Some effects of ORG GC 94, a potential anti-migraine drug, on human platelets.

Abstract:

:Some effects of Org GC 94 (1,3,4,14b-tetrahydro-2,7-dimethyl-2H-dibenzo[b,f]pyrazino[1,2-d][1,4]oxazepine maleate) on human platelets have been investigated. Without pretreatment with ADP, 5-HT-induced aggregation of humam platets was completely inhibited by 2.5 x 10(-8) M of Org GC 94. Aggregation triggered by noradrenaline (2.5 x 10(-5) M) and uptake of 5-HT by human platelets were inhibited only at the high concentrations of 10(-5) and 10(-4) M of Org GC 94 respectively. Up to millimolar concentrations, Org GC 94 did not liberate lactate dehydrogenase from human platelets. Org GC 94 did not block the oxidative deamination of benzylamine by human platelet rich plasma up to 2.5 x 10(-4) M.

journal_name

Eur J Pharmacol

authors

Bhargava N,Matthijsen R,Schönbaum E

doi

10.1016/0014-2999(77)90290-4

subject

Has Abstract

pub_date

1977-04-07 00:00:00

pages

241-5

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(77)90290-4

journal_volume

42

pub_type

杂志文章
  • The role of ATP-sensitive potassium channel on acute urinary retention and subsequent catheterization in the rat.

    abstract::We investigated the role of K(ATP) channel on acute urinary retention (AUR) induced bladder dysfunction. Eight-week-old female Sprague-Dawley rats were divided into seven groups: a sham-operated control group, an AUR group, and five AUR groups treated with: two different K(ATP) channel openers namely nicorandil (3 or ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.02.052

    authors: Ohmasa F,Saito M,Shimizu S,Taniguchi S,Dimitriadis F,Satoh I,Kinoshita Y,Satoh K

    更新日期:2010-06-10 00:00:00

  • Effect of dihydralazine on the renal kallikrein-kinin system of the rat.

    abstract::Dihydralazine (0.1 mg/kg), injected intravenously into male Sprague-Dawley rats, caused a decrease in mean arterial blood pressure and an increase in renal plasma flow, while urine volume remained unchanged. Dihydralazine had no effect on kallikrein excretion in the urine and on kallikrein activity in the renal cortex...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90239-4

    authors: Bönner G,Beck D,Deeg M,Marin-Grez M,Gross F

    更新日期:1982-02-26 00:00:00

  • Evidence that the purported dopaminergic agonist (3,4-dihydroxyphenylimino)-2-imidazolidine (DPI) may reduce rat striatal dopamine turnover by an alpha 2-adrenergic mechanism.

    abstract::The potent alpha-adrenergic agonist DPI, which has also been claimed to be a selective dopaminergic agonist, was shown to reduce rat striatal dopamine (DA) synthesis, DA utilization and DA metabolism following intraperitoneal administration (25 mumol/kg). An analytical procedure for the determination of DPI was develo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90603-3

    authors: van Oene JC,Houwing HA,Horn AS

    更新日期:1982-06-16 00:00:00

  • Inhibitory effects of benzodiazepines on the adenosine A(2B) receptor mediated secretion of interleukin-8 in human mast cells.

    abstract::The activation of adenosine A(2B) receptors in human mast cells causes pro-inflammatory responses such as the secretion of interleukin-8. There is evidence for an inhibitory effect of benzodiazepines on mast cell mediated symptoms in patients with systemic mast cell activation disease. Therefore, we investigated the e...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.12.003

    authors: Hoffmann K,Xifró RA,Hartweg JL,Spitzlei P,Meis K,Molderings GJ,von Kügelgen I

    更新日期:2013-01-30 00:00:00

  • Modulation of antigen-induced responses by serotonin and prostaglandin E2 via EP1 and EP4 receptors in the peripheral rat lung.

    abstract::The cyclooxygenase (COX) pathway and prostanoids may critically contribute to the early allergic airway response. In the rat lung, serotonin (5-HT) is a major mediator of antigen-induced contractions. The aim of this study was therefore to examine the relative role of the COX pathway and serotonin for antigen-induced ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.11.039

    authors: Larsson-Callerfelt AK,Dahlén SE,Kühl AR,Lex D,Uhlig S,Martin C

    更新日期:2013-01-15 00:00:00

  • Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys.

