Sulphonamide modulation of sodium content in rat pancreatic islets.

abstract：:The binding profile of cyclazosin, a new prazosin-related alpha 1-adrenoceptor antagonist, at alpha 1-, alpha 2-adrenoceptors, dopamine D2 and 5-HT1A receptors was compared to that of 5-methylurapidil, spiperone, risperidone and other prazosin-related ligands. In addition, cyclazosin was investigated at native and clo...

journal_title：European journal of pharmacology

authors： Giardinà D,Crucianelli M,Melchiorre C,Taddei C,Testa R

更新日期：1995-12-04 00:00:00

abstract：:The effect of DL-propranolol on NO release in perfused rat hindquarters was studied by using oxyhemoglobin as a capture system to allow the quantitative assay of NO production. In some experiments the stable prostacyclin metabolite 6-keto-PGF1 alpha (6-keto) was simultaneously assayed. We observed that: (1) DL-propran...

journal_title：European journal of pharmacology

authors： Mota-Filipe H,Castro M,Gião-T-Rico JM

更新日期：1992-03-24 00:00:00

abstract：:The alpha-adrenoceptor antagonist properties of doxazosin and its enantiomers were characterized using human prostate tissue and cell membranes isolated from rat-1 fibroblast expressing each of the cloned human alpha 1-adrenoceptor subtypes. In the alpha 1-adrenoceptor-binding studies on the human prostate with [3H]do...

journal_title：European journal of pharmacology

authors： Hatano A,Tang R,Walden PD,Lepor H

更新日期：1996-10-10 00:00:00

abstract：:Angiotensin-converting enzymes, ACE and ACE2, are key members of renin angiotensin system. Activation of ACE2/Ang-(1-7) pathway enhances cardiovascular protective functions of bone marrow-derived stem/progenitor cells. The current study evaluated the selectivity of ACE2 inhibitors, MLN-4760 and DX-600, and ACE and ACE...

journal_title：European journal of pharmacology

authors： Joshi S,Balasubramanian N,Vasam G,Jarajapu YP

更新日期：2016-03-05 00:00:00

abstract：:Dynorphin (1-100 nM) dose dependently inhibited both spontaneous and electrically evoked endogenous dopamine (DA) release from slices of the nucleus accumbens of untreated rats. When this inhibitory effect was compared, it was significantly reduced in rats pretreated (for 9 days) with methamphetamine (6 mg/kg per day ...

journal_title：European journal of pharmacology

authors： Yokoo H,Yamada S,Yoshida M,Tanaka M,Nishi S

更新日期：1992-11-03 00:00:00

abstract：:Hops (Humulus lupulus L.), a major component of beer, contain potentially neuroactive compounds that made it useful in traditional medicine as a sleeping aid. The present study aims to investigate the individual components in hops acting as allosteric modulators in GABAA receptors and bring further insight into the mo...

journal_title：European journal of pharmacology

authors： Benkherouf AY,Logrén N,Somborac T,Kortesniemi M,Soini SL,Yang B,Salo-Ahen OMH,Laaksonen O,Uusi-Oukari M

更新日期：2020-04-15 00:00:00

abstract：:Calmodulin antagonists have calcium entry blocking properties. In order to quantitatively investigate the interactions of these drugs with calcium channels, their effect on [3H]nitrendipine and [3H]d-cis-diltiazem binding to rat cerebral cortex membrane preparations was compared to their inhibitory effect on the activ...

journal_title：European journal of pharmacology

authors： Schaeffer P,Lugnier C,Stoclet JC

更新日期：1991-04-25 00:00:00

abstract：:Approximately 3% of the world׳s population suffers from chronic infections with hepatitis C virus (HCV). Although current treatment regimes are capable of effectively eradicating HCV infection from these patients, the cost of these combinations of direct-acting antivirals are prohibitive. Approximately 80% of untreate...

journal_title：European journal of pharmacology

authors： Douglas DN,Kneteman NM

更新日期：2015-07-15 00:00:00

abstract：:Global forebrain ischemia results in damage to the pyramids in the CA1 hippocampal subfield, which is particularly vulnerable to excitotoxic processes. Morphological and functional disintegration of this area leads to a cognitive dysfunction and neuropsychiatric disorders. Treatment with N-methyl-d-aspartate receptor ...

