Emetic, central nervous system, and pulmonary activities of rolipram in the dog.


:Rolipram was characterized for its emetic, behavioral, cardiovascular and pulmonary activities in dogs, to assess its systemic pharmacology and potential bronchodilatory selectivity. At doses > or = 0.1 mg/kg i.v., rolipram induced emesis, anxiety, and stepping behaviors in conscious dogs, and increased heart rate and cardiac contractility in anesthetized instrumented dogs not treated with a beta-adrenoceptor antagonist. Cardiovascular effects in anesthetized dogs were apparently related to rolipram's central nervous system activities, in that they were associated with a reversal pentobarbital-induced anesthesia and could be ablated by pentobarbital supplementation. Rolipram's reversal of anesthesia was confirmed in uninstrumented dogs, where rolipram shortened pentobarbital sleep time while increasing heart and respiratory rates. After intragastric administration, rolipram exhibited greater emetic potency (100% emesis at 0.1 mg/kg p.o.) and lesser bronchodilatory potency (ED50 = 0.04 mg/kg i.d.) than after i.v. administration. The data demonstrate that rolipram is a potent bronchodilator that produces central nervous system effects only at higher doses when administered i.v. to the dog. Administered intragastrically, however, the bronchodilatory selectivity of rolipram is reduced presumably as a result of the activation of emetic reflexes at sites within the gastrointestinal tract.


Eur J Pharmacol


Heaslip RJ,Evans DY




Has Abstract


1995-11-24 00:00:00














  • A kinetic analysis of a catechol-specific binding site in the microsomal fraction from the rabbit aorta.

    abstract::(-)-3/-Norepinephrine (3H-NE) binding to the microsomal fraction of the rabbit aorta has been studied. Binding appears to increase linearly with time up to at least 30 min, shows no evidence of stereoselectivity and may be inhibited only by compounds possessing the catechol or 3-methoxy-4hydroxyphenyl moieties, with t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Ruffolo RR,Mccreery RL,Patil PN

    更新日期:1976-08-01 00:00:00

  • Augmentation with a 5-HT(1A), but not a 5-HT(1B) receptor antagonist critically depends on the dose of citalopram.

    abstract::Pharmacokinetic and pharmacodynamic parameters of the selective serotonin reuptake inhibitor 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-5-phtalancarbonitril (citalopram) were determined in order to find optimal conditions for augmentation of its effect on extracellular serotonin [5-hydroxytryptamine (5-HT)] through ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Cremers TI,de Boer P,Liao Y,Bosker FJ,den Boer JA,Westerink BH,Wikström HV

    更新日期:2000-05-26 00:00:00

  • Influence of benzodiazepine binding site ligands on fear-conditioned contextual memory.

    abstract::Eight compounds that bind to the benzodiazepine binding site on the gamma-amino butyric acid(A) (GABA(A)) receptor were assessed for their influence on contextual memory, an aspect of memory affected in various cognitive disorders including Alzheimer's disease. Using a Pavlovian fear-conditioning paradigm, each ligand...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: DeLorey TM,Lin RC,McBrady B,He X,Cook JM,Lameh J,Loew GH

    更新日期:2001-08-24 00:00:00

  • Gender-related drug effect on several markers of oxidation stress in diabetes patients with and without complications.

    abstract::We previously reported that circulating lipid (malondialdehyde, MDA) and protein oxidation (carbonyl residues, CO) products can be used as markers of risk for complications in poorly controlled type 2 diabetics. Now, we aimed to evaluate the existence of a gender effect on classical disease markers and oxidative stres...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Lodovici M,Bigagli E,Luceri C,Mannucci E,Rotella CM,Raimondi L

    更新日期:2015-11-05 00:00:00

  • Effect of nomifensine on acetylcholine and choline in the rat striatum and brainstem.

    abstract::Nomifensine, at a dose of 40 mg/kg, slightly but significantly increased rat striatal acetylcholine 60 min after i.p. administration without affecting choline levels or choline O-acetyltransferase and cholinesterase activities. This drug had no effect on brainstem acetylcholine. In contrast, d-amphetamine and desipram...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Garattini S,Consolo S,Chittò G,Peri G,Ladinsky H

    更新日期:1976-01-01 00:00:00

  • Indirubin inhibits inflammatory reactions in delayed-type hypersensitivity.

