Endothelial P2Y receptors induce hyperpolarisation of vascular smooth muscle by release of endothelium-derived hyperpolarising factor.

Abstract:

:The effects of P2Y receptor agonists on smooth muscle membrane potential in isolated ring segments of rat mesenteric artery were examined by intracellular microelectrodes. In the presence of inhibitors of nitric oxide-synthase and cyclo-oxygenase, the selective P2Y1 receptor agonist adenosine 5'-O-thiodiphosphate (ADPbetaS) induced endothelium-dependent membrane hyperpolarisations, which were abolished by a combination of the K+ channel inhibitors charybdotoxin and apamin, providing direct evidence that ADPbetaS releases endothelium-derived hyperpolarising factor (EDHF). 2-MethylthioATP and ATP, each which stimulates both endothelial P2Y receptors and P2X receptors on the smooth muscle cells, also elicited hyperpolarisation, but only after desensitisation of P2X receptors with alphabeta-methylATP indicating that simultaneous activation of P2X receptors may counteract the action of EDHF. In conclusion, activation of endothelial P2Y receptors induce release of EDHF.

journal_name

Eur J Pharmacol

authors

Malmsjö M,Erlinge D,Högestätt ED,Zygmunt PM

doi

10.1016/s0014-2999(98)00848-6

subject

Has Abstract

pub_date

1999-01-08 00:00:00

pages

169-73

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(98)00848-6

journal_volume

364

pub_type

杂志文章
  • In vivo modulation of benzodiazepine receptor function after inhibition of endogenous gamma-aminobutyyric acid synthesis.

    abstract::The influence of decreased endogenous gamma-aminobutyric acid (GABA) concentration on benzodiazepine receptor function was studied in the brain of living baboons. Positron emission tomography and the radiotracer [11C]flumazenil combined with electroencephalography were used to determine the pharmacological properties ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)00004-6

    authors: Bottlaender M,Schmid L,Fuseau C,Fournier D,Brouillet E,Mazière M

    更新日期:1997-02-19 00:00:00

  • Chronic antidepressant administration fails to attenuate apomorphine-induced decreases in rat striatal dopamine metabolites.

    abstract::The responsiveness of the rat striatal dopamine (DA) receptor system to apomorphine (APO) was assessed after 10 days of antidepressant administration. Desipramine (DMI), dothiepin (DOTH), iprindole (IPR) and nomifensine (NOM) were administered intra-peritoneally, twice daily, to rats for 10 days and 42 h after the las...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90617-4

    authors: Diggory GL,Buckett WR

    更新日期:1984-10-15 00:00:00

  • Anti-inflammatory effect of dual nociceptin and opioid receptor agonist, BU08070, in experimental colitis in mice.

    abstract::Endogenous opioid and nociceptin systems are widely distributed in the gastrointestinal tract where they seem to play a crucial role in maintaining the intestinal homeostasis. The aim of our study was to assess whether activation of nociceptin (NOP) and µ-opioid (MOP) receptors by a mixed NOP/MOP receptor agonist, BU0...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.09.021

    authors: Zielińska M,Ben Haddou T,Cami-Kobeci G,Sałaga M,Jarmuż A,Padysz M,Kordek R,Spetea M,Husbands SM,Fichna J

    更新日期:2015-10-15 00:00:00

  • Intratracheal dosing with disodium cromoglycate inhibits late asthmatic response by attenuating eicosanoid production in guinea pigs.

    abstract::Disodium cromoglycate is an anti-asthmatic drug that has mast cell-stabilizing effects and other anti-inflammatory effects. However, the mechanisms of its anti-inflammatory effects are unclear. In this study, we evaluated effects of disodium cromoglycate on eosinophilia, early and late asthmatic responses, and product...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.06.033

    authors: Nabe T,Yamamoto M,Suga M,Kohno S

    更新日期:2004-08-16 00:00:00

  • Reversal by [D-Ala2,D-Leu5]enkephalin of the dopamine transporter loss caused by methamphetamine.

    abstract::A single administration of 40 mg/kg (i.p.) of methamphetamine caused a loss of dopamine transporter in the striatum of albino Swiss (CD-1) mouse for at least 3 weeks. The administration of a single dose of [D-Ala2,D-Leu5]enkephalin (DADLE) (18 mg/kg, i.p.), given at day 14 after the administration of methamphetamine, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00240-x

    authors: Tsao LI,Cadet JL,Su TP

    更新日期:1999-05-21 00:00:00

  • Locus of action of Ni2+ on histamine-induced inositol phosphate formation in brain slices and in HeLa cells.

