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














  • Electrophysiological effects of cocaine on central monoaminergic neurons.

    abstract::The electrical activity of three different single, identified, spontaneously firing central neurons was monitored by extracellular microelectrodes. Intravenous cocaine administration (0.25-2 mg/kg) elicited an activation of cerebellar Purkinje neurons (PN) and an inhibition of serotonergic dorsal raphe (DRN) and norad...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Pitts DK,Marwah J

    更新日期:1986-11-12 00:00:00

  • Characterization of the interaction of the novel antihypertensive etamicastat with human dopamine-β-hydroxylase: comparison with nepicastat.

    abstract::The interaction of etamicastat, a novel peripherally acting dopamine-β-hydroxylase (DBH) inhibitor, with the enzyme was studied using a classical kinetic approach and the pharmacodynamics effect of the compound upon administration to rats was also evaluated. SK-N-SH cell homogenates convert tyramine into octopamine wi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bonifácio MJ,Sousa F,Neves M,Palma N,Igreja B,Pires NM,Wright LC,Soares-da-Silva P

    更新日期:2015-03-15 00:00:00

  • Avarol and avarone, two new anti-inflammatory agents of marine origin.

    abstract::The anti-inflammatory activity of avarol and avarone, sesquiterpenoid derivatives from the Mediterranean sponge Dysidea avara, was investigated. Both compounds potently inhibited paw oedema induced by carrageenan (approximated ED50 = 9.2 and 4.6 mg/kg, p.o., respectively) as well as ear oedema induced by 12-O-tetradec...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Ferrándiz ML,Sanz MJ,Bustos G,Payá M,Alcaraz MJ,De Rosa S

    更新日期:1994-02-21 00:00:00

  • Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells.

    abstract::Intrinsic drug resistance occurs in many renal carcinomas and is associated with increased expression of multidrug resistant proteins, which inhibits intracellular drug accumulation. Multidrug resistant protein 1, also known as P-glycoprotein, is a membrane drug efflux pump belonging to the ATP-binding cassette (ABC) ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Sato H,Siddig S,Uzu M,Suzuki S,Nomura Y,Kashiba T,Gushimiyagi K,Sekine Y,Uehara T,Arano Y,Yamaura K,Ueno K

    更新日期:2015-01-05 00:00:00

  • Direct effect of phenylethylamine upon isolated rat aortic strip.

    abstract::Phenylethylamine (PEA) has been implicated in a number of central and peripheral nervous system disorders. Its possible mechanisms of action include stimulation via catecholamine release and direct stimulation by PEA. We have examined the effects of PEA on isolated vascular smooth muscle (VSM) to further explore the m...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Hansen TR,Greenberg J,Mosnaim AD

    更新日期:1980-05-02 00:00:00

  • Antidiabetic effect of T-1095, an inhibitor of Na(+)-glucose cotransporter, in neonatally streptozotocin-treated rats.

    abstract::3-(Benzo[b]furan-5-yl)-2', 6'-dihydroxy-4'-methylpropiophenone-2'-O-(6-O-methoxycarbonyl)-bet a-D -glucopyranoside (T-1095) is a derivative of phlorizin, a potent inhibitor of Na(+)-glucose cotransporters. We determined the antidiabetic effect of T-1095 in neonatally streptozotocin-treated diabetic rats. Orally admini...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Oku A,Ueta K,Nawano M,Arakawa K,Kano-Ishihara T,Matsumoto M,Saito A,Tsujihara K,Anai M,Asano T

    更新日期:2000-03-10 00:00:00

  • Fluoxetine selectively induces p53-independent apoptosis in human colorectal cancer cells.

    abstract::Fluoxetine has been shown to induce anti-tumour activity. The aim of this study was to determine the effect of fluoxetine on HCT116+/+ and p53 gene-depleted HCT116-/- human colorectal cancer cells and the mechanisms, including potential p53-dependence, of its action. Fluoxetine-induced apoptosis was investigated by mi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Marcinkute M,Afshinjavid S,Fatokun AA,Javid FA

    更新日期:2019-08-15 00:00:00

  • Effect of colchicine on jejunal adenylate cyclase activity, PGE2 and cAMP contents.

    abstract::The effect of colchicine on jejunal adenylate cyclase activity, prostaglandin E2 (PGE2) and cAMP contents, the enzyme and mediators involved in intestinal fluid secretion was tested in rats. Four h after the intraperitoneal injection of colchicine (0.5 mg/100 g body wt.) mucosal PGE2 content, adenylate cyclase activit...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Rachmilewitz D,Karmeli F

    更新日期:1980-10-17 00:00:00

  • Nicotine cue: lack of effect of the alpha 7 nicotinic receptor antagonist methyllycaconitine.

    abstract::To assess the role of the alpha 7 neuronal nicotinic acetylcholine receptor in the discriminative stimulus properties of (-)-nicotine, this study investigated the ability of the alpha 7 receptor antagonist methyllycaconitine to modulate the nicotine cue. In rats trained to discriminate (-)-nicotine from saline, intrap...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Brioni JD,Kim DJ,O'Neill AB

