence of increasing concentrations of histamine (0.1 microM-1 mM) was studied on proximal and distal ring segments of left anterior descendens coronary arteries isolated from rats. Addition of histamine to prostaglandin F2 alpha (10 microM)-precontracted proximal segments elicited a further contraction. This e...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90259-3
更新日期:1994-12-12 00:00:00
abstract::Acute administration of delta 9-tetrahydrocannabinol (THC) (50 mg/kg) at puberty (35-40 days) significantly (P less than 0.05) reduced Ca2+ ATPase activity in hypothalamic plasma membranes but increased, although not significantly, enzyme activity in hypothalamic tissue obtained from adult mice. In contrast, testicula...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90186-5
更新日期:1987-05-07 00:00:00
abstract:UNLABELLED:The influence of different nonsteroidal anti-inflammatory drugs (NSAIDs) and of a proton pump inhibitor on the healing parameters of a chronic gastric ulcer was evaluated. Wistar rats were used after the induction of a chronic acetic acid ulcer. The animals were treated orally for 8 and 15 days, twice daily,...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01494-2
更新日期:2002-05-03 00:00:00
abstract::By using acutely dissociated dorsal raphe nucleus neurons (DRN) from young mice, direct and anti-opioid effects of Neuropeptide FF (NPFF) receptors were measured. The NPFF analog 1 DMe (10 µM) had no effect on resting Ca2+ channels but reduced the magnitude of Ca2+ transients induced by depolarization in 83.3% neurons...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.07.013
更新日期:2014-10-05 00:00:00
abstract::We have characterized the rat prostanoid EP1, EP2, EP3alpha and EP4 receptor subtypes cloned from spleen, hepatocyte and/or kidney cDNA libraries. Comparison of the deduced amino acid sequences of the rat EP receptors with their respective homologues from mouse and human showed 91% to 98% and 82% to 89% identity, resp...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01383-6
更新日期:1997-12-11 00:00:00
abstract::Adenosine relaxes the coronary arteries of various species through A2 receptors. The mechanism(s) by which adenosine causes relaxation of the coronary smooth muscle through changes in intracellular Ca levels is not understood. Therefore, the aim of this study was to evaluate the vasodilatory action of adenosine in nor...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90040-x
更新日期:1989-01-02 00:00:00
abstract::Adenosine (10(-4)-10(-3) M) contracted the isolated rat tail artery. This effect exhibited rapidly developing tachyphylaxis. Methysergide (10(-7) M) prevented the contractile response to adenosine and 5-hydroxytryptamine (5-HT) without affecting that to noradrenaline. Pretreatment of rats with parachlorophenylalanine ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90513-6
更新日期:1981-12-03 00:00:00
abstract::The present study describes the effect of sertindole, clozapine and haloperidol on the number of spontaneously active dopamine neurons in ventral tegmental area and substantia nigra pars compacta after daily oral treatment for 1, 2 or 3 weeks. In general, daily administration of high dosages (sertindole: 2.8 mumol/kg/...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90468-5
更新日期:1994-03-21 00:00:00
abstract::Previous studies of myocardium have shown that ischemic preconditioning could be mimicked by nitroglycerin through stimulating the release of calcitonin gene-related peptide (CGRP). The present study examined whether nitroglycerin could also provide a preconditioning stimulus in the peripheral vascular bed (the anse i...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01256-0
更新日期:2001-11-02 00:00:00
abstract::The high-level production of nitric oxide (NO) induced by inflammatory cytokines has been shown to play a key role in the pathogenesis of inflammation-mediated osteoporosis. In the present work, we observed that 1mM of the NO donor sodium nitroprusside (SNP) induced an increase of the cytosolic calcium concentration (...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.05.009
更新日期:2013-09-05 00:00:00
abstract::We used male Wistar rats to determine the effects of lipopolysaccharide (LPS) on gastric secretion. After pylorus ligation, 24-h fasted rats received i.p. injections of different doses of LPS dissolved in sterile saline. The amounts of gastric acid and pepsin secreted were determined 2, 4 or 8 h after injection. Small...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90256-6
更新日期:1990-05-31 00:00:00
abstract::In the rat substantia nigra Type II benzodiazepine recognition sites (measured as the portion of [3H]flunitrazepam binding which remain after the addition of 2 X 10(-7) M Cl 218872) represent 50% of the total benzodiazepine recognition sites. The density of Type II sites was increased by 35% following the degeneration...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90507-2
更新日期:1985-06-07 00:00:00