Biochemical and cellular effects of heparin-protamine injection in rabbits are partially inhibited by a PAF-acether receptor antagonist.

Abstract:

:The origin of the thrombocytopenia and leucopenia induced by protamine-heparin complexes is unknown. We studied the biochemical and cellular effects of protamine (6 mg x kg-1, i.v.) injected after heparin (5 mg x kg-1, i.v.) in New Zealand rabbits. After protamine injection (0.5 min) increases in blood platelet-activating factor (PAF-acether, PAF) (27.6 +/- 27.6 to 148.2 +/- 48.9 pg x ml-1, P < 0.05), thrombocytopenia (403 +/- 64 to 166 +/- 13 cells x 10(-3) x mm-3, P < 0.05) and leucopenia (7650 +/- 930 to 4300 +/- 668 cells x mm-3, P < 0.05) were noted. Plasma thromboxane B2 increased at 1 min (125.6 +/- 24.4 to 879.7 +/- 141.0 pg x ml-1, P < 0.01). Protamine alone induced no change. Indomethacin (3 mg x kg-1, i.v.) did not counteract the effects of heparin-protamine. Pretreatment with the PAF receptor antagonist BN 52021 [9H1, 7a-(epoxymethano)-1 H,6aH-cyclopenta[c]furo[2,3-b]furo-[3',2',3,4]cyclopenta[1,2-d]fur an-5,9, 12(4H)trione,3-tert-butylhexahydro-4,7b,11 hydroxy-8 methyl] alone (3 mg x kg-1, i.v.) delayed thrombocytopenia and reduced plasma thromboxane B2 concentration but did not modify leucopenia. Thus thrombocytopenia and thromboxane B2 release triggered by heparin-protamine may be potentiated by the release of PAF.

journal_name

Eur J Pharmacol

authors

Aïssa J,Nathan N,Arnoux B,Benveniste J

doi

10.1016/0014-2999(96)00069-6

subject

Has Abstract

pub_date

1996-04-29 00:00:00

pages

123-8

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(96)00069-6

journal_volume

302

pub_type

杂志文章
  • Characterization of [3H]thiocolchicoside binding sites in rat spinal cord and cerebral cortex.

    abstract::Thiocolchicoside, a semi-synthetic derivative of the naturally occurring compound colchicoside with a relaxant effect on skeletal muscle, has been found to displace both [3H]gamma-aminobutyric acid ([3H]GABA) and [3H]strychnine binding, suggesting an interaction with both GABA and strychnine-sensitive glycine receptor...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00371-4

    authors: Balduini W,Cimino M,Depoortere H,Cattabeni F

    更新日期:1999-07-02 00:00:00

  • The relationship between morphine, aspartic acid and L-asparaginase in rats.

    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

    authors: Koyuncuoğlu H,Keyer-Uysal M,Berkman K,Güngör M,Genç EM

    更新日期:1979-12-20 00:00:00

  • From vasotocin to stress and cognition.

    abstract::Sex and stress hormones coordinate experience and behaviour with physiological regulations. In the brain the sex hormones act to promote the repertoire of affiliative and reproductive behaviours. Stress hormones target in particular brain circuits underlying emotional arousal and cognition. To exert these actions the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2009.10.017

    authors: de Kloet ER

    更新日期:2010-01-10 00:00:00

  • Targeting CD52 does not affect murine neuron and microglia function.

    abstract::The humanized anti-CD52 antibody alemtuzumab is successfully used in the treatment of multiple sclerosis (MS) and is thought to exert most of its therapeutic action by depletion and repopulation of mainly B and T lymphocytes. Although neuroprotective effects of alemtuzumab have been suggested, direct effects of anti-C...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.172923

    authors: Ellwardt E,Vogelaar CF,Maldet C,Schmaul S,Bittner S,Luchtman D

    更新日期:2020-03-15 00:00:00

  • GR127935 acts as a partial agonist at recombinant human 5-HT1D alpha and 5-HT1D beta receptors.

    abstract::In this study we have investigated the functional activity of GR127935 (2-methyl-1,2,4 oxadiazol-3-yl)-biphenyl-[4-carboxylic acid 4-methoxy-3-(4-methyl-piperazine-1-yl]-amide) at human 5-HT1D alpha and 5-HT1D beta receptors which have been expressed in a Chinese Hamster Ovary (CHO) cell line. Using [35S] GTP gamma S ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00579-1

    authors: Watson JM,Burton MJ,Price GW,Jones BJ,Middlemiss DN

    更新日期:1996-10-31 00:00:00

  • On the ability of choline and its analogues to interact with muscarinic cholinergic receptors in the rat brain.

