Morphine promotes phosphorylation of the human delta-opioid receptor at serine 363.

abstract：:COVID-19 pandemic presents an unprecedented challenge to identify effective drugs for treatment. Despite multiple clinical trials using different agents, there is still a lack of specific treatment for COVID-19. Having the potential role in suppressing inflammation, immune modulation, antiviral and improving respirato...

journal_title：European journal of pharmacology

authors： Monji F,Al-Mahmood Siddiquee A,Hashemian F

更新日期：2020-11-15 00:00:00

abstract：:In the presence of RS-15385-197 to preclude binding to alpha 2-adrenoceptors, [3H]p-aminoclonidine labelled a low affinity high capacity site, (Kd = 127.6 +/- 19.7 nM, Bmax 978 +/- 172 fmol/mg protein) whereas [3H]idazoxan labelled a high affinity low capacity site (Kd = 1.66 +/- 0.28 nM, Bmax 45.3 +/- 11.4 fmol/mg pr...

journal_title：European journal of pharmacology

authors： MacKinnon AC,Stewart M,Olverman HJ,Spedding M,Brown CM

更新日期：1993-02-23 00:00:00

abstract：:Selective L-type voltage-operated calcium channel (VOCC) antagonists nicardipine, diltiazem and verapamil all produced pronounced falls in mean arterial blood pressure (MAP) in the anaesthetized artificially ventilated guinea-pig. This fall in MAP was associated with a significant reduction of the pressor response ind...

journal_title：European journal of pharmacology

authors： Bond A,Boot JR

更新日期：1992-07-21 00:00:00

abstract：:We previously reported that the functional deletion of p21, a cyclin-dependent kinase inhibitor, in mice attenuated renal cell senescence in streptozotocin (STZ)-induced type 1 diabetic mice. In the present study, we investigated the effect of iron chelation on renal cell senescence and inflammation in the type 1 diab...

journal_title：European journal of pharmacology

authors： Morita T,Nakano D,Kitada K,Morimoto S,Ichihara A,Hitomi H,Kobori H,Shiojima I,Nishiyama A

更新日期：2015-06-05 00:00:00

abstract：:The anti-migraine drug, eletriptan [(R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]-1 H-indole; UK-116,044], is a novel 5-HT(1B/1D) receptor agonist. In this paper, the regional vasoconstrictor profile of eletriptan, in comparison with sumatriptan, was examined in the anaesthetised dog. The inhibit...

journal_title：European journal of pharmacology

authors： Gupta P,Butler P,Shepperson NB,McHarg A

更新日期：2000-06-09 00:00:00

abstract：:Direct instillation of a recombinant human form of MMP-12 (rhMMP-12) in mice airways elicited an early inflammatory response characterized by neutrophil influx, cytokine release and gelatinase activation followed by a delayed response, mainly characterized by macrophage recruitment. As this experimental model of lung ...

journal_title：European journal of pharmacology

authors： Nénan S,Lagente V,Planquois JM,Hitier S,Berna P,Bertrand CP,Boichot E

更新日期：2007-03-15 00:00:00

abstract：:Cytochrome P450 2J2 (CYP2J2) is highly expressed in human tumors and carcinoma cell lines, and has been implicated in the pathogenesis of human cancers. The aim of this study was to identify a compound that could inhibit the activity of CYP2J2, and to examine its anticancer activity. To identify CYP2J2 inhibitors, 10 ...

journal_title：European journal of pharmacology

authors： Jeon YJ,Kim JS,Hwang GH,Wu Z,Han HJ,Park SH,Chang W,Kim LK,Lee YM,Liu KH,Lee MY

更新日期：2015-10-05 00:00:00

abstract：:Insulin resistance is a major pathophysiological feature in the development of type 2 diabetes. The liver is an important organ responsible for the development of insulin resistance, and exploring liver glucose metabolism is important to study insulin resistance. We first established the model of insulin resistance in...

journal_title：European journal of pharmacology

authors： Fan X,Tao J,Zhou Y,Hou Y,Wang Y,Gu D,Su Y,Jang Y,Li S

更新日期：2019-01-15 00:00:00

abstract：:The pharmacological profile of YM358, 2,7-diethyl-5-[[2'-(1 H-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]tri azole potassium salt monohydrate, a novel non-peptide angiotensin AT1 receptor antagonist, was studied in vitro and in vivo. YM358 competed with [125I][Sar1, Ile8]angiotensin II for angiotensi...

