Mixed type inhibition of [D-Ala2, D-Leu5]enkephalin binding to mu-opiate binding sites by mu-, but not by kappa-opiate ligands.

abstract：:Animal models of arthritis are widely used to de-convolute disease pathways and to identify novel drug targets and therapeutic approaches. However, the high attrition rates of drugs in Phase II/III rates means that a relatively small number of drugs reach the market, despite showing efficacy in pre-clinical models. Th...

journal_title：European journal of pharmacology

authors： McNamee K,Williams R,Seed M

更新日期：2015-07-15 00:00:00

abstract：:In the present study, the mechanism of relaxant response of nitric oxide precursor, L-arginine, was investigated in goat isolated coronary artery. L-arginine (1 mM) reversed the U-46619 (1 microM)-induced contraction both in endothelium-intact and endothelium-denuded arterial ring preparations. L-arginine analogues, L...

journal_title：European journal of pharmacology

authors： Deka DK,Mishra SK,Raviprakash V

更新日期：2009-05-01 00:00:00

abstract：:Recombinant human tumor necrosis factor alpha (TNF alpha) decreases social exploration and induces weight loss in mice in a dose- and time-dependent manner (2.5-40 micrograms/mouse). To assess the role of interleukin-1 (IL-1) in these effects, mice pretreated with IL-1 receptor antagonist (IL-1ra, 500 micrograms/mouse...

journal_title：European journal of pharmacology

authors： Bluthé RM,Dantzer R,Kelley KW

更新日期：1991-12-17 00:00:00

abstract：:N-0437, a non-catecholic aminotetralin has recently been described as a very potent and selective dopamine D-2 agonist. In this study the in vitro binding of [3H]N-0437 (specific activity 80.6 Ci/mmol) to calf caudate membranes is described. It was found that [3H]N-0437 binds with a high affinity (KD = 0.17 nM) and a ...

journal_title：European journal of pharmacology

authors： Van der Weide J,De Vries JB,Tepper PG,Horn AS

更新日期：1987-02-10 00:00:00

abstract：:Rats were administered haloperidol, clozapine, raclopride, or no drug for either 28 days or 8 months and then withdrawn from drug treatment for 3 weeks. Oral movements were repeatedly recorded, both by a human observer and by a computerized video analysis system which determined mouth openings and closings, or compute...

journal_title：European journal of pharmacology

authors： See RE,Ellison G

更新日期：1990-06-08 00:00:00

abstract：:The 8-substituted 9-ethyladenine derivatives: 8-bromo-9-ethyladenine (ANR 82), 8-ethoxy- 9-ethyladenine (ANR 94), and 8-furyl-9-ethyladenine (ANR 152) have been characterized in vitro as adenosine receptor antagonists. Adenosine is deeply involved in the control of motor behaviour and substantial evidences indicate th...

journal_title：European journal of pharmacology

authors： Pinna A,Volpini R,Cristalli G,Morelli M

更新日期：2005-04-11 00:00:00

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

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

更新日期：1996-10-31 00:00:00

abstract：:Tricyclic antidepressants not only inhibit monoamine reuptake but also modulate Cys-loop receptors. However, it is not understood how this modulation is involved in their therapeutic effects. We analyzed the mechanisms of inhibition of homomeric 5-HT(3A) and alpha7-5HT(3A) receptors by tricyclic antidepressants at the...

journal_title：European journal of pharmacology

authors： Gumilar F,Bouzat C

更新日期：2008-04-14 00:00:00

abstract：:Lycopene, a natural carotenoid, has potential chemopreventive effects in many cancers. This study aimed to examine the effects of lycopene on regulating the inflammation and apoptosis of N-nitrosomethylbenzylamine(NMBzA) induced esophageal cancer in F344 rats. After the rats were fed normal diets containing different ...

journal_title：European journal of pharmacology

authors： Cui L,Xu F,Wu K,Li L,Qiao T,Li Z,Chen T,Sun C

更新日期：2020-08-15 00:00:00

abstract：:Prostate cancer is one of the most severe malignancies in men, and many genes and non-coding RNAs, included microRNAs (miRs), have been demonstrated to regulate prostate cancer progression. In the present study, we investigated the role of miR-671 in prostate cancer cell proliferation. We found that miR-671 was signif...

