Irreversible beta-adrenoceptor blockade of atrial rate and tension responses.


:The competitive reversible beta-adrenoceptor antagonist activity of Ro 03-5255 [1-(5-acetylaminobenzfuran-2-yl)-2-isopropylaminoethanol] upon isoprenaline-induced increases of the rate and tension of guinea-pig isolated atria is described. The chlorinated derivative [Ro 03-7894; 1-[5-chloracetylaminobenzfuran-2-yl)-2-isopropyl-aminoethanol] in contrast exhibited concentration-dependent non-competitive irreversible blocking activity as measured by depression of the maximum responses which were not restored by a washout period that successfully reversed Ro 03-5255. When orciprenaline was used as a weak agonist of low efficacy, the maximum responses were depressed to a greater extent. The blockade by Ro 03-7894 was relatively specific for beta-adrenoceptors since it did not antagonize histamine or calcium chloride. The depression of the maximum responses to orciprenaline was reduced by the presence of sodium thiosulphate. Sodium thiosulphate was ineffective in reversing an established blockade. The blockade by Ro 03-7894 was therefore assumed to involve irreversible binding to the beta-adrenoceptor after conversion to an appropriate electrophilic ligand. The significance of this is discussed.


Eur J Pharmacol


Nicholson CD,Broadley KJ




Has Abstract


1978-12-01 00:00:00














  • Stereotyped behavior correlates better than ataxia with phencyclidine-receptor interactions.

    abstract::The interaction of phencyclidine, dexoxadrol, their analogs and stereoisomers with phencyclidine receptors was compared to their ability to induce stereotyped behavior and ataxia after i.c.v. administration to rats. The order of potency for binding to phencyclidine receptors revealed that among the stereoisomers of ph...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Contreras PC,Rice KC,Jacobson AE,O'Donohue TL

    更新日期:1986-02-11 00:00:00

  • Ifenprodil influences changes in mouse behaviour related to acute and chronic ethanol administration.

    abstract::The aim of the present study was to examine the influence of ifenprodil (a non-competitive NMDA receptor antagonist which also blocks 5-HT3 receptors and alpha1-adrenoceptors) on the effects of ethanol in the mouse in vivo and to elucidate the role of various receptors in these actions. The ethanol (4 g/kg i.p.)-induc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Malinowska B,Napiórkowska-Pawlak D,Pawlak R,Buczko W,Göthert M

    更新日期:1999-07-14 00:00:00

  • Central injection of CDP-choline suppresses serum ghrelin levels while increasing serum leptin levels in rats.

    abstract::In this study we aimed to test central administration of CDP-choline on serum ghrelin, leptin, glucose and corticosterone levels in rats. Intracerebroventricular (i.c.v.) 0.5, 1.0 and 2.0 µmol CDP-choline and saline were administered to male Wistar-Albino rats. For the measurement of serum leptin and ghrelin levels, b...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Kiyici S,Basaran NF,Cavun S,Savci V

    更新日期:2015-10-05 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


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

    更新日期:1996-10-31 00:00:00

  • A comparison of the vasodepressor effects of the cyclic effects of the cyclic endoperoxides PGG, and PGH2 with those of PGD2 and PGE2 in hypertensive and normotensive rats.

    abstract::The vasodepressor actions of the cyclic endoperoxides PGG2 and PGH2 were compared with those of their products PGD2 and PGE2 using anaesthetised normotensive and genetically hypertensive rats. Given into the aortic arch of normotensives PGE2 was approximately 6 times more potent than PGH2 and 11 times more potent tha...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Armstrong JM,Boura AL,Hamberg M,Samuelsson B

    更新日期:1976-10-01 00:00:00

  • The discriminative stimulus properties of cocaine: effects of BAY K 8644 and nimodipine.

    abstract::Calcium channel blockers appear to reduce the cardiac toxicity of cocaine and some stimulant-induced behaviors. The present experiment was designed to test whether the internal state induced by cocaine is altered by the calcium antagonist nimodipine. Substitution tests with the calcium agonist BAY K 8644 were also con...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Callahan PM,Cunningham KA