    abstract::Polygonum tinctorium Lour. (P. tinctorium) is known to have the ability to suppress inflammation. We attempted to isolate the active compounds from P. tinctorium based on their inhibitory effects on the production of interferon-gamma, which is a well-known inflammatory cytokine. We thus isolated indirubin, an isomer o...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Kunikata T,Tatefuji T,Aga H,Iwaki K,Ikeda M,Kurimoto M

    更新日期:2000-12-20 00:00:00

  • Melanocortins and the brain: from effects via receptors to drug targets.

    abstract::The lack of specific receptors (and antagonists) has hampered the research on the neural mechanism of action of adrenocorticotropic hormone (ACTH)- and melanocyte-stimulating hormone (MSH)-like peptides. Yet the original observations in the 1970s already pointed to cAMP as a possible mediator of ACTH/MSH effects in ne...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Adan RA,Gispen WH

    更新日期:2000-09-29 00:00:00

  • Combination therapy of dexamethasone with epigallocatechin enhances tibiotarsal bone articulation and modulates oxidative status correlates with cartilage cytokines expression in the early phase of experimental arthritis.

    abstract::The inclusion of antioxidant for the treatment of arthritis, especially under the therapy with immunosuppressant, is motivated because antioxidant plays an essential role in disease progression and moreover, immunosuppressive treatment suffers redox homeostasis balance of the organism. The aim of the present study was...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Roy S,Sannigrahi S,Ghosh B,Pusp P,Roy T

    更新日期:2013-01-05 00:00:00

  • Sympathetic nerve terminal destruction has no effect on specific [3H]ouabain binding to intact mouse and rat skeletal muscle.

    abstract::Following pretreatment with 6-OH-dopamine, the sympathetic nerve endings of the iris and skeletal muscle of mice and rats were not longer detectable by cytochemistry for noradrenaline. In the same animals, the specific binding of [3H] ouabain to intact soleus muscles was not significantly different from that measured ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Clausen T,Hansen O,Larsson LI

    更新日期:1981-07-10 00:00:00

  • Magnetic bead-based proteomic technology to study paricalcitol effect in kidney transplant recipients.

    abstract::Secondary hyperparathyroidism is a common complication in patients with chronic kidney disease and frequently persists after kidney transplantation. Paricalcitol, a selective vitamin D receptor activator, is indicated in the management of this disorder and recent evidences have suggested that this drug has other benef...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,随机对照试验


    authors: Pérez V,Sánchez-Escuredo A,Lauzurica R,Bayés B,Navarro-Muñoz M,Pastor MC,Cañas L,Bonet J,Romero R

    更新日期:2013-06-05 00:00:00

  • The tachykinin NK1 receptor antagonist PD 154075 blocks cisplatin-induced delayed emesis in the ferret.

    abstract::The activity of a selective tachykinin NK1 receptor antagonist, PD 154075 ([(2-benzofuran)-CH2OCO]-(R)-alpha-MeTrp-(S)-NHCH(CH3) Ph), was examined in radioligand binding studies, in a [Sar9,Met(O2)11]substance P-induced foot-tapping model in the gerbil, and in cisplatin-induced acute and delayed emesis in the ferret. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Singh L,Field MJ,Hughes J,Kuo BS,Suman-Chauhan N,Tuladhar BR,Wright DS,Naylor RJ

    更新日期:1997-02-26 00:00:00

  • pH dependent efflux of methamphetamine derivatives and their reversal through human Caco-2 cell monolayers.

    abstract::The purpose of this study was to investigate possible efflux mechanisms involved in amphetamine derivative transport such as for 3,4-methylenedioxymethamphetamine (MDMA), 3,4-methylenedioxyethylamphetamine (MDEA), para-methoxyamphetamine (p-MA), dexamphetamine and pseudoephedrine, especially across pH gradients that e...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Crowe A,Diep S

    更新日期:2008-09-11 00:00:00

  • Interference of the PAF receptor antagonist, PCA 4248, with the rat pleurisy evoked by inflammatory mediators or allergen.

    abstract::This study investigated the effect of the platelet-activating factor (PAF) receptor antagonist, PCA 4248, on the rat pleurisy caused by PAF, serotonin, bradykinin, histamine or allergen. The pleurisy was assessed by measuring liquid extravasation and leucocyte infiltration. Oral pretreatment with PCA 4248 (2.5-20 mg/k...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Martins MA,Lima MC,Bozza PT,Faria Neto HC,Silva PM,Sunkel CE,Cordeiro RS

    更新日期:1993-06-11 00:00:00

  • Resveratrol provides late-phase cardioprotection by means of a nitric oxide- and adenosine-mediated mechanism.