journal_title：European journal of pharmacology

authors： Yu Y,Wang Z,Sun D,Zhou X,Wei X,Hou W,Ding Y,Ma Y,Hou Y

更新日期：2018-03-15 00:00:00

abstract：:The effects of the [Ti IV (C(5)H(5))(2) NCS(2)] metallocene (BCDT), a Titanocene Dichloride derivative, on the growth and differentiation of granulocyte-macrophage progenitor cells [colony-forming unit-granulocyte-macrophage (CFU-GM)] and bone marrow cellularity in normal and Ehrlich ascites tumour-bearing mice were s...

journal_title：European journal of pharmacology

authors： Valadares MC,Queiroz ML

更新日期：2002-03-29 00:00:00

abstract：:Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid that contracts most smooth muscles. Although S1P has been shown to contract bladder smooth muscle, the mechanism(s) by which S1P initiates contraction has not been extensively investigated. The goal of this study was to determine if S1P-induced force generation...

journal_title：European journal of pharmacology

authors： Kendig DM,Matsumoto AK,Moreland RS

更新日期：2013-11-15 00:00:00

abstract：:The effect of diazoxide, verapamil and compound D600 on calcium and isoproterenol dose-response relationships was investigated in isolated rabbit atrial preparations. All three agents shifted calcium dose-force relationships parallel and to the right. D600 acted as a competitive antagonist of calcium, as a plot of log...

journal_title：European journal of pharmacology

authors： Bristow MR,Green RD

更新日期：1977-10-01 00:00:00

abstract：:To investigate the role of ATP-sensitive K+(KATP) channels on pacemaker activity in interstitial cells of Cajal (ICC), whole-cell patch clamping, RT-PCR, and intracellular Ca2+([Ca2+]i) imaging were performed in cultured colonic ICC. Pinacidil (a K+ channel opener) hyperpolarized the membrane and inhibited the generat...

journal_title：European journal of pharmacology

authors： Na JS,Hong C,Kim MW,Park CG,Kang HG,Wu MJ,Jiao HY,Choi S,Jun JY

更新日期：2017-08-15 00:00:00

abstract：:Certain enkephalin analogues, including those which contain the conformationally restricted amino acid E-(2R,3S)-cyclopropylphenylalanine [2R,3S)-delta E Phe), have been shown to have high affinity for brain delta opioid receptors but are much less active in mouse vas deferens bioassays. To investigate whether there a...

journal_title：European journal of pharmacology

authors： Vaughn LK,Wire WS,Davis P,Shimohigashi Y,Toth G,Knapp RJ,Hruby VJ,Burks TF,Yamamura HI

更新日期：1990-02-20 00:00:00

abstract：:Ischemia reperfusion (I/R) injury is a cellular damage in a hypoxic organ following the restoration of oxygen delivery. It may occur during organ transplantation, trauma and hepatectomies. Nitric oxide (NO) effects during hepatic I/R are complicated. The iNOS-derived NO has a deleterious effect, whereas eNOS-derived N...

journal_title：European journal of pharmacology

authors： Atef Y,El-Fayoumi HM,Abdel-Mottaleb Y,Mahmoud MF

更新日期：2017-11-15 00:00:00

abstract：:Biphalin (0.3 mg/kg) administered intravenously (i.v.) to urethane-chloralose anaesthetized rats consistently evoked apnoea, followed by breathing at subnormal respiratory rate with increased tidal volume. Mean arterial pressure and heart rate were lowered. Naloxone completely antagonized the respiratory and cardiovas...

journal_title：European journal of pharmacology

authors： Wojciechowski P,Szereda-Przestaszewska M,Lipkowski AW

更新日期：2009-01-05 00:00:00

abstract：:The present investigation was designed to identify potential biomarker(s) and assess the involvement of inflammatory pathway in dimethylnitrosamine (DMN)-induced liver fibrosis in rats. Following DMN-treatment (10 mg/ml/kg, i.p., given three consecutive days each week for 4 weeks) body and liver weights were significa...

journal_title：European journal of pharmacology

authors： Saha JK,Xia J,Sandusky GE,Chen YF,Gerlitz B,Grinnell B,Jakubowski JA

更新日期：2007-12-01 00:00:00

abstract：:Donepezil (E2020) is a novel cholinesterase inhibitor for the treatment of Alzheimer's disease. Recent studies show that it may act on targets other than acetylcholinesterase in the brain. In the present study, the actions of donepezil on voltage-gated Na+ and K+ channels were investigated in rat dissociated hippocamp...

journal_title：European journal of pharmacology

authors： Yu B,Hu GY

更新日期：2005-01-31 00:00:00

abstract：:The effects of inhibitors of Ca(2+)-dependent endopeptidases (antipain and leupeptin) on morphine analgesia, reinforcing properties of morphine and on the development of opiate physical dependence were studied. Male Wistar rats were used. The analgesic action of morphine in the tail-immersion test was increased signif...