    更新日期:1990-09-04 00:00:00

  • The glutathione reductase inhibitor carmustine induces an influx of Ca2+ in PC12 cells.

    abstract::We studied the effects of carmustine (1,3-bis(2-chloroethyl)-1-nitrosourea) on the intracellular Ca(2+) concentration ([Ca(2+)](i)) in PC12 cells using fura-2 fluorescence imaging. Carmustine (100 microM) caused a delayed increase in [Ca(2+)](i) that developed within approximately 3 h. This effect was enhanced in cell...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Doroshenko N,Doroshenko P

    更新日期:2004-08-16 00:00:00

  • Decrease of recurrent and feed-forward inhibitions under high pressure of helium in rat hippocampal slices.

    abstract::The effect of high helium pressure on inhibitory synaptic transmission was studied in rat hippocampal slices with extracellular recordings. Both feed-forward and recurrent GABAergic inhibition were tested in the CA1 region with paired-pulse stimulation paradigms. The efficiency of both types of inhibition decreased un...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Zinebi F,Fagni L,Hugon M

    更新日期:1988-08-24 00:00:00

  • Acute delta 9-tetrahydrocannabinol exposure alters Ca2+ ATPase activity in neuroendocrine and gonadal tissues in mice.

    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


    authors: Dalterio SL,Bernard SA,Esquivel CR

    更新日期:1987-05-07 00:00:00

  • Protocatechuic acid from Alpinia oxyphylla promotes migration of human adipose tissue-derived stromal cells in vitro.

    abstract::Human adipose tissue-derived stromal cells (hADSCs) demonstrate promising potential in various clinical applications, including the transplantation to regenerate injured or degenerative tissues. The migration of engrafted hADSCs to the correct site of injure is essential for the curative effect of stem cell therapy. W...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wang H,Liu TQ,Guan S,Zhu YX,Cui ZF

    更新日期:2008-12-03 00:00:00

  • Gender difference in the role of endothelium-derived relaxing factors modulating renal vascular reactivity.

    abstract:UNLABELLED:This study analyzed the role of nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) in gender differences in the renal vascular reactivity of rats. Renal responses to vasoconstrictors and vasodilators were studied in isolated kidneys from male and female rats under basal conditions, after...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wangensteen R,Moreno JM,Sainz J,Rodríguez-Gómez I,Chamorro V,Luna Jde D,Osuna A,Vargas F

    更新日期:2004-02-23 00:00:00

  • 5-HT1A receptor knockout mice and mice overexpressing corticotropin-releasing hormone in models of anxiety.

    abstract::Pharmacological experiments have implicated a role for serotonin (5-HT)(1A) receptors in the modulation of anxiety. More recent is the interest in corticotropin-releasing hormone (CRH) system as a potential target for the treatment of anxiety disorders. However, selective pharmacological tools for the CRH system are l...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Groenink L,Pattij T,De Jongh R,Van der Gugten J,Oosting RS,Dirks A,Olivier B

    更新日期:2003-02-28 00:00:00

  • A possible mechanism of choleretic action of 3-(2,4,5-triethoxybenzoyl)-propionic acid (AA-149) in dogs.

    abstract::The choleretic action of 3-(2,4,5-triethoxybenzoyl)propionic acid (AA-149) was studied in anesthetized dogs. AA-149 produced a dose-dependent increase of the bile flow with both i.v. and intrajejunal administration of doses 1 mg/kg and higher. Biliary clearance of 14C-erythritol showed that AA-149 stimulated canalicul...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Satoh H,Kanno M,Maki Y

    更新日期:1978-03-01 00:00:00

  • Long-term oral nicotine administration reduces insulin resistance in obese rats.

    abstract::This study aimed to investigate the effect of long-term oral nicotine administration on insulin resistance in an animal model of obesity. Eight-week-old male Zucker fatty rats (ZFRs) were administered nicotine tartrate dihydrate (4.6 mg/kg/day) in the drinking water. The control group was pair-fed. The body weights an...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Liu RH,Mizuta M,Matsukura S

