ETB receptor antagonist, IRL 1038, selectively inhibits the endothelin-induced endothelium-dependent vascular relaxation.

Abstract:

:In isolated rat aorta, endothelin-1 induced contractions at lower concentrations than endothelin-3. The contractile effects were augmented by removing the endothelium. In contrast, endothelium-1 and endothelin-3 at similar concentrations induced endothelium-dependent relaxation in norepinephrine-stimulated aorta. IRL 1038 ([Cys11,Cys15]endothelin-1(11-21); 3 microM) augmented the contractile effects of endothelins only in the presence of the endothelium. IRL 1038 (0.3-3 microM) inhibited the endothelium-dependent relaxation induced by endothelins but not by carbachol. IRL 1038 itself did not change muscle tension. These results suggest that IRL 1038 is a novel antagonist of the ETB receptor responsible for the release of relaxing factor from the vascular endothelium.

journal_name

Eur J Pharmacol

authors

Karaki H,Sudjarwo SA,Hori M,Sakata K,Urade Y,Takai M,Okada T

doi

10.1016/0014-2999(93)90112-u

subject

Has Abstract

pub_date

1993-02-16 00:00:00

pages

371-4

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(93)90112-U

journal_volume

231

pub_type

杂志文章
  • Contractile actions of imidazoline alpha-adrenoceptor agonists and effects of noncompetitive alpha1-adrenoceptor antagonists in human vas deferens.

    abstract::The contractile actions of imidazoline alpha-adrenoceptor agonists were investigated in human vas deferens longitudinal and circular muscle. The effects of phenoxybenzamine were studied in comparison to dibenamine and SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo[2,2,2]octa-2,5-dienylcarbonyl-2-piperazine)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(03)01346-3

    authors: Amobi N,Guillebaud J,Kaisary A,Lloyd-Davies RW,Turner E,Smith IC

    更新日期:2003-02-21 00:00:00

  • Modification of hepatic cytochrome P450 profile by cocaine-induced hepatotoxicity in DBA/2 mouse.

    abstract::Previous studies in our laboratory have shown that a hepatotoxic dose of cocaine increases coumarin 7-hydroxylase activity in male DBA/2 mouse liver. In the present study, the dose- and time-dependent responses of the hepatic CYP2A4/5 complex to cocaine-induced liver damage were studied. Cocaine increased CYP2A4/5 lev...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0926-6917(94)90026-4

    authors: Pellinen P,Stenbäck F,Raunio H,Pelkonen O,Pasanen M

    更新日期:1994-11-01 00:00:00

  • Targeting different angiogenic pathways with combination of curcumin, leflunomide and perindopril inhibits diethylnitrosamine-induced hepatocellular carcinoma in mice.

    abstract::No effective chemopreventive agent has been approved against hepatocellular carcinoma (HCC) to date. Since HCC is one of the hypervascular solid tumors, blocking angiogenesis represents an intriguing approach to HCC chemoprevention. The aim of the current study was to examine the combined effect of the anti-angiogenic...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.11.022

    authors: Nasr M,Selima E,Hamed O,Kazem A

    更新日期:2014-01-15 00:00:00

  • Blood serum profiling of the rat spinal nerve ligation model using ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry.

    abstract::Peripheral nerve injury, which gives rise to persistent chronic pain, has become an area of intense research activity, largely because it represents a disorder with a high unmet medical need. In this study, serum biomarkers of the spinal nerve ligation model were successfully investigated with the metabolomic method. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.03.079

    authors: Mao YF,Liu XR,Liao XZ,Lv YH,Xu H,Deng XM,Yan SK,Xiong YC,Zhang WD

    更新日期:2009-08-01 00:00:00

  • Adenosine A2A receptor stimulation enhances striatal extracellular glutamate levels in rats.

    abstract::The influence of CGS 21680, an adenosine A2A receptor agonist, on striatal glutamate extracellular levels was tested in a microdialysis study in rats. CGS 21680 (10 mu M), infused intrastriatally through the microdialysis probe, greatly enhanced glutamate extracellular levels. These results show that striatal adenosin...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00679-6

    authors: Popoli P,Betto P,Reggio R,Ricciarello G

    更新日期:1995-12-12 00:00:00

  • Phorbol ester regulates stimulatory and inhibitory pathways of the hormone-sensitive adenylate cyclase system in rat reticulocytes.