journal_title：European journal of pharmacology

authors： Lyupina YV,Sudakov SK,Yarygin VN

更新日期：1996-05-23 00:00:00

abstract：:The effects of antagonists of N-methyl-D-aspartate (NMDA) on the capsaicin-induced cough reflex in rats were studied. Intracisternal (i. cist.) injection of MK-801, a non-competitive antagonist of NMDA, significantly decreased the number of coughs in a dose-dependent manner. The competitive antagonists of NMDA, 2-DL-a...

journal_title：European journal of pharmacology

authors： Kamei J,Tanihara H,Igarashi H,Kasuya Y

更新日期：1989-09-13 00:00:00

abstract：:To evaluate the cardiac effect of an inhibitor of angiotensin-converting enzyme, the effect of intracoronary (i.c.) captopril on coronary blood flow and regional myocardial function was examined in the anesthetized open-chest dog. Blood flow of the left circumflex coronary artery (LCX), left ventricular pressure (LVP)...

journal_title：European journal of pharmacology

authors： Noguchi K,Kato T,Ito H,Aniya Y,Sakanashi M

更新日期：1985-03-26 00:00:00

abstract：:The cyclooxygenase (COX) pathway and prostanoids may critically contribute to the early allergic airway response. In the rat lung, serotonin (5-HT) is a major mediator of antigen-induced contractions. The aim of this study was therefore to examine the relative role of the COX pathway and serotonin for antigen-induced ...

journal_title：European journal of pharmacology

authors： Larsson-Callerfelt AK,Dahlén SE,Kühl AR,Lex D,Uhlig S,Martin C

更新日期：2013-01-15 00:00:00

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

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

abstract：:1-(Meta-chloro)phenylpiperazine (m-CPP) is a 5-HT receptor agonist which has been purported to be relatively selective for the 5-HT2C receptor. In particular, the hypolocomotion produced by m-CPP has been suggested to be mediated by 5-HT2C receptors. m-CPP binds with high affinity to 5-HT1 as well as 5-HT2 receptors, ...

journal_title：European journal of pharmacology

authors： Gleason SD,Shannon HE

更新日期：1998-01-12 00:00:00

abstract：:Activation of imidazoline receptors in the central nervous system has protective effect on several types of arrhythmias. We demonstrated that centrally administered rilmenidine, a selective imidazoline receptor agonist, prevented adrenaline-induced arrhythmias during halothane anaesthesia. However, detailed myocardial...

journal_title：European journal of pharmacology

authors： Yamanaka H,Hayashi Y,Iwasaki M,Kamibayashi T,Yamatodani A,Mashimo T

更新日期：2010-11-25 00:00:00

abstract：:Terfenadine and astemizole rarely cause cardiac arrhythmias by suppressing the cardiac rapid delayed rectifier K+ channel encoded by the human ether-a-go-go-related gene (HERG). Epinastine, however, has not been reported to have the adverse effect. We have therefore compared the effects of epinastine, terfenadine and ...

journal_title：European journal of pharmacology

authors： Chachin M,Katayama Y,Yamada M,Horio Y,Ohmura T,Kitagawa H,Uchida S,Kurachi Y

更新日期：1999-06-25 00:00:00

abstract：:CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this mod...

journal_title：European journal of pharmacology

authors： Sekioka T,Kadode M,Yonetomi Y,Kamiya A,Fujita M,Nabe T,Kawabata K

更新日期：2017-01-05 00:00:00

abstract：:A natural monoterpene alkaloid incarvillateine isolated from the plant Incarvillea sinensis is known to relieve inflammatory and neuropathic pain. However, the molecular target for the action of incarvillateine remains elusive. Here, we report that incarvillateine exacerbates epileptic seizures by inhibiting subtypes ...

journal_title：European journal of pharmacology

authors： Bian X,Zhang Y,Huang B,Wang X,Wang G,Zhu Y,Liu Y,Liang J,Jia Y,Wang K

更新日期：2019-09-05 00:00:00

abstract：:Pre- and postjunctional pA2 values of the muscarinic antagonist hexahydrosiladifenidol were determined with guinea-pig ileum and rat heart. Hexahydrosiladifenidol did not discriminate between pre- and postjunctional receptors within the same organ but was more potent on the ileum (20-80 times) than on the heart. It is...

journal_title：European journal of pharmacology

authors： Fuder H,Kilbinger H,Müller H

更新日期：1985-07-11 00:00:00