    abstract::We used two experimental models to prove that resveratrol (trans-3,4',5-trihydroxystilbene) reduces cardiac ischemic-reperfusion injury by means of a nitric oxide- and adenosine-dependent mechanism. (1). ACUTE EX VIVO: resveratrol (10 microM, 10 min) infusion in Langendorff-perfused normoxic rat hearts significantly i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bradamante S,Barenghi L,Piccinini F,Bertelli AA,De Jonge R,Beemster P,De Jong JW

    更新日期:2003-03-28 00:00:00

  • Potentiation by neuropeptide Y of 5HT2A receptor-mediated contraction in porcine coronary artery.

    abstract::Potentiation by neuropeptide Y of serotonin (5-HT)-induced vasoconstriction was investigated in porcine coronary artery. 5-HT caused concentration-dependent contraction through 5-HT2A receptors. Neuropeptide Y (30 nM) significantly increased the 5HT-induced contraction by 16+/-5% in arteries with intact endothelium. R...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Tsurumaki T,Nagai S,Bo X,Toyosato A,Higuchi H

    更新日期:2006-08-21 00:00:00

  • Brain phospholipase C, diacylglycerol lipase and monoacylglycerol lipase are involved in (±)-epibatidine-induced activation of central adrenomedullary outflow in rats.

    abstract::We previously reported that intracerebroventricularly (i.c.v.) administered (±)-epibatidine (a potent agonist of nicotinic acetylcholine receptors) (1, 5 and 10 nmol/animal) dose-dependently elevated plasma levels of noradrenaline and adrenaline and that this response was reduced by i.c.v. administered indomethacin (c...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Shimizu T,Tanaka K,Nakamura K,Taniuchi K,Yokotani K

    更新日期:2012-09-15 00:00:00

  • Increase in P-glycoprotein levels in the blood-brain barrier of partial portal vein ligation /chronic hyperammonemia rats is medicated by ammonia/reactive oxygen species/ERK1/2 activation: In vitro and in vivo studies.

    abstract::Liver failure altered P-glycoprotein (P-gp) function and expression at blood-brain barrier (BBB), partly owing to hyperammonemia. We aimed to examine the effects of partial portal vein ligation (PVL) plus chronic hyperammonemia (CHA) on P-gp function and expression at rat BBB. Experimental rats included sham-operation...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Zhou Y,Zhou J,Li P,Xie Q,Sun B,Li Y,Chen Y,Zhao K,Yang T,Zhu L,Xu J,Liu X,Liu L

    更新日期:2019-03-05 00:00:00

  • The alpha 1-adrenoceptor is inactivated by alterations in membrane phospholipids.

    abstract::The influence of the membrane environment on the alpha 1-adrenoceptor has been investigated by examining the effect of phospholipase digestion on the binding of [3H]prazosin to aortic and hepatic membranes. Membrane digestion by phospholipase A2 and phospholipase C was found to markedly reduce prazosin binding to the ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Shreeve SM,Valliere JE

    更新日期:1992-05-12 00:00:00

  • Effect of sirolimus on liver cirrhosis and hepatic encephalopathy of common bile duct-ligated rats.

    abstract::Cirrhosis is often associated with portal hypertension and portal-systemic collateral vessels formation attributed to angiogenesis, which leads to severe complications as hepatic encephalopathy. Sirolimus has anti-fibrosis and anti-angiogenesis effects, but whether it influences the severity of portal-systemic collate...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wu KC,Huang HC,Chang T,Lee WS,Chuang CL,Hsin IF,Hsu SJ,Lee FY,Chang CC,Lee SD

    更新日期:2018-04-05 00:00:00

  • alpha-Methylnoradrenaline induced hypotension and bradycardia after administration into the area of the nucleus tractus solitarii.

    abstract::Bilateral injections of alpha-methylnoradrenaline into the area of the nucleus tractus solitarii of the brain stem caused a dose-dependent decrease of systemic arterial blood pressure and heart rate of anesthetized rats. The effects were prevented and even reversed by a preceding injection of the alpha-adrenoceptor bl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Nijkamp FP,De Jong W

    更新日期:1975-06-01 00:00:00

  • Pharmacological inhibition of JAK3 enhances the antitumor activity of imatinib in human chronic myeloid leukemia.