    abstract::Inhibition of local cortisol regeneration from circulating cortisone by blocking 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been shown to ameliorate the risk factors associated with the metabolic syndrome. Chronic modulation of glucocorticoid homeostasis may result in hypothalamic-pituitary-adrenal (HPA) axis s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.07.004

    authors: Hamilton BS,Schoelch C,Schuler-Metz A,Krosky P,Lala DS,Claremon DA,McGeehan GM

    更新日期:2016-10-15 00:00:00

  • The role of Levosimendan in cardiopulmonary resuscitation.

    abstract::Although initial resuscitation from cardiac arrest (CA) has increased over the past years, long term survival rates remain dismal. Epinephrine is the vasopressor of choice in the treatment of CA. However, its efficacy has been questioned, as it has no apparent benefits for long-term survival or favorable neurologic out...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2014.06.024

    authors: Varvarousi G,Stefaniotou A,Varvaroussis D,Aroni F,Xanthos T

    更新日期:2014-10-05 00:00:00

  • Effect of repeated administration of various doses of cocaine and WIN 35,065-2 on locomotor behavior of mice.

    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

    authors: Reith ME

    更新日期:1986-10-14 00:00:00

  • Differential effect of potassium on the action of digoxin and digoxigenin in guinea-pig heart.

    abstract::The effect of potassium on the binding of digoxin or digoxigenin to isolated Na+, K+-ATPase was compared with that of potassium on the positive inotropic action of the agents in guinea-pig hearts. The binding of digoxigenin to the enzyme in vitro was reduced to a greater extent by potassium than was the binding of dig...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(79)90497-7

    authors: Akera T,Wiest SA,Brody TM

    更新日期:1979-08-15 00:00:00

  • [3H]p-aminoclonidine and [3H]idazoxan label different populations of imidazoline sites on rat kidney.

    abstract::In the presence of RS-15385-197 to preclude binding to alpha 2-adrenoceptors, [3H]p-aminoclonidine labelled a low affinity high capacity site, (Kd = 127.6 +/- 19.7 nM, Bmax 978 +/- 172 fmol/mg protein) whereas [3H]idazoxan labelled a high affinity low capacity site (Kd = 1.66 +/- 0.28 nM, Bmax 45.3 +/- 11.4 fmol/mg pr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90731-v

    authors: MacKinnon AC,Stewart M,Olverman HJ,Spedding M,Brown CM

    更新日期:1993-02-23 00:00:00

  • The effect of cismethrin on the rat dorsal root potentials.

    abstract::Dorsal root potentials were recorded from urethane-anaesthetised rats. Bicuculline, a recognised GABA antagonist, reduced the amplitude of the potential to 67% of control. Cismethrin, a synthetic pyrethroid insecticide, enhanced the potential to 142% of control values. The convulsions associated with cismethrin poison...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90304-0

    authors: Smith PR

    更新日期:1980-08-22 00:00:00

  • The role of endogenous hydrogen sulfide in pathogenesis of chronotropic dysfunction in rats with cirrhosis.

    abstract::Endogenous hydrogen sulfide is produced by cystathionine-γ-lyase and cystathionine-β-synthase in a variety of tissues and has recently been implicated in the regulation of cardiac functions. Acceleration of the heart rate in response to catecholamines is impaired in patients with cirrhosis. The present study was aimed...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.09.039

    authors: Babaei-Karamshahlou M,Hooshmand B,Hajizadeh S,Mani AR

    更新日期:2012-12-05 00:00:00

  • Influence of pharmacologically-induced experimental anxiety on nociception and antinociception in rats.

    abstract::Animal studies reveal that diverse environmental stimuli that generate anxiety-like behaviors also induce antinociception; conversely, clinical data show that pain perception is reduced under anxiolysis. This study was conducted to investigate the influence of pharmacologically induced-anxiety on nociception and antin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.06.060

    authors: Jiménez-Velázquez G,Fernández-Guasti A,López-Muñoz FJ

    更新日期:2006-10-10 00:00:00

  • Gender difference of atorvastatin's vasoprotective effect in balloon-injured rat carotid arteries.

    abstract::The effect of estrogen on neointimal formation in injured rat arteries has been reported to be a sexual dimorphic effect. Recently, it has been reported that 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) exhibit vasoprotective effects, which are independent of their cholesterol-lowerin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.09.036

    authors: Kurumazuka D,Mori T,Matsumoto N,Shirakawa H,Kimura S,Nakano D,Hayashi T,Kitaura Y,Matsumura Y