journal_title：European journal of pharmacology

authors： Gellért L,Fuzik J,Göblös A,Sárközi K,Marosi M,Kis Z,Farkas T,Szatmári I,Fülöp F,Vécsei L,Toldi J

更新日期：2011-09-30 00:00:00

abstract：:The neuroprotective effects of erythropoietin on 1-methyl-4-phenylpyridinium (MPP(+))-induced oxidative stress and apoptosis in cultured PC12 cells as well as the underlying mechanism were investigated. Treatment of PC12 cells with MPP(+) caused the loss of cell viability, which was associated with the elevation in ap...

journal_title：European journal of pharmacology

authors： Wu Y,Shang Y,Sun S,Liu R

更新日期：2007-06-14 00:00:00

abstract：:Failed medical therapy is a common problem in inflammatory bowel disease. P-glycoprotein (P-gp), an efflux pump encoded by MDR1 (ABCB1) gene can actively pump drugs out of cells conferring the phenotype of multidrug resistance. Various studies evoked that cyclooxygenase (COX) system may be involved in the regulation o...

journal_title：European journal of pharmacology

authors： Zrieki A,Farinotti R,Buyse M

更新日期：2010-06-25 00:00:00

abstract：:The novel substituted benzamide eticlopride, (S)-(-)-5-chloro-3-ethyl-N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxy salicylamide hydrochloride (A38503; FLB 131), was radiolabelled to high specific activity and used for in vivo receptor binding studies in the rat brain. Intravenous injections of [3H]eticlopride resulted...

journal_title：European journal of pharmacology

authors： Köhler C,Hall H,Gawell L

更新日期：1986-01-21 00:00:00

abstract：:The effect of treatment with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) on juvenile (6-8 months), young adult (2-4 years) and aged (8-10 years) common marmosets were compared. Juvenile marmosets were more resistant to the actions of MPTP and required a greater cumulative dose over a longer period to induce th...

journal_title：European journal of pharmacology

authors： Rose S,Nomoto M,Jackson EA,Gibb WR,Jaehnig P,Jenner P,Marsden CD

更新日期：1993-01-12 00:00:00

abstract：:The activity of the four glycoterpenoids: two saponins, verbascosaponin A and verbascosaponin, and two iridoids, scropolioside A and scrovalentinoside, isolated from Scrophularia auriculata ssp. pseudoauriculata, were studied in different models of acute and chronic inflammation. Both saponins significantly inhibited ...

journal_title：European journal of pharmacology

authors： Giner RM,Villalba ML,Recio MC,Máñez S,Cerdá-Nicolás M,Ríos J

更新日期：2000-02-18 00:00:00

abstract：:The effect of eliprodil on P-type Ca2+ channels was investigated in acutely dissociated rat Purkinje neurons, by using the whole-cell patch-clamp technique. Eliprodil inhibited in a reversible manner the omega-agatoxin-IVA-sensitive Ba2+ current elicited by step depolarizations from a -80 mV holding voltage (IC50 = 1....

journal_title：European journal of pharmacology

authors： Biton B,Granger P,Depoortere H,Scatton B,Avenet P

更新日期：1995-12-27 00:00:00

abstract：:We have examined the motor responses to the dopamine D(3) receptor-preferring agonist, S(+)-(4aR,10bR)-3,4,4a, 10b-tetrahydro-4-propyl-2H,5H-1-benzopyranol[4,3-b]-1,4-oxazin+ ++-9-ol ((+)-PD128,907), by non-habituated male rats during postnatal development. (+)-PD128,907 (0.025 and 0.1 mg/kg) increased motor activity ...

journal_title：European journal of pharmacology

authors： Heijtz RD,Ogren SO,Fuxe K

更新日期：2000-03-24 00:00:00

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

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

abstract：:The effect of intrathecal clonidine on thermal nociception and hindlimb flexion was assessed in acute and chronic spinally transected rats. After an acute, 1-day spinalization, there was no change in the antinociceptive dose-response function to clonidine, relative to intact rats. However, there was a significant incr...

journal_title：European journal of pharmacology

authors： Advokat C

更新日期：2002-02-15 00:00:00

abstract：:The aim of this study was to investigate the effects of chronic lithium treatment on calcium (Ca2+)-stimulated adenylate cyclase activity in rat striatum and hippocampus, and to elucidate the effect of lithium treatment on the neurotransmitter/GTP-mediated inhibition of Ca2+-stimulated enzyme activity in the two brain...