    abstract::Choline displaced [3H]QNB binding from rat brain muscarinic receptors competitively, (Ki = 460 microM) but it was only 1/1000th as potent as ACh. Deanol was an extremely weak displacer of [3H]QNB binding while hemicholinium-3 was 50 times more potent than choline. Although brain levels of choline are well below its Ki...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(79)90012-8

    authors: Speth RC,Yamamura HI

    更新日期:1979-09-15 00:00:00

  • Ca2+ dependence of the amphetamine, nomifensine, and Lu 19-005 effect on in vivo dopamine transmission.

    abstract::The present in vivo microdialysis study examined the role of vesicular- and carrier-mediated mechanisms underlying dopamine (DA) release, uptake and metabolism in halothane-anaesthetized rats. Omission of calcium (Ca2+) from the dialysis perfusing medium, thereby reducing the concentration of Ca2+ in the striatal micr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90067-8

    authors: Hurd YL,Ungerstedt U

    更新日期:1989-07-18 00:00:00

  • Effect of uncouplers of oxidative phosphorylation on transmitter release in dystrophic mice.

    abstract::Intracellular recording was used to study the effect of uncouplers of oxidative phosphorylation on miniature endplate potentials (m.e.p.p.s) in skeletal muscles from dystrophic mice and their clinically normal littermates. Control m.e.p.p. frequency in muscles from dystrophic mice was not significantly different from ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90637-1

    authors: Kelly S,Morgan G,Smith J

    更新日期:1988-02-16 00:00:00

  • Effect of P-glycoprotein modulators on the human extraneuronal monoamine transporter.

    abstract::The aim of this work was to investigate the effect of P-glycoprotein modulators on human extraneuronal monoamine transporter (EMT)-mediated transport. The experiments were performed using a cell line from human embryonic kidney (HEK293 cells) stably transfected with pcDNA3hEMT (293(hEMT)), or with pcDNA3 alone (293(co...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01055-x

    authors: Martel F,Keating E,Azevedo I

    更新日期:2001-06-22 00:00:00

  • Antitussive effects of Ca2+ channel antagonists.

    abstract::The effects of Ca2+ channel antagonists on the capsaicin-induced cough reflex in guinea pigs were studied. Intraperitoneal injection of nifedipine, verapamil and flunarizine in doses that ranged from 0.3 to 3.0 mg/kg decreased the number of coughs in a dose-dependent manner. These Ca2+ channel antagonists exhibited an...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90072-c

    authors: Kamei J,Kasuya Y

    更新日期:1992-02-25 00:00:00

  • Differential effects of sulindac on renal hemodynamics and function in the rat.

    abstract::Renal hemodynamics were studied using an electromagnetic perivascular flow sensor in anesthetized rats injected i.v. with vehicle, 5 or 10 mg/kg body weight (b.w.) sulindac. No hemodynamic changes occurred with vehicle (n = 6), but mean arterial pressure was significantly decreased (by 15 mmHg) with sulindac (n = 12)....

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)00178-7

    authors: Kramp RA,Caron N,Genard J,Lejeune C,Gulbis E,Herman A

    更新日期:1997-07-09 00:00:00

  • Methylhexaneamine causes tachycardia and pressor responses indirectly by releasing noradrenaline in the rat.

    abstract::We have investigated the mode of cardiovascular action of the stimulant methylhexaneamine (MHA) in terms of direct or indirect adrenergic actions in anaesthetised rats. Male and female rats were anaesthetised with pentobarbitone and pressor (changes in diastolic blood pressure) and cardioaccelerator responses to MHA w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.10.047

    authors: Alsufyani HA,Docherty JR

    更新日期:2019-01-15 00:00:00

  • Pharmacological blockade of brain alpha1-adrenoceptors as measured by ex vivo [3H]prazosin binding is correlated with behavioral immobility.

    abstract::The present studies examined the relationship between the blockade of central alpha1-adrenoceptors, as measured by ex vivo binding of [3H]prazosin in the cerebral cortex and the inhibition of behavioral activation to a mildly novel environment (cage change). It was found that intraventricular (i.v.t.) terazosin, a sal...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01003-2

    authors: Stone EA,Rosengarten H,Lin Y,Quartermain D

    更新日期:2001-05-25 00:00:00

  • Cannabinoid receptor antagonism and inverse agonism in response to SR141716A on cAMP production in human and rat brain.

    abstract::The effects of cannabinoid drugs on cAMP production were examined in mammalian brain. The cannabinoid receptor agonist (R)-(+)-[2,3-dihydro-5-methyl-3-[(4-morpholinyl)methyl]pyrrolo[1,2,3,-d,e-1,4-benzoxazin-6-yl]-(1-naphthalenyl) methanone (WIN55,212-2) decreased forskolin-induced cAMP accumulation in a concentration...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01575-3

    authors: Mato S,Pazos A,Valdizán EM

    更新日期:2002-05-17 00:00:00

  • Human and rat alveolar macrophages express multiple EDG receptors.