    abstract::Treatment of rat reticulocytes with tetradecanoyl phorbol acetate (TPA), a tumor-promoting phorbol ester which activates protein kinase C, resulted in an about 50% decrease in the stimulation of adenylate cyclase activity by a subsequent challenge with a beta-adrenoceptor agonist. This phenomenon mimics agonist-induce...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90797-2

    authors: Yamashita A,Kurokawa T,Une Y,Ishibashi S

    更新日期:1988-07-07 00:00:00

  • Inhibition of store-operated Ca2+ entry channels and K+ channels by caffeic acid phenethylester in T lymphocytes.

    abstract::The increase of cytoplasmic Ca2+ concentration (Delta[Ca2+]c) in response to antigenic stimulation is a critical step of signals activating immune responses. In addition, the voltage-gated K+ channels (Kv) in T lymphocytes draw attention as an effective target of immune-modulation. Caffeic acid phenethyl ester (CAPE),...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.04.004

    authors: Nam JH,Shin DH,Zheng H,Kang JS,Kim WK,Kim SJ

    更新日期:2009-06-10 00:00:00

  • Extract of kava (Piper methysticum) and its methysticin constituents protect brain tissue against ischemic damage in rodents.

    abstract::The purpose of the present study was to test whether kava extract and its constituents kawain, dihydrokawain, methysticin, dihydromethysticin and yangonin provide protection against ischemic brain damage. To this end, we used a model of focal cerebral ischemia in mice and rats. Ischemia was induced by microbipolar coa...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90037-5

    authors: Backhauss C,Krieglstein J

    更新日期:1992-05-14 00:00:00

  • The antinociceptive effect induced by FR140423 is mediated through spinal 5-HT2A and 5-HT3 receptors.

    abstract::The involvement of 5-HT receptors in the antinociceptive effect of FR140423, 3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4-(methylsulfinyl)phenyl]py razole, was investigated in mice by means of the tail-pinch test. The antinociceptive effect of FR140423 injected i.t. was completely abolished by co-administration of the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00832-3

    authors: Ochi T,Goto T

    更新日期:2000-12-08 00:00:00

  • Effect of chronic moderate ethanol consumption on heart brain natriuretic peptide.

    abstract::There is experimental evidence indicating that chronic moderate ethanol consumption delays the age-dependent increase in blood pressure. Since the brain natriuretic peptide (BNP) is a potent hypotensive hormone, the effect of chronic ethanol treatment on the heart BNP system was investigated, using spontaneously hyper...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00644-9

    authors: Guillaume P,Jankowski M,Gutkowska J,Gianoulakis C

    更新日期:1996-11-28 00:00:00

  • Gastrodin inhibits the activity of acid-sensing ion channels in rat primary sensory neurons.

    abstract::Acid-sensing ion channels (ASICs), a family of proton-gated cation channels, are believed to mediate pain caused by extracellular acidification. Gastrodin is a main bioactive constituent of the traditional herbal Gastrodia elata Blume, which has been widely used in Oriental countries for centuries. As an analgesic, ga...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.02.044

    authors: Qiu F,Liu TT,Qu ZW,Qiu CY,Yang Z,Hu WP

    更新日期:2014-05-15 00:00:00

  • Anorexigenic and electrophysiological actions of novel ghrelin receptor (GHS-R1A) antagonists in rats.

    abstract::Here we provide the first pharmacological exploration of the impact of acute central nervous system exposure to three recently developed ghrelin receptor (GHS-R1A) ligands on food intake and on the electrical activity of the target cells for ghrelin in the hypothalamus. Central (i.c.v) injection of GHS-R1A antagonists...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2009.03.066

    authors: Salomé N,Haage D,Perrissoud D,Moulin A,Demange L,Egecioglu E,Fehrentz JA,Martinez J,Dickson SL

    更新日期:2009-06-10 00:00:00

  • N-(3-acetylaminophenyl)piperazine hydrochloride (BEA 1654), a putative 5-HT1 agonist, causes constriction of arteriovenous anastomoses and dilatation of arterioles.

    abstract::Using 3H-ligands and radioactive microspheres we studied the binding characteristics and the effects on the distribution of carotid arterial blood flow of n-(3-acetylaminophenyl)piperazine hydrochloride (BEA 1654). The compound had a Ki value of 32 nM (5-HT: 8 nM) on 5-HT1 but no or very weak affinity for 5-HT2, alpha...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90259-6

    authors: Verdouw PD,Jennewein HM,Mierau J,Saxena PR

    更新日期:1985-01-08 00:00:00

  • In vitro inhibition of allergic histamine release by calcium antagonists.

    abstract::The ability of calcium entry blockers to inhibit allergic histamine release from rabbit leukocytes was studied. Bepridil, verapamil, nifedipine, diltiazem and TMB-8 produced concentration-dependent inhibition of allergic histamine release from rabbit leukocytes. The calculated IC50s (microM) were as follows: verapamil...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90261-4

    authors: Chand N,Pillar J,Diamantis W,Sofia RD

    更新日期:1985-01-08 00:00:00

  • Antagonism of Ca2+-induced contractions of K+-depolarized smooth muscle by local anaesthetics.