journal_title：European journal of pharmacology

authors： Shibasaki M,Fujimori A,Takanashi M,Kusayama T,Tokioka T,Satoh Y,Okazaki T,Uchida W,Inagaki O,Yanagisawa I

更新日期：1997-09-24 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：:The Na(+)/Ca(2+) exchanger (NCX) is involved in myocardial ischemia-reperfusion injuries. We examined the effects of 2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline (SEA0400), a potent and selective inhibitor of NCX, on myocardial ischemia-reperfusion injury models. In canine cardiac sarcolemmal vesicles an...

journal_title：European journal of pharmacology

authors： Takahashi K,Takahashi T,Suzuki T,Onishi M,Tanaka Y,Hamano-Takahashi A,Ota T,Kameo K,Matsuda T,Baba A

更新日期：2003-01-01 00:00:00

abstract：:A recent study indicates that elevation of [Ca(2+)](i) enhances the release of calcein, an anionic fluorescent dye, from isolated exocrine acinar cells, so cytoplasmic calcein is useful for monitoring the secretion of organic anions. In this study, we investigated the effect of cAMP on the calcein release evoked by el...

journal_title：European journal of pharmacology

authors： Sugita M,Hirono C,Furuya K,Yamagishi S,Kanno Y,Shiba Y

更新日期：2000-02-04 00:00:00

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

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

更新日期：1986-02-11 00:00:00

abstract：:The purpose of our study was to examine whether a significant interaction occurs between NMDA and non-NMDA receptor antagonists on respiratory function. For this purpose chloralose-anesthetized cats were used and respiratory minute volume (VE), tidal volume (Vt) respiratory rate (f), inspiratory and expiratory duratio...

journal_title：European journal of pharmacology

authors： McManigle JE,Taveira DaSilva AM,Dretchen KL,Gillis RA

更新日期：1994-01-24 00:00:00

abstract：:The calmodulin inhibitor 1,3-dihydro-1-[1-((4-methyl-4H,6H-pyrrolo[1,2-a]-[4,1]benzoxazepin - 4-yl)methyl)-4-piperidinyl]-2H-benzimidazol-2-one maleate (CGS 9343B) caused a reversible block of voltage-activated Ca2+, Na+, and K+ currents in differentiated rat pheochromocytoma (PC12) cells. The drug also inhibited nico...

journal_title：European journal of pharmacology

authors： Neuhaus R,Reber BF

更新日期：1992-06-05 00:00:00

abstract：:Adenosine 5'-triphosphate (ATP), beta, gamma-methylene ATP and alpha, beta-methylene ATP produced relaxation of carbachol-precontracted isolated trachealis muscle from the guinea-pig in the presence of indomethacin (2.8 microM) and the adenosine uptake inhibitor S-(4-nitrobenzyl)-6-thioinosine (NBTI; 300 nM). The pote...

journal_title：European journal of pharmacology

authors： Piper AS,Hollingsworth M

更新日期：1996-06-27 00:00:00

abstract：:Phenylalanine and tyrosine reportedly decrease blood pressure in conscious restrained rats. However, tyrosine has recently been found to increase blood pressure in anesthetized animals, questioning the generality of findings obtained in restrained animals. The present study therefore evaluated the effects of phenylala...

journal_title：European journal of pharmacology

authors： Yourick DL,Tessel RE

更新日期：1989-01-31 00:00:00

abstract：:The thromboxane A2/prostaglandin endoperoxide (TXA2/PGH2) receptor antagonist activity of CV-4151, a potent TXA2 synthetase inhibitor, was examined. CV-4151 inhibited guinea pig and human platelet aggregation induced by U-44069 with IC50 values of 1.2 +/- 0.3 X 10(-5) and 1.9 +/- 0.4 X 10(-5) M, respectively, and inhi...