    abstract::Endothelial differentiation gene (EDG) receptors are a new family of eight G protein-coupled receptors for the lysophospholipids lysophosphatitic acid and sphingosine-1-phosphate. In the present experiments, the expression of EDG receptors in rat and human alveolar macrophages was studied by reverse transcription-poly...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01329-2

    authors: Hornuss C,Hammermann R,Fuhrmann M,Juergens UR,Racké K

    更新日期:2001-10-19 00:00:00

  • Contribution of dopaminergic and adenosinergic systems in the antinociceptive effect of p-chloro-selenosteroid.

    abstract::This study investigated the antinociceptive action of p-chloro-selenosteroid (PCS), administered by intragastric route (i.g.) to mice against acute models. The contribution of adenosinergic, dopaminergic, serotonergic, nitric oxide and opioid systems was investigated. It was evaluated if the administration of PCS trig...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.01.004

    authors: Marcondes Sari MH,Guerra Souza AC,Gonçalves Rosa S,Souza D,Dorneles Rodrigues OE,Wayne Nogueira C

    更新日期:2014-02-15 00:00:00

  • Pharmacological studies on the NOP and opioid receptor agonist PWT2-[Dmt1]N/OFQ(1-13).

    abstract::An innovative chemical strategy named peptide welding technology (PWT) has been developed for the facile synthesis of tetrabranched peptides. [Dmt1]N/OFQ(1-13)-NH2 acts as a universal agonist for nociceptin/orphanin FQ (N/OFQ) and classical opioid receptors. The present study investigated the pharmacological profile o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.11.026

    authors: Cerlesi MC,Ding H,Bird MF,Kiguchi N,Ferrari F,Malfacini D,Rizzi A,Ruzza C,Lambert DG,Ko MC,Calo G,Guerrini R

    更新日期:2017-01-05 00:00:00

  • Evidence for a 5-HT1D receptor-mediated hypothermic effect of the alpha 1-adrenoceptor agonist, SDZ NVI-085, in guinea-pigs.

    abstract::The alpha 1-adrenoceptor agonist, SDZ NVI-085 ((-)-(4aR,10aR)-3,4,4a,5,10,10a-hexahydro-6-methoxy-4- methyl-9-(methylthio)-2H-naphth[2,3-b]-1,4-oxazine.HCl; 1 mg/kg i.p.), decreased body temperature of guinea-pigs. Two 5-HT1D receptor antagonists, GR127935 (N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00526-q

    authors: Kalkman HO,Neumann V

    更新日期:1995-10-24 00:00:00

  • Meta-chlorophenylpiperazine induced changes in locomotor activity are mediated by 5-HT1 as well as 5-HT2C receptors in mice.

    abstract::1-(Meta-chloro)phenylpiperazine (m-CPP) is a 5-HT receptor agonist which has been purported to be relatively selective for the 5-HT2C receptor. In particular, the hypolocomotion produced by m-CPP has been suggested to be mediated by 5-HT2C receptors. m-CPP binds with high affinity to 5-HT1 as well as 5-HT2 receptors, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01474-x

    authors: Gleason SD,Shannon HE

    更新日期:1998-01-12 00:00:00

  • Tachykinin NK(2) receptors facilitate acetylcholine release from guinea-pig isolated trachea.

    abstract::The release of newly synthesised [3H]acetylcholine was evoked by electrical field stimulation (5 Hz, 600 pulses) of epithelium-deprived guinea-pig trachea strips after sensory neuropeptides depletion with 3 microM capsaicin. The selective tachykinin NK(2) receptor agonist [betaAla(8)]neurokinin A-(4-10) increased in a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00199-0

    authors: D'Agostino G,Erbelding D,Kilbinger H

    更新日期:2000-05-12 00:00:00

  • The effect of a Titanocene Dichloride derivative, Ti IV (C5H5)(2) NCS(2), on the haematopoietic response of Ehrlich tumour-bearing mice.

    abstract::The effects of the [Ti IV (C(5)H(5))(2) NCS(2)] metallocene (BCDT), a Titanocene Dichloride derivative, on the growth and differentiation of granulocyte-macrophage progenitor cells [colony-forming unit-granulocyte-macrophage (CFU-GM)] and bone marrow cellularity in normal and Ehrlich ascites tumour-bearing mice were s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)01411-5

    authors: Valadares MC,Queiroz ML

    更新日期:2002-03-29 00:00:00

  • Molecular biology of the dopamine receptors.