    更新日期:1996-04-22 00:00:00

  • In vivo neuroprotective effects of the novel imidazolyl nitrone free-radical scavenger (Z)-alpha-[2-thiazol-2-yl)imidazol-4-yl]-N-tert-butylnitrone (S34176).

    abstract::Herein, we report an extensive investigation of the neuroprotective effects of the compound (Z)-alpha-[2-thiazol-2-yl)imidazol-4-yl]-N-tert-butylnitrone (S34176) and the prototypic nitrone alpha-phenyl-N-tert-butylnitrone (PBN), in different in vivo paradigms of neuronal degeneration. Administration of S34176 (75 mg/k...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Lockhart B,Roger A,Bonhomme N,Goldstein S,Lestage P

    更新日期:2005-03-28 00:00:00

  • O-GlcNAc impairs endothelial function in uterine arteries from virgin but not pregnant rats: The role of GSK3β.

    abstract::Increased O-Linked β-N-acetylglucosamine (O-GlcNAc) is observed in several pathologies, and unbalanced O-GlcNAcylation levels favor endothelial dysfunction. Whether augmented O-GlcNAc impacts the uterine artery (UA) function and how it affects the UA during pregnancy remains to be elucidated. We hypothesized that gluc...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Dela Justina V,Priviero F,Dos Passos RR Jr,Webb RC,Lima VV,Giachini FR

    更新日期:2020-08-05 00:00:00

  • Delta-9-tetrahydrocannabinol differently affects striatal c-Fos expression following haloperidol or clozapine administration.

    abstract::It was previously shown that haloperidol, but not clozapine, induced intense rat catalepsy when co-administered with delta-9-tetrahydrocannabinol. The present study investigated whether similar alterations could be observed on striatal c-Fos immunoreactivity after administration of the same drug combinations. Western ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Marchese G,Sanna A,Casu G,Casti P,Spada GP,Ruiu S,Pani L

    更新日期:2008-11-19 00:00:00

  • Vagal apnea and hypotension evoked by systemic injection of an antinociceptive analogue of endomorphin-2.

    abstract::PK20M (Dmt-D-Lys-Phe-Phe-OH) is a novel modified endomorphin-2 (EM-2) peptide producing strong dose- and time-dependent antinociceptive activity. Yet its prototype, endogenous EM-2, has been reported to trigger respiratory and vascular effects such as apnea and hypotension. The purpose of this study was to investigate...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wojciechowski P,Kleczkowska P,Mollica A,Stefanucci A,Kaczyńska K

    更新日期:2020-10-15 00:00:00

  • The effect of arachidonic acid and free fatty acids on vesicular uptake of glutamate and gamma-aminobutyric acid.

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    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Roseth S,Fykse EM,Fonnum F

    更新日期:1998-01-12 00:00:00

  • Differential effects of tyrosine kinase inhibitors on contraction and relaxation of the aortas of normotensive and hypertensive rats.

    abstract::The contribution of tyrosine kinase activity to vasoreactivity in normotensive Wistar-Kyoto (WKY) and spontaneously hypertensive (SHR) rats was investigated on isolated aortic preparations by the use of two tyrosine kinase inhibitors: methyl-2,5-dihydroxycinnamate (30 microM) and genistein (30 microM). The pretreatmen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Zerrouk A,Auguet M,Dabiré H,Brisac AM,Safar M,Chabrier PE

    更新日期:1999-06-11 00:00:00

  • Bimoclomol elevates heat shock protein 70 and cytoprotects rat neonatal cardiomyocytes.

    abstract::Bimoclomol is a new compound that improves cell survival under experimental stress conditions partly by increasing intracellular heat shock proteins (HSPs). HSPs, especially HSP70, play a cytoprotective role in the rat heart. Rat neonatal cardiomyocytes were used to determine the ability of bimoclomol to induce HSP70 ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Polakowski JS,Wegner CD,Cox BF

    更新日期:2002-01-18 00:00:00

  • The inflammatory reaction in an experimental model of open wounds in the rat. The effect of arachidonic acid metabolites.

    abstract::The study concerned the effect of arachidonic acid metabolites on the inflammatory reaction in granulation tissue of open wounds in rats. Metabolites or inhibitors were applied in a wound chamber attached to circular, open, full-thickness skin wounds 5 days post-wounding. The adjacent wound served as control. Blood fl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Lundberg C,Gerdin B

    更新日期:1984-01-27 00:00:00

  • Inhibitory action of L-type Ca2+ current by paeoniflorin, a major constituent of peony root, in NG108-15 neuronal cells.

    abstract::The effects of paeoniflorin, a glycoside isolated from the root of Paeonia lactiflora, on ion currents in a mouse neuroblastoma and rat glioma hybrid cell line, NG108-15 were investigated. Paeoniflorin (1-300 microM) reversibly produced an inhibition of L-type voltage-dependent Ca2+ current (I(Ca,L)) in a concentratio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Tsai TY,Wu SN,Liu YC,Wu AZ,Tsai YC