    abstract::Imatinib (IMA) is the standard treatment for CML; however, stopping IMA sometimes results in disease relapse, which suggests that leukemic stem cells (LSCs) remain in such patients, even after complete molecular remission has been achieved. Therefore, new strategies will be required to eradicate LSCs. The Janus kinase...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Yagi K,Shimada A,Sendo T

    更新日期:2018-04-15 00:00:00

  • Increase in nigral type II benzodiazepine recognition sites following striatonigral denervation.

    abstract::In the rat substantia nigra Type II benzodiazepine recognition sites (measured as the portion of [3H]flunitrazepam binding which remain after the addition of 2 X 10(-7) M Cl 218872) represent 50% of the total benzodiazepine recognition sites. The density of Type II sites was increased by 35% following the degeneration...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Porceddu ML,Corda MG,Sanna E,Biggio G

    更新日期:1985-06-07 00:00:00

  • Vascular bed and vasoconstrictor-dependent selectivity of the calcium channel antagonist, PN 200-110.

    abstract::The potency of the dihydropyridine calcium channel blocker, PN 200-110 was assessed in vitro against contractions induced by potassium (20-55 mM) and histamine (1-300 microM) in rabbit thoracic aorta, coronary, basilar, renal and central ear arteries. PN 200-110 was particularly effective against potassium responses i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Bijak A,Pasternac A,McPherson GA,Bevan JA

    更新日期:1986-12-16 00:00:00

  • Role of nitric oxide in the gastric cytoprotection induced by central vagal stimulation.

    abstract::The role of nitric oxide (NO) in the vagal cholinergic-mediated cytoprotective effect of intracisternal (i.c.) injection of the stable thyrotropin-releasing hormone (TRH) analog, RX 77368, was investigated in conscious rats. RX 77368 (1.5 ng i.c.) reduced by 88% gastric hemorrhagic lesions induced by oral administrati...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Király A,Sütö G,Taché Y

    更新日期:1993-08-24 00:00:00

  • Preclinical murine models of Chronic Obstructive Pulmonary Disease.

    abstract::Chronic Obstructive Pulmonary Disease (COPD) is a major incurable global health burden and is the 4th leading cause of death worldwide. It is believed that an exaggerated inflammatory response to cigarette smoke causes progressive airflow limitation. This inflammation, where macrophages, neutrophils and T lymphocytes ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审


    authors: Vlahos R,Bozinovski S

    更新日期:2015-07-15 00:00:00

  • Inhibition by agmatine on morphine-induced conditioned place preference in rats.

    abstract::Our previous studies demonstrated the ability of exogenous agmatine to inhibit tolerance to and physical dependence on morphine in mice, rats and monkeys. The present study further evaluated the effect of agmatine on the psychological dependence induced by morphine in conditioned place preference assay. Agmatine (0.75...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Wei XL,Su RB,Lu XQ,Liu Y,Yu SZ,Yuan BL,Li J

    更新日期:2005-05-16 00:00:00

  • Brivaracetam and seletracetam, two new SV2A ligands, improve paroxysmal dystonia in the dt sz mutant hamster.

    abstract::Previous examinations demonstrated antidystonic effects of the synaptic vesicle protein 2A (SV2A) ligand levetiracetam in the dt(sz) mutant hamster, an animal model of paroxysmal non-kinesiogenic dyskinesia in which dystonic episodes can be induced by stress. In the present study, we examined the effects of the two ne...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Hamann M,Sander SE,Richter A

    更新日期:2008-12-28 00:00:00

  • Differential effect of potassium on the action of digoxin and digoxigenin in guinea-pig heart.

    abstract::The effect of potassium on the binding of digoxin or digoxigenin to isolated Na+, K+-ATPase was compared with that of potassium on the positive inotropic action of the agents in guinea-pig hearts. The binding of digoxigenin to the enzyme in vitro was reduced to a greater extent by potassium than was the binding of dig...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Akera T,Wiest SA,Brody TM

    更新日期:1979-08-15 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


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

    更新日期:2000-06-02 00:00:00

  • Influence of 7-nitroindazole on the anticonvulsive action of conventional antiepileptic drugs.

    abstract::7-Nitroindazole (a selective neuronal nitric oxide (NO) synthase inhibitor) at 25 and 50 mg/kg, 30 min before the test, did not influence the electroconvulsive threshold. However, at 50 mg/kg, it enhanced the anticonvulsive activity of phenobarbital against maximal electroshock and did not affect that of carbamazepine...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章


    authors: Borowicz KK,Kleinrok Z,Czuczwar SJ

    更新日期:1997-07-23 00:00:00