    abstract::Because of their importance in pathophysiology, the dopamine receptors have been the subjects of intense pharmacological and physiological research. Their structures have remained mostly unknown until recently with the application of molecular biological approaches. The cloning of the first dopamine receptor, the D2 r...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/0922-4106(91)90001-x

    authors: Civelli O,Bunzow JR,Grandy DK,Zhou QY,Van Tol HH

    更新日期:1991-08-14 00:00:00

  • Effect of Ca2+ entry blockers on myosin light-chain kinase and protein kinase C.

    abstract::Thirteen Ca2+ entry blockers were compared with respect to their inhibitory effects on the activity of smooth muscle myosin light-chain kinase and smooth muscle protein kinase C, and the Ca2+-induced contraction of basilar artery rings. Comparison of the IC50 values obtained for these compounds, suggests that with the...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90410-x

    authors: Schächtele C,Wagner B,Rudolph C

    更新日期:1989-04-12 00:00:00

  • Effect of vascular smooth muscle relaxants on the protein kinase C-mediated contraction in the rat pulmonary artery.

    abstract::In the rat pulmonary artery, phorbol 12,13-dibutyrate induces a contraction due to the activation of the protein kinase C. We investigated the sensitivity of this protein kinase C-mediated contraction to a variety of vascular smooth muscle relaxants. Pretreatment of rat pulmonary artery with relaxant compounds altered...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90432-h

    authors: Savineau JP,Gonzalez De La Fuente P,Marthan R

    更新日期:1993-11-09 00:00:00

  • Sustained 5-hydroxytryptamine release-inhibitory and anxiolytic-like action of the partial 5-HT1A receptor agonist, buspirone, after prolonged chronic administration.

    abstract::The effect of prolonged administration of high doses of buspirone on its 5-hydroxytryptamine (5-HT) release-inhibitory and anxiolytic-like properties was investigated. The 5-HT release-inhibitory effect of a challenge dose of buspirone (0.5 mg/kg, s.c.) was identical in rats chronically treated with vehicle or buspiro...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90977-p

    authors: Söderpalm B,Lundin B,Hjorth S

    更新日期:1993-08-03 00:00:00

  • Relaxing effects of adenosine in coronary artery in calcium-free medium.

    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

    authors: Ramagopal MV,Nakazawa M,Mustafa SJ

    更新日期:1989-01-02 00:00:00

  • Effects of nitric oxide synthase inhibitor N(G)-nitro-L-arginine methyl ester on phencyclidine-induced effects in rats.

    abstract::Phencyclidine (PCP) is widely used as an animal model of schizophrenia. In rats, acute PCP treatment increased locomotor activity and induced stereotyped behaviours consisting of head weaving, turning and backpedalling. PCP had differential regional effects on c-fos expression in rat brain, suggesting different patter...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00830-x

    authors: Bujas-Bobanovic M,Robertson HA,Dursun SM

    更新日期:2000-12-01 00:00:00

  • Stimulation of P1-purinoceptors by ATP depends partly on its conversion to AMP and adenosine and partly on direct action.

    abstract::The effects of degradative enzymes and enzyme inhibitors were examined on the inhibitory actions of adenosine, AMP and ATP on atrial muscle and on the cholinergic responses of the ileum to transmural stimulation of the guinea-pig, in order to determine whether ATP responses are mediated by its breakdown products, AMP ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90511-9

    authors: Moody CJ,Meghji P,Burnstock G

    更新日期:1984-01-13 00:00:00

  • Endothelin ET(A) receptor antagonist reverses the inhibitory effect of platelet-derived growth factor on cytokine-induced nitric oxide production.

    abstract::Cytokines and cytokine-induced nitric oxide (NO) play important roles in inflammatory glomerular diseases, and both platelet-derived growth factor and transforming growth factor-beta inhibit cytokine-induced NO production. In this study, we demonstrated that a selective endothelin ET(A) receptor antagonist, BQ-485 (He...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00849-8

    authors: Hirahashi J,Nakaki T,Hishikawa K,Marumo T,Hayashi M,Saruta T

    更新日期:1999-01-15 00:00:00

  • Antinociceptive, brain-penetrating derivatives related to improgan, a non-opioid analgesic.

    abstract::The antinociceptive profile of selected histamine H(2) and histamine H(3) receptor antagonists led to the discovery of improgan, a non-brain-penetrating analgesic agent which does not act on known histamine receptors. Because no chemical congener of improgan has yet been discovered which has both antinociceptive and b...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.08.040

    authors: Hough LB,Nalwalk JW,Lu Q,Shan Z,Svokos K,Wentland MP,Montero MJ

    更新日期:2005-10-17 00:00:00