    abstract::Drugs known to interact with Na+ channels were compared as antagonists of Ca2+-induced contractions of K+-depolarized taenia preparations from guinea-pig caecum. Tetracaine (apparent pA2 5.3 +/- 0.2), quinidine (5.2 +/- 0.1) quinine (5.1 +/- 0.1), d-propranolol (4.7 +/- 0.1), 1-propranolol (4.7 +/- 0.1), lignocaine (4...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90718-6

    authors: Spedding M,Berg C

    更新日期:1985-01-22 00:00:00

  • Activation of epithelial sodium channel in human middle ear epithelial cells by dexamethasone.

    abstract::The middle ear epithelium functions to maintain a fluid-free middle ear cavity. Dysfunction of the middle ear epithelial ion and fluid transport is implicated in the pathogenesis of fluid collection in the middle ear cavity, characteristic of otitis media with effusion. The efficacy of steroid therapy for the treatmen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.11.012

    authors: Son EJ,Kim SH,Park HY,Kim SJ,Yoon JH,Chung HP,Choi JY

    更新日期:2009-01-14 00:00:00

  • Ontogenesis of kappa-opioid receptors in rat brain using [3H]U-69593 as a binding ligand.

    abstract::The ontogenesis of kappa-opioid receptors has been studied in the postnatal period from day 5 to day 30 using the highly selective kappa-site ligand [3H]U-69593 in binding studies. Analyses of saturation curves revealed a marked increase in the binding capacities between day 5 and day 10 with no further increment in t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90157-2

    authors: Kitchen I,Kelly M,Viveros MP

    更新日期:1990-01-03 00:00:00

  • Selective inhibition of the inducible nitric oxide synthase by aminoguanidine.

    abstract::Overproduction of the free radical nitric oxide (NO) has been implicated in the pathogenesis of a variety of inflammatory and immunologically mediated diseases as well as complications of diabetes. In the present study we have demonstrated that aminoguanidine selectively inhibits the cytokine-inducible isoform of NO s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90357-n

    authors: Misko TP,Moore WM,Kasten TP,Nickols GA,Corbett JA,Tilton RG,McDaniel ML,Williamson JR,Currie MG

    更新日期:1993-03-16 00:00:00

  • The effects of dopamine receptor agents on naloxone-induced jumping behaviour in morphine-dependent mice.

    abstract::In the present study, the effects of dopamine receptor agonists and antagonists on naloxone-induced jumping in morphine-dependent mice were examined. Mice were rendered dependent as described in the methods section. Naloxone was injected to elicit jumping (as withdrawal sign). The first group received dopamine recepto...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02149-0

    authors: Zarrindast MR,Habibi M,Borzabadi S,Fazli-Tabaei S,Hossein Yahyavi S,Rostamin P

    更新日期:2002-09-20 00:00:00

  • A specific transcriptional response of yeast cells to camptothecin dependent on the Swi4 and Mbp1 factors.

    abstract::Topoisomerase I (Top1) is the specific target of the anticancer drug camptothecin (CPT) that interferes with enzyme activity promoting Top1-mediated DNA breaks and inhibition of DNA and RNA synthesis. To define the specific transcriptional response to CPT, we have determined the CPT-altered transcription profiles in y...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.12.002

    authors: Lotito L,Russo A,Bueno S,Chillemi G,Fogli MV,Capranico G

    更新日期:2009-01-28 00:00:00

  • Behavioral evidence for the involvement of gamma-aminobutyric acid in the actions of ethanol.

    abstract::Behavioral interactions between ethanol and GABA-mimetic and GABA antagonist drugs were evaluated by duration of narcosis and motor incoordination (inhibition of bar holding) in mice. Aminooxyacetic acid (AOAA), baclofen, and tetrahydroisoxazolopyridineol (THIP) (GABA mimetics) lengthened ethanol narcosis, while picro...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90607-6

    authors: Martz A,Deitrich RA,Harris RA

    更新日期:1983-04-22 00:00:00

  • Neurotoxicity of the meperidine analogue N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine on brain catecholamine neurons in the mouse.

    abstract::The effect of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (NMPTP) on central monoamine neurons in mice was investigated using histo- and biochemical techniques. NMPTP (2 X 10 mg/kg i.v.) produced a rapid and long-lasting reduction (-30%) of striatal dopamine, while the dopamine levels were only transiently reduced in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90521-1

    authors: Hallman H,Olson L,Jonsson G

    更新日期:1984-01-13 00:00:00

  • Further evidence for involvement of adenosine-5'-triphosphate in non-adrenergic non-cholinergic relaxation of the isolated rat duodenum.