    更新日期:2003-01-01 00:00:00

  • Cardiac and hemodynamic effects of S(-)- and (R(+)-DPI 201-106 and of racemic DPI 201-106 in conscious dogs.

    abstract::The cardiac and hemodynamic effects of (+/-)-DPI 201-106 (0.6 mg/kg), S(-)-DPI (0.3 mg/kg), R(+)-DPI (0.3 mg/kg), and their vehicle were compared in chronically implanted conscious dogs. (+/-)-DPI and S(-)-DPI induced qualitatively and quantitatively similar effects, increasing LV dP/dt, cardiac output and stroke volu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Gérard JL,Berdeaux A,Giudicelli JF

    更新日期:1990-08-10 00:00:00

  • Unchanged cardiac angiotensin II levels accompany losartan-sensitive cardiac injury due to nitric oxide synthase inhibition.

    abstract::Chronic nitric oxide synthase (NOS) inhibition results in hypertension and myocardial injury. In a rapid and severe model of chronic NOS inhibition, we determined the role of angiotensin II in these effects by using angiotensin II receptor blockade and by measuring cardiac angiotensin II concentrations before and duri...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Verhagen AM,Hohbach J,Joles JA,Braam B,Boer P,Koomans HA,Gröne H

    更新日期:2000-07-21 00:00:00

  • Treatment of insulin resistance in diabetes mellitus.

    abstract::Insulin resistance is a condition in which the glycemic response to insulin is less than normal. The change in insulin sensitivity leads to several sets of responses. One set effects the beta cell and leads to its accelerated destruction and the development of diabetes mellitus. The other set generates a series of non...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Lebovitz HE,Banerji MA

    更新日期:2004-04-19 00:00:00

  • Effects of spinorphin and tynorphin on synaptic transmission in rat hippocampal slices.

    abstract::Spinorphin has been isolated from the bovine spinal cord as an endogenous inhibitor of enkephalin-degrading enzymes (aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase), and tynorphin has been synthesized as a more potent inhibitor of dipeptidyl aminopeptidase III. In this s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Yamazaki T,Honda M,Yamamoto Y,Hazato T,Ono H

    更新日期:2001-02-16 00:00:00

  • Turning behaviour following nigral injections of dopamine agonists and glycine.

    abstract::Glycine, ADTN and ergometrine, but not LSD, induced strong dose-related contraversive turning following unilateral microinjections into the substantia nigra (zona reticulata) of conscious rats. The responses to glycine and ADTN were blocked by low doses of systemically injected cis-Z-flupenthixol but were unaffected b...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Andrews CD,Woodruff GN

    更新日期:1982-10-22 00:00:00

  • A dose ratio comparison of the interaction between morphine and cyclazocine with naloxone in rhesus monkeys on the shock titration task.

    abstract::Dose-response curves for morphine (0.5-20 mg/kg) were obtained in 4 rhesus monkeys performing the discrete trials shock titration task. Naloxone (5-500 microgram/kg) uniformly produced a dose dependent, parallel shift of the morphine dose-response curves to right. Plots for the 4 animals of the Log (dose ratio--1) ver...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Yaksh TL,Rudy TA

    更新日期:1977-11-15 00:00:00

  • Differentiation-inducing factor-1-induced growth arrest of K562 leukemia cells involves the reduction of ERK1/2 activity.

    abstract::The differentiation-inducing factor-1 (DIF-1) is a signal molecule that induces stalk cell differentiation in the cellular slime mold Dictyostelium discoideum. In addition, DIF-1 is a potent antileukemic agent that induces growth arrest in K562 cells. In this study, we investigated the mechanism of action of DIF-1 in ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Akaishi E,Narita T,Kawai S,Miwa Y,Sasaguri T,Hosaka K,Kubohara Y

    更新日期:2004-02-06 00:00:00

  • Effects of alpha-adrenoceptor agents on norepinephrine release from vas deferens of several species including man.