    更新日期:2006-12-28 00:00:00

  • Histamine-operated calcium channels in intestinal smooth muscle of the guinea-pig.

    abstract::The effects of Bay K 8644 and of nifedipine on histamine-induced mechanical and electrical responses were studied in the longitudinal smooth muscle of the ileum and in the taenia coli isolated from the guinea-pig. Nifedipine (10(-9)-10(-7) M) depressed the tonic and phasic components of histamine contraction. Phasic t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90758-8

    authors: Morel N,Hardy JP,Godfraind T

    更新日期:1987-03-03 00:00:00

  • Effects of S 21403 on hormone secretion from isolated rat pancreas at different glucose concentrations.

    abstract::We investigated the in vitro effects of therapeutical concentrations of S 21403 (a succinic acid derivative also known as KAD 1229 and mitiglinide) on insulin and glucagon secretion during a metabolic stimulus (glucose rising from 5 to 8.33 mM) or at a stable 2.22 mM glucose using the isolated perfused rat pancreas mo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02620-1

    authors: Gregorio F,Ambrosi F,Boemi M,Carle F,Filipponi P

    更新日期:2002-12-05 00:00:00

  • Cocaine and GBR 12783 recognize nonidentical, overlapping binding domains on the dopamine neuronal carrier.

    abstract::In incubation medium containing Na+ as the only cation, the specific binding of [3H]cocaine to a membrane preparation obtained from rat striatum reached a maximal level for 10 mM Na+, whereas higher concentrations decreased its affinity. The specific binding of [3H]cocaine was inhibited monophasically by GBR 12783, ma...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90188-0

    authors: Saadouni S,Refahi-Lyamani F,Costentin J,Bonnet JJ

    更新日期:1994-07-15 00:00:00

  • 5-Lipoxygenase is required for proliferation of immature cerebellar granule neurons in vitro.

    abstract::Primary cultures of rat cerebellar granule neurons express 5-lipoxygenase, an enzyme from the inflammatory pathway of arachidonic acid. Outside the central nervous system (CNS) 5-lipoxygenase participates in cell proliferation. We hypothesized that 5-lipoxygenase is needed for proliferation of immature cerebellar gran...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00924-4

    authors: Uz T,Manev R,Manev H

    更新日期:2001-04-20 00:00:00

  • Cordycepin inhibits LPS-induced acute lung injury by inhibiting inflammation and oxidative stress.

    abstract::Acute lung injury (ALI) is a common severe clinical syndrome in intensive care unit. Inflammation has been reported to play a critical role in the development of ALI. Cordycepin, an active component isolated from Cordyceps militaris, has been reported to have anti-inflammatory effects. However, the anti-inflammatory e...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.10.029

    authors: Lei J,Wei Y,Song P,Li Y,Zhang T,Feng Q,Xu G

    更新日期:2018-01-05 00:00:00

  • Antinociception of spirocyclopiperazinium salt compound LXM-10-M targeting α7 nicotinic receptor and M4 muscarinic receptor and inhibiting CaMKIIα/CREB/CGRP signaling pathway in mice.

    abstract::The present study was designed to investigate the antinociception of spirocyclopiperazinium salt compound LXM-10-M (2,4-dimethyl-9-β-m-hydroxyphenylethyl-3-oxo-6, 9-diazaspiro [5.5] undecane chloride) in thermal and chemical pain models, and further to explore the molecular target and potential signal pathway. We asse...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.11.056

    authors: Wan D,Wang D,Sun Q,Song Y,Jiang Y,Li R,Ye J

    更新日期:2016-01-05 00:00:00

  • Modulatory effect of imetit, a histamine H3 receptor agonist, on C-fibers, cholinergic fibers and mast cells in rabbit lungs in vitro.

    abstract::The pharmacological mechanisms involved in the interactions between C-fibers, cholinergic fibers and mast cells were investigated in tracheally perfused rabbit lungs by measuring the simultaneous release of substance P and histamine in lung effluents. The amounts of substance P and histamine released in lung superfusa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00176-4

    authors: Nemmar A,Delaunois A,Beckers JF,Sulon J,Bloden S,Gustin P

    更新日期:1999-04-23 00:00:00

  • Glucocorticoids for the treatment of post-traumatic stress disorder and phobias: a novel therapeutic approach.