    abstract::Histamine-induced [3H]inositol monophosphate ([3H]IP1) accumulation in slices of rat cerebral cortex and guinea-pig cerebral cortex and cerebellum was inhibited in a concentration-dependent manner by Ni2+ ions. The effect of Ni2+ on the concentration-response curve for histamine in rat cerebral cortex was consistent w...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90100-n

    authors: Arias-Montaño JA,Young JM

    更新日期:1993-05-15 00:00:00

  • Hypophysectomy does not prevent development of striatal dopamine receptor supersensitivity induced by repeated neuroleptic treatment.

    abstract::Hruska et al. (1980) reported that hypophysectomy prevented the onset of dopamine receptor supersensitivity. We have repeated this investigation administering haloperidol (0.75 mg/day) or sulpiride (2 X 15 mg/day) or saline for 17 days, followed by a 3 day drug washout period, to sham-operated or hypophysectomised rat...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(81)90006-6

    authors: Jenner P,Rupniak NM,Hall MD,Dyer R,Leigh N,Marsden CD

    更新日期:1981-11-19 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

  • Interaction of leukocytes and endotoxin with the plasmin and kinin systems.

    abstract::Leukocytes can generate a substance that, when added to some partially purified human kininogen, is capable of forming kinins. The addition of endotoxin or polystyrene latex particles to the incubated leukocytes doubled the amount of kinin generated. Certain preparations of kininogen, however, failed to allow kinin fo...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(75)90137-5

    authors: Miller RL,Webster ME,Melmon KL

    更新日期:1975-08-01 00:00:00

  • Antinociceptive effects of tetrahydrocannabinol side chain analogs: dependence upon route of administration.

    abstract::The role of flexibility of the alkyl side chain in the tetrahydrocannabinols to cannabinoid activity has been delineated in previous studies with side chain analogs of Delta(8)-tetrahydrocannabinol with double or triple bonds. This study investigated the site of antinociceptive action for these analogs through analysi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00259-4

    authors: Wiley JL,Patrick GS,Crocker PC,Saha B,Razdan RK,Martin BR

    更新日期:2000-06-02 00:00:00

  • Solubilization and characterization of the kappa-opioid receptor type from guinea-pig cerebellum.

    abstract::The kappa-opioid receptor (kappa Op) from guinea-pig cerebellum membranes has been solubilized in an active form and in good yield (30-40%) with digitonin in 10 mM Tes-KOH buffer, pH 7.4. [3H]Bremazocine (KD = 1.1 nM in the soluble extract) was used to monitor the binding and hydrodynamic characteristics of the digito...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90755-8

    authors: Francés B,Moisand C,Meunier JC

    更新日期:1988-05-20 00:00:00

  • MicroRNA-301b promotes the proliferation and invasion of glioma cells through enhancing activation of Wnt/β-catenin signaling via targeting Glypican-5.

    abstract::Accumulating evidence has suggested that Glypican-5 (GPC5) is a tumor suppressor gene in many types of cancers. However, whether GPC5 is involved in glioma remains unknown. This study was designed to explore the expression, biological function and regulatory mechanism of GPC5 in glioma. Our results demonstrated that G...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2019.03.057

    authors: Hong X,Zhang Z,Pan L,Ma W,Zhai X,Gu C,Zhang Y,Bi X,Huang W,Pei H,Liu Z

    更新日期:2019-07-05 00:00:00

  • Anti-tumor necrosis factor agent PEG-sTNFRI improves the growth hormone/insulin-like growth factor-I system in adjuvant-induced arthritic rats.

    abstract::Adjuvant-induced arthritis is associated with body weight loss and decreased pituitary growth hormone (GH) and hepatic insulin-like growth factor-I (IGF-I) synthesis. Cytokines as tumor necrosis factor (TNF) mediate wasting associated with chronic inflammation. The aim of this study was to analyse whether the inhibiti...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.02.035

    authors: Granado M,Priego T,Martín AI,Vara E,López-Calderón A,Angeles Villanúa M

    更新日期:2006-04-24 00:00:00

  • Residues stabilizing the heme moiety of the nitric oxide sensor soluble guanylate cyclase.