    abstract::The nature of the inhbitory non-adrenergic non-cholinergic (NANC) neurotransmitter responsible for neurogenic relaxation of rat duodenum was studied with in vitro techniques. Adenosine 5'-triphosphate (ATP)(1 mM), gamma-aminobutyric acid (GABA, 1 mM), dimethylphenylpiperazinium (DMPP, 0.1 mM) and field stimulation (60...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(85)90088-3

    authors: Manzini S,Maggi CA,Meli A

    更新日期:1985-07-31 00:00:00

  • Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective.

    abstract::In order to identify new atypical antipsychotic drugs which are more selective for the human dopamine D4 receptor than for the human dopamine D2 (long) receptor, we tested enantiomer pairs of dopamine agonists and dopamine antagonists on the expressed proteins of these cloned receptors. The (+)-aporphines ((+)-N-propy...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90365-o

    authors: Seeman P,Van Tol HH

    更新日期:1993-03-16 00:00:00

  • Cytotrienin A, a translation inhibitor that induces ectodomain shedding of TNF receptor 1 via activation of ERK and p38 MAP kinase.

    abstract::Cytotrienin A, a member of the triene-ansamycin family, was initially identified to be an inducer of apoptosis and recently shown to be an inhibitor of translation that interferes with eukaryotic elongation factor 1A function. In human lung carcinoma A549 cells, cytotrienin A was found to inhibit more strongly the cel...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.05.072

    authors: Yamada Y,Taketani S,Osada H,Kataoka T

    更新日期:2011-09-30 00:00:00

  • Effects of adenosine receptor agonists and antagonists on audiogenic seizure-sensible DBA/2 mice.

    abstract::We have studied the effects of selective and non-selective adenosine receptor agonists and antagonists in audiogenic-seizure-sensitive DBA/2 mice, an animal model of generalized reflex epilepsy. With the exception of the adenosine A3 receptor agonist, N6-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine (IB-MECA), all th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00132-6

    authors: De Sarro G,De Sarro A,Di Paola ED,Bertorelli R

    更新日期:1999-04-29 00:00:00

  • Influence of peptides on reduced response of rats to electric footshock after acute administration of morphine.

    abstract::Acute treatment of rats with morphine (10 mg/kg) resulted in a marked reduction of motor response to inescapable electric footshock (EFS). Nalorphine (2mg/kg) antagonized this action of morphine. Pretreatment with synthetic ACTH 1-24 (10 IU) 60 min prior to testing also inhibited this morphine-induced reduction, where...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(75)90143-0

    authors: Gispen WH,Van Wimersma Greidanus TB,Waters-Ezrin C,Zimmermann E,Krivoy WA,De Wied D

    更新日期:1975-08-01 00:00:00

  • Neonatal damage to neocortex abolishes the anxiolytic action of diazepam in adult rats.

    abstract::A neonatal cerebral cortical lesion was made in rats and the effects of diazepam on ultrasonic isolation calls in pups and footshock-elicited ultrasonic distress calls in young adult rats were assessed. There was no indication that the cortical lesion influenced the production of the ultrasonic distress calls in eithe...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)00657-s

    authors: Naito H,Arishima K,Tonoue T

    更新日期:1995-01-16 00:00:00

  • p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors.

    abstract::The effects of a serotonin (5-HT) releasing drug, p-chloroamphetamine, on plasma glucose levels were investigated in rats. p-Chloroamphetamine elicited a significant hyperglycemia. The hyperglycemic effects of p-chloroamphetamine were completely prevented by the 5-HT synthesis inhibitor, p-chlorophenylalanine. Prior a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00639-6

    authors: Yamada J,Sugimoto Y,Yoshikawa T

    更新日期:1998-10-23 00:00:00

  • (+)-Cyclazosin, a selective alpha1B-adrenoceptor antagonist: functional evaluation in rat and rabbit tissues.

    abstract::To shed light on the discrepancy between reported binding and functional affinity and selectivity at alpha(1b/B)-adrenoceptors, the antagonist (+)-cyclazosin was reinvestigated in rat and rabbit tissues. It displayed a competitive antagonism at alpha(1A) and alpha(1D)-adrenoceptors of rat prostatic vas deferens and ao...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.08.044

    authors: Marucci G,Angeli P,Buccioni M,Gulini U,Melchiorre C,Sagratini G,Testa R,Giardinà D

    更新日期:2005-10-17 00:00:00