    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

    authors: de Quervain DJ,Margraf J

    更新日期:2008-04-07 00:00:00

  • Role of Ca2+ in the vascular contraction caused by a thrombin receptor activating peptide.

    abstract::Thrombin receptor activating peptide (TRAP) caused a slowly developing, sustained contraction of endothelium denuded rat aortic rings. Both nifedipine (10 microM) and removal of Ca2+ from the physiological salt solution (PSS) caused significant (60-75%) reductions in the contractile response to TRAP. In Ca(2+)-free PS...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90613-0

    authors: Antonaccio MJ,Normandin D

    更新日期:1994-04-11 00:00:00

  • The effect of intracisternally administered bombesin on cysteamine-induced duodenal ulcers in rats.

    abstract::Cysteamine (420 mg/kg s.c.) increased gastric acid secretion in rats 3-6 h post-injection; duodenal pH fell from 6.0 +/- 0.2 (S.E.M.) at 0 time to 2.2 +/- 0.3 at 12 h. A high (60-80%) incidence of duodenal ulcerations was observed 18 h after cysteamine injection. Intracisternal (i.c.) administration of bombesin (1 mic...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(82)90203-5

    authors: Hernandez DE,Adcock JW,Nemeroff CB,Prange AJ Jr

    更新日期:1982-10-22 00:00:00

  • Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640.

    abstract::5-HT(1A) receptor activation by the very-high-efficacy, selective 5-HT(1A) receptor agonist F 13640 [(3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-([(5-methyl-pyridin-2-ylmethyl)-amino]-methyl)piperidin-1-yl]-methanone] was recently discovered to constitute a novel central mechanism of broad-spectrum analgesia that, remarkab...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01566-8

    authors: Bruins Slot LA,Koek W,Tarayre JP,Colpaert FC

    更新日期:2003-04-18 00:00:00

  • The effect of troxypyrrolidinium, a choline uptake inhibitor, on the excitatory innervation of the rat urinary bladder.

    abstract::Troxypyrrolidinium, a choline uptake inhibitor, reduced but failed to abolish responses of the rat urinary bladder to electrical stimulation at 1-100 Hz although it reduced acetylcholine output during stimulation at 10 Hz to a level similar to that of spontaneous release. Inhibition of the response to stimulation was ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(80)90131-4

    authors: Choo LK,Mitchelson F

    更新日期:1980-02-08 00:00:00

  • Neuropharmacology of glucocorticoids: focus on emotion, cognition and cocaine.

    abstract::Hormone pharmacology has been quite interesting in The Netherlands the past century and this contribution is dedicated to the glucocorticoid hormones underlying adaptation to stress. The story starts in 1936 with Tadeus Reichstein and Ernst Laqueur who discovered corticosterone at the time Hans Selye formulated the st...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2008.03.011

    authors: de Kloet ER,de Jong IE,Oitzl MS

    更新日期:2008-05-13 00:00:00

  • Protective effects of fluoroquinolones on UV-induced damage of cultured ocular cell lines.

    abstract::Although the fluoroquinolones have strong antibacterial effects, some of them also have adverse ocular effects such as diplopia, uveitis, optic neuropathy, and retinal detachment. The purpose of this study was to determine whether low concentrations of fluoroquinolones can lessen the cytotoxic effects of ultraviolet (...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.04.004

    authors: Nishida T,Kuse Y,Mochizuki K,Shimazawa M,Yamamoto T,Hara H

    更新日期:2017-07-05 00:00:00

  • Termination of ouabain-induced ventricular tachycardia by flunarizine in conscious dogs.

    abstract::The ability of flunarizine to terminate ouabain-induced ventricular tachycardia was investigated in conscious dogs. These arrhythmias result from triggered activity based on delayed afterdepolarizations. Sustained ventricular tachycardia was induced by ouabain (48 +/- 6 micrograms/kg) and pacing in 13 animals with sur...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90780-2

    authors: Vos MA,Gorgels AP,Drenth JP,Leunissen JD,Wellens HJ

    更新日期:1989-06-08 00:00:00

  • Regulatory role of the dopamine and norepinephrine transporters in pentylenetetrazol-kindled mice: association with effect of antidepressants.

    abstract::In clinical practice, patients with epilepsy are frequently associated with psychiatric disorders, including cognitive impairment, depression, and attention deficit hyperactivity disorder. In fact, patients with epilepsy often take centrally acting drugs, such as antidepressants and anxiolytics; however, it remains un...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.10.017

    authors: Takechi K,Suemaru K,Kawasaki H,Araki H

    更新日期:2011-12-30 00:00:00