    abstract::Soluble guanylate cyclase, a heterodimer consisting of an alpha- and a heme-containing beta-subunit, is the major receptor for the biological messenger nitric oxide (NO) and is involved in various signal transduction pathways. The heme moiety of the enzyme is bound between the axial heme ligand histidine(105) and the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.02.046

    authors: Schmidt PM,Rothkegel C,Wunder F,Schröder H,Stasch JP

    更新日期:2005-04-18 00:00:00

  • Chronic clonidine treatment and its withdrawal: effects on blood pressure and catecholamine synthesizing enzymes in brain-stem nuclei.

    abstract::We have studied the effects of withdrawal from chronic clonidine treatment in the adult male spontaneously hypertensive rat (SHR). SHR received clonidine, 0.1 mg X kg-1 X day-1 i.v. for 10 days. Clonidine was delivered via osmotic minipumps. After 7 days of treatment there was a 16.5 +/- 2.5 mm Hg fall in mean arteria...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90397-3

    authors: Atkinson J,Lambas-Senas L,Parker M,Boillat N,Luthi P,Sonnay M,Seccia M,Renaud B

    更新日期:1986-02-11 00:00:00

  • Salvianolic acid B regulates macrophage polarization in ischemic/reperfused hearts by inhibiting mTORC1-induced glycolysis.

    abstract::Macrophages play important roles in the healing and remodeling of cardiac tissues after myocardial ischemia/reperfusion (MI/R) injury. Here we investigated the potential effects of salvianolic acid B (SalB), one of the abundant and bioactive compounds extracted from Chinese herb Salvia Miltiorrhiza (Danshen), on macro...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.172916

    authors: Zhao M,Li F,Jian Y,Wang X,Yang H,Wang J,Su J,Lu X,Xi M,Wen A,Li J

    更新日期:2020-03-15 00:00:00

  • The effects of selective cyclooxygenase-2 inhibitors, celecoxib and rofecoxib, on experimental colitis induced by acetic acid in rats.

    abstract::Several mediators may be involved in the pathogenesis of inflammatory bowel disease, as well as in experimental colitis. The present work was conducted to investigate the effects of the two selective cyclooxygenase-2 inhibitors, celecoxib and rofecoxib, on experimentally induced colitis in rats. Rectal instillation of...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.11.036

    authors: El-Medany A,Mahgoub A,Mustafa A,Arafa M,Morsi M

    更新日期:2005-01-10 00:00:00

  • Animal models of rheumatoid arthritis: How informative are they?

    abstract::Animal models of arthritis are widely used to de-convolute disease pathways and to identify novel drug targets and therapeutic approaches. However, the high attrition rates of drugs in Phase II/III rates means that a relatively small number of drugs reach the market, despite showing efficacy in pre-clinical models. Th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2015.03.047

    authors: McNamee K,Williams R,Seed M

    更新日期:2015-07-15 00:00:00

  • Bioallethrin causes permanent changes in behavioural and muscarinic acetylcholine receptor variables in adult mice exposed neonatally to DDT.

    abstract::We recently reported changes in the density of muscarinic acetylcholine receptors in cerebral cortex of mice treated neonatally with DDT (1,1,1-trichloro-2,2-bis(p-chlorophenyl)-ethane) and receiving bioallethrin as adults. We also found behavioural aberrations in adult mice treated with bioallethrin, whether neonatal...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0926-6917(95)00012-7

    authors: Johansson U,Fredriksson A,Eriksson P

    更新日期:1995-07-01 00:00:00

  • Characterization of C-terminal tail determinants involved in CRTH2 receptor trafficking: identification of a recycling motif.

    abstract::The molecular mechanisms regulating the trafficking of the CRTH2 receptor are poorly understood. In the present study, we characterize C-terminal tail determinants involved in the agonist-induced trafficking of the CRTH2 receptor for prostaglandin D(2). Our results showed that progressive deletion of C-terminal tail r...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.12.022

    authors: Roy SJ,Parent A,Gallant MA,de Brum-Fernandes AJ,Stanková J,Parent JL

    更新日期:2010-03-25 00:00:00

  • Galanin/GALP and galanin receptors: role in central control of feeding, body weight/obesity and reproduction?

    abstract::Scientific and commercial pharmacological interest in the role of galanin and galanin receptors in the regulation of food intake, energy balance, and obesity has waned recently, following initial enthusiasm during the 1980-1990s. It has been replaced by efforts to understand the role of newly discovered peptide system...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(02)01433-4

    authors: Gundlach AL

    更新日期:2002-04-12 00:00:00

  • Electrophysiological effects of dopamine autoreceptor antagonists, (+)-AJ 76 and (+)-UH 232.