journal_title：European journal of pharmacology

authors： Mørk A,Geisler A

更新日期：1989-09-22 00:00:00

abstract：:Effects of PGI2 upon pulmonary vascular resistance and systemic arterial pressure of near term fetuses were evaluated in anesthetized, exteriorized, unventilated fetal lambs by means of an open-chest, pump-perfused lung preparation. These effects were compared to those of PGE1 and PGE2 in the same animals. Intrapulmon...

journal_title：European journal of pharmacology

authors： Leffler CW,Hessler JR

更新日期：1979-02-15 00:00:00

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

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

更新日期：2015-10-05 00:00:00

abstract：:We synthesized the o-, m- and p-bromo derivatives of dl-threo-methylphenidate from the corresponding bromophenylacetonitriles by modification of the literature synthesis of methylphenidate (Panizzon, Helv. Chim. Acta 1944, 27, 1748). In in vitro binding assays all three dl-threo bromo compounds had higher affinities t...

journal_title：European journal of pharmacology

authors： Pan D,Gatley SJ,Dewey SL,Chen R,Alexoff DA,Ding YS,Fowler JS

更新日期：1994-10-24 00:00:00

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

authors： Martz A,Deitrich RA,Harris RA

更新日期：1983-04-22 00:00:00

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

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

abstract：:Depression is a serious mental disorder that is becoming more common. To better treat patients suffering from this illness, elucidation of the underlying psychopathological and neurobiological mechanisms of depression is needed. Based on the evidence, we sought to investigate the effects of hesperidin in a model of de...

journal_title：European journal of pharmacology

authors： Antunes MS,Jesse CR,Ruff JR,de Oliveira Espinosa D,Gomes NS,Altvater EET,Donato F,Giacomeli R,Boeira SP

更新日期：2016-10-15 00:00:00

abstract：:The pharmacological mechanisms involved in the interactions between C-fibers, cholinergic fibers and mast cells were investigated in tracheally perfused rabbit lungs by measuring the simultaneous release of substance P and histamine in lung effluents. The amounts of substance P and histamine released in lung superfusa...

journal_title：European journal of pharmacology

authors： Nemmar A,Delaunois A,Beckers JF,Sulon J,Bloden S,Gustin P

更新日期：1999-04-23 00:00:00

abstract：:Multiple myeloma is an incurable hematological malignancy. Different studies demonstrated the occurrence of genetic and epigenetic alterations in multiple myeloma. Histone lysine methylation has emerged as a central epigenetic change in the organization of eukaryotic chromatin with far-reaching implications for the re...

journal_title：European journal of pharmacology

authors： Zhao F,Chen Y,Zeng L,Li R,Zeng R,Wen L,Liu Y,Zhang C

更新日期：2010-11-10 00:00:00

abstract：:The anticonvulsant activity of 1-methyl-1,2,3,4-tetrahydroisoquinoline (MeTHIQ--an endogenous parkinsonism-preventing substance) administered alone and in combination with four conventional antiepileptic drugs (carbamazepine, phenytoin, phenobarbital and valproate) was determined in the mouse maximal electroshock-indu...

journal_title：European journal of pharmacology

authors： Luszczki JJ,Antkiewicz-Michaluk L,Czuczwar SJ

更新日期：2009-01-14 00:00:00

abstract：:The release of newly synthesised [3H]acetylcholine was evoked by electrical field stimulation (5 Hz, 600 pulses) of epithelium-deprived guinea-pig trachea strips after sensory neuropeptides depletion with 3 microM capsaicin. The selective tachykinin NK(2) receptor agonist [betaAla(8)]neurokinin A-(4-10) increased in a...

journal_title：European journal of pharmacology

authors： D'Agostino G,Erbelding D,Kilbinger H

更新日期：2000-05-12 00:00:00

abstract：:Kinin B1 receptors on rabbit aorta smooth muscle cells in culture were investigated. [3H]Des-Arg10-kallidin labeled a single site in cells at early passage with an equilibrium dissociation constant of 258 pM and a maximal binding density of approximately 680 sites/cell. Treatment of the same cells for 18 h with epider...

journal_title：European journal of pharmacology

authors： Schneck KA,Hess JF,Stonesifer GY,Ransom RW

更新日期：1994-02-15 00:00:00