    abstract::Unlike the situation with the vas deferens of rats, guinea-pigs, rabbits and dogs, neither phentolamine nor yohimbine enhanced electrically-evoked release of [3H]norepinephrine from the in vitro human vas deferens. However, clonidine produced, by a phentolamine-sensitive mechanism, a concentration-related inhibition o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Belis JA,Colby JE,Westfall DP

    更新日期:1982-03-26 00:00:00

  • Stereoselective action of (+)-morphine over (-)-morphine in attenuating the (-)-morphine-produced antinociception via the naloxone-sensitive sigma receptor in the mouse.

    abstract::We have previously demonstrated that (+)-morphine and (-)-morphine given spinally stereoselectively attenuate the spinally-administered (-)-morphine-produced tail-flick inhibition in the mouse. The phenomenon has been defined as antianalgesia. Present studies were then undertaken to determine if the systemic administr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wu HE,Hong JS,Tseng LF

    更新日期:2007-10-01 00:00:00

  • Chronic gastric ulcer healing in rats subjected to selective and non-selective cyclooxygenase-2 inhibitors.

    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


    authors: Berenguer B,Alarcón de la Lastra C,Moreno FJ,Martín MJ

    更新日期:2002-05-03 00:00:00

  • RO 16-6028, a benzodiazepine receptor partial agonist, does not exhibit anticonvulsant tolerance in mice.

    abstract::The development of anticonvulsant tolerance with RO 16-6028, a benzodiazepine receptor partial agonist, was assessed in mice using an i.v. infusion of pentylenetetrazol as the convulsive stimulus. In contrast to other benzodiazepines tested previously in this seizure model the anticonvulsant protection afforded by RO ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Haigh JR,Feely M

    更新日期:1988-03-01 00:00:00

  • Alpha-adrenergic regulation of the activity of thymidylate synthetase and thymidine kinase during liver regeneration after partial hepatectomy.

    abstract::The increases in activity of hepatic thymidylate synthetase and of thymidine kinase, which catalyze the formation of thymidylate via the de novo and salvage pathways, respectively, were significantly suppressed during liver regeneration in rats which had been given alpha-adrenoceptor antagonists (phenoxybenzamine and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Nakata R,Tsukamoto I,Nanme M,Makino S,Miyoshi M,Kojo S

    更新日期:1985-08-27 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


    authors: Miller RL,Webster ME,Melmon KL

    更新日期:1975-08-01 00:00:00

  • The binding of [3H]leukotriene C4 to guinea-pig lung membranes. The lack of correlation of LTC4 functional activity with binding affinity.

    abstract::High affinity binding sites for [3H]leukotriene C4 ([3H]LTC4) have been identified and characterised in guinea-pig lung membranes. [3H]LTC4 bound to these membranes with a pharmacological specificity totally distinct to that previously observed for [3H]LTD4 binding in guinea-pig lung. Scatchard analysis of saturation ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Norman P,Abram TS,Kluender HC,Gardiner PJ,Cuthbert NJ

    更新日期:1987-11-17 00:00:00

  • The effect of phosphorylation on amphetamine-mediated outward transport.

    abstract::Amphetamine elicits its locomotor-activating and drug-reinforcing effects by releasing the catecholamines dopamine and norepinephrine into the synapse. Amphetamine is a substrate of the plasmalemmal transporters for both dopamine and norepinephrine. As such, it binds to the transporters in conjunction with Na+ and Cl-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Gnegy ME

    更新日期:2003-10-31 00:00:00

  • Neuromedin-induced excessive grooming/scratching behavior is suppressed by naloxone, neurotensin and a dopamine D1 receptor antagonist.

    abstract::Neuromedin B and neuromedin C were tested for their grooming/scratching-inducing effects and the composition of neuromedin-induced grooming was established by calculating the relative contribution of various grooming elements to the total grooming scores. Excessive grooming induced by neuromedins is characterized by a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Van Wimersma Greidanus TB,Maigret C

    更新日期:1991-12-10 00:00:00