    abstract::The weak aminotetralin stimulants, (+)-AJ 76, cis-(+)-5-methoxy-1-methyl-2-(n-propylamino)tetralin and (+)-UH 232, cis-(+)-5-methoxy-1-methyl-2-(di-n-propylamino)tetralin, were tested for their effects on firing rates of dopaminergic (DA) neurons in the substantia nigra pars compacta (SNPC). (+)-AJ 76 and (+)-UH 232 a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90280-j

    authors: Piercey MF,Lum JT

    更新日期:1990-07-03 00:00:00

  • A novel anticancer agent Broussoflavonol B downregulates estrogen receptor (ER)-α36 expression and inhibits growth of ER-negative breast cancer MDA-MB-231 cells.

    abstract::Estrogen receptor (ER)-negative breast cancers are aggressive and unresponsive to antiestrogens, and current therapeutic modalities for ER-negative breast cancer patients are usually associated with strong toxicity and side effects. Less toxic and more effective targeted therapies are urgently needed to treat this typ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.05.047

    authors: Guo M,Wang M,Deng H,Zhang X,Wang ZY

    更新日期:2013-08-15 00:00:00

  • Influence of psychotomimetics and lisuride on synaptosomal dopamine release in the nucleus accumbens of rats.

    abstract::In superfusion experiments with a crude synaptosomal fraction from the nucleus accumbens of rats, lysergic acid diethylamide, mescaline and N,N-dimethyltryptamine (representing different chemical classes of psychotomimetics) produced a concentration-related inhibition of K+-evoked [3H]dopamine release whereas spontane...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90140-1

    authors: Hetey L,Schwitzkowsky R,Oelssner W

    更新日期:1983-09-30 00:00:00

  • FMS-like tyrosine kinase 3 (FLT3) inhibitors: Molecular docking and experimental studies.

    abstract::Activating mutations in FMS-like tyrosine kinase 3 (FLT3) occur in 25% of acute lymphoid and 30% of acute myeloid leukaemia cases. Therefore, FLT3 is a potential therapeutic target for small molecule kinase inhibitors. In this study, protein-ligand interactions between FLT3 and kinase inhibitors (CEP701, PKC412, sunit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.02.048

    authors: Mashkani B,Tanipour MH,Saadatmandzadeh M,Ashman LK,Griffith R

    更新日期:2016-04-05 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

  • Ligand affinities at recombinant N-methyl-D-aspartate receptors depend on subunit composition.

    abstract::The ligand preferences of recombinant NR1 homomeric and NR1-NR2 heteromeric NMDA receptors were examined by homogenate binding assay. The binding affinities for most ligands were similar to those reported for native NMDA receptors. The order of affinity for [3H]glutamate was NR1-NR2B > NR1-NR2A approximately NR1-NR2D ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90058-2

    authors: Laurie DJ,Seeburg PH

    更新日期:1994-08-16 00:00:00

  • Alpha 1-adrenoceptor stimulation increases intracellular pH and Ca2+ in cardiomyocytes through Na+/H+ and Na+/Ca2+ exchange.

    abstract::The effects of alpha 1-adrenergic stimulation on intracellular pH (pHi) and Ca2+ concentration ([Ca2+]i) were investigated in isolated rat cardiomyocytes with fluorescence dyes, BCECF and fura-2, respectively. In the presence of 5 or 25 mM HCO3- norepinephrine (NE) increased pHi in a dose-dependent manner. Intracellul...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)94057-5

    authors: Iwakura K,Hori M,Watanabe Y,Kitabatake A,Cragoe EJ Jr,Yoshida H,Kamada T

    更新日期:1990-09-04 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

  • AMP-activated kinase relaxes agonist induced contractions in the mouse aorta via effects on PKC signaling and inhibits NO-induced relaxation.

    abstract::Adenosine monophosphate activated kinase (AMPK), a regulator of cellular metabolism, has been shown to relax arterial smooth muscle via endothelium-dependent and independent mechanisms. We have examined the role of AMPK in different smooth muscles using the activating compound, 5-amino-4-imidazolecarboxamide riboside-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.07.025

    authors: Davis B,Rahman A,Arner A

    更新日期:2012-11-15 00:00:00