    更新日期:2005-10-31 00:00:00

  • Lycopodine triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in androgen sensitive and refractory prostate cancer cells without modulating p53 activity: signaling cascade and drug-DNA interaction.

    abstract::When the prostate cancer cells become unresponsive to androgen therapy, resistance to chemotherapy becomes imminent, resulting in high mortality. To combat this situation, lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatum spores, was tested against hormone sensitive (LnCaP)...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bishayee K,Chakraborty D,Ghosh S,Boujedaini N,Khuda-Bukhsh AR

    更新日期:2013-01-05 00:00:00

  • Magnesium valproate attenuates hyperactivity induced by dexamphetamine-chlordiazepoxide mixture in rodents.

    abstract::A mixture of dexamphetamine and chlordiazepoxide induces hyperactivity in both mice and rats. This type of hyperactivity has been proposed as an animal model of mania. Magnesium valproate itself had little influence on the activity of normal mice and rats. Acute pretreatment of mice with magnesium valproate (75-300 mg...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Cao BJ,Peng NA

    更新日期:1993-06-24 00:00:00

  • Unusual cholinergic response of bullfrog sympathetic ganglion cells.

    abstract::The membrane of bullfrog sympathetic ganglion cells was hyperpolarized by a direct action of ACh (more than 0.5 mM) in a solution containing both nicotine (0.24 mM) and atropine (0.14 mM). This ACh hyperpolarization could be imitated by neither carbachol nor bethanechol, suggesting that the ACh hyperpolarization was t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Koketsu K,Yamamoto K

    更新日期:1975-04-01 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


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

    更新日期:1988-07-07 00:00:00

  • Serotonin-like actions of quipazine and CPP on spinal motoneurones.

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    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Neuman RS,White SR

    更新日期:1982-06-16 00:00:00

  • Imidazoline I2 receptors: target for new analgesics?

    abstract::Pain remains a major clinical challenge because there are no effective analgesics for some pain conditions and the mainstay analgesics for severe pain, opioids, have serious unwanted effects. There is a dire need for novel analgesics in the clinic. Imidazoline receptors are a family of three receptors (I(1), I(2) and ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Li JX,Zhang Y

    更新日期:2011-05-11 00:00:00

  • Increased sensitivity to dopamine agonists following a single dose of morphine or levorphanol in mice.

    abstract::Acute administration of an opiate has been suggested to result in the development of supersensitive dopamine receptors. This hypothesis was tested in mice by determining the effect of a single administration of morphine or levorphanol on dopamine agonist-induced stereotypic behaviors and [3H]spiroperidol binding. Admi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Martin JR,Takemori AE

    更新日期:1985-12-10 00:00:00

  • Involvement of the dopaminergic receptors of the rat basolateral amygdala in anxiolytic-like effects of the cholinergic system.

    abstract::Cholinergic system stimulation in some parts of the brain may affect anxiety-related behaviors. This system has many interactions with dopaminergic neurotransmission in the brain. We have studied the effect of cholinergic system activation in the basolateral amygdala on anxiety-related behaviors in adult male wistar r...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Zarrindast MR,Sroushi A,Bananej M,Vousooghi N,Hamidkhaniha S

    更新日期:2011-12-15 00:00:00

  • Cadherins as novel targets for anti-cancer therapy.

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    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Blaschuk OW,Devemy E

    更新日期:2009-12-25 00:00:00

  • Dopamine D3 receptor modulation of dopamine efflux in the rat nucleus accumbens.

    abstract::The effect of antipsychotics on electrically evoked dopamine efflux in the rat nucleus accumbens core and shell was investigated, using in vitro fast cyclic voltammetry. In the nucleus accumbens core, the dopamine D2/D3 receptor agonist, (+/-)7-OH-DPAT ((+/-)-2-dipropylamino-7-hydroxy-1,2,3,4-tetrahydronaphthalene), i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Roberts C,Cummins R,Gnoffo Z,Kew JN

    更新日期:2006-03-18 00:00:00

  • Chronic administration of modafinil induces hyperalgesia in mice: reversal by L-NG-nitro-arginine methyl ester and 7-nitroindazole.

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    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Gupta R,Gupta LK,Bhattacharya SK

    更新日期:2014-08-05 00:00:00

  • Methamphetamine selectively alters brain glutathione.

    abstract::As methamphetamine-induced neurotoxicity has been proposed to involve oxidative stress, reduced and oxidized glutathione (GSH and GSSG, respectively), vitamin E and ascorbate were measured in the striata of rats killed 2 or 24 h after a neurotoxic regimen of methamphetamine. At 2 h, methamphetamine increased GSH and G...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Harold C,Wallace T,Friedman R,Gudelsky G,Yamamoto B

    更新日期:2000-07-14 00:00:00