journal_title：European journal of pharmacology

authors： Imura Y,Terashita Z,Shibouta Y,Nishikawa K

更新日期：1988-03-15 00:00:00

abstract：:Loss of beta cells is a pathogenic cause for the development of type 2 diabetes. High glucose/free fatty acid (HG/FFA)-induced glucolipotoxicity was thought to play a role in the beta cell loss. Thus, application of small molecules capable of preventing HG/FFA-induced glucolipotoxicty to beta cells could be an avenue ...

journal_title：European journal of pharmacology

authors： Lee SJ,Choi SE,Hwang YC,Jung IR,Yi SA,Jung JG,Ku JM,Jeoung K,Han SJ,Kim HJ,Kim DJ,Lee KW,Kang Y

更新日期：2012-12-05 00:00:00

abstract：:The chick has a practical advantage in the screening process in that chicks require only small quantities of drugs. The chick separation stress paradigm has traditionally been recognized as a valid form of anxiolytic screening. Further, chick behavior involving standing motionless with eyes closed or sitting motionles...

journal_title：European journal of pharmacology

authors： Furuse M

更新日期：2015-09-05 00:00:00

abstract：:The effect of prolonged administration of high doses of buspirone on its 5-hydroxytryptamine (5-HT) release-inhibitory and anxiolytic-like properties was investigated. The 5-HT release-inhibitory effect of a challenge dose of buspirone (0.5 mg/kg, s.c.) was identical in rats chronically treated with vehicle or buspiro...

journal_title：European journal of pharmacology

authors： Söderpalm B,Lundin B,Hjorth S

更新日期：1993-08-03 00:00:00

abstract：:Agonists of adenosine A1 receptors have been frequently proposed as candidates for clinical development in treatment of cerebral ischemia and stroke. Numerous experimental studies have shown that pre- and postischemic administration of these drugs results in a very significant reduction of postischemic brain damage. H...

journal_title：European journal of pharmacology

authors： Von Lubitz DK,Beenhakker M,Lin RC,Carter MF,Paul IA,Bischofberger N,Jacobson KA

更新日期：1996-04-29 00:00:00

abstract：:The influence of degradation by peptidases on concentration-response relationships for peptide agonists of the tachykinin and bombesin-like families was investigated. The combined presence of three peptidase inhibitors, phosphoramidon (1 microM), captopril (1 microM) and bestatin (100 microM), had no significant effec...

journal_title：European journal of pharmacology

authors： Hall JM,Fox AJ,Morton IK

更新日期：1990-02-06 00:00:00

abstract：:The influence of ethanol (0.5, 1.0 and 2.0 g/kg i.p.) on the Bezold-Jarisch reflex in urethane-anaesthetized rats was studied. 5-Hydroxytryptamine (serotonin; 5-HT; 1, 3, 10 and 30 micrograms/kg i.v.) and capsaicin (1, 3 and 10 micrograms/kg i.v.) reflexly decreased heart rate in a dose-dependent manner. The 5-HT3 rec...

journal_title：European journal of pharmacology

authors： Malinowska B,Göthert M,Godlewski G,Wróbel B,Bönisch H,Buczko W

更新日期：1995-05-26 00:00:00

abstract：:To determine if an Ag(+)-induced contracture is associated with the Ca(2+)-induced Ca2+ release mechanism in the sarcoplasmic reticulum, effects of Ca(2+)-induced Ca2+ release modulators on the Ag(+)-induced contracture were studied with single fibers of frog toe skeletal muscle. The fiber treated with 1 mM caffeine c...

journal_title：European journal of pharmacology

authors： Oba T,Nihonyanagi K,Yamaguchi M

更新日期：1995-03-16 00:00:00

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

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

更新日期：1988-07-07 00:00:00

abstract：:In isolated, perfused rabbit ear artery bradykinin, like [Met5]enkephalin and angiotensin II, inhibited neurogenic constrictions in concentrations lower than 10(-8) M without affecting the responses to exogenous norepinephrine. The IC50 value of bradykinin was 1.95 x 10(-10) M. The inhibitory action of bradykinin and ...

journal_title：European journal of pharmacology

authors： Rónai AZ

更新日期：1991-05-30 00:00:00

abstract：:In many vascular smooth muscle cells, physiological and pharmacological agonists initiate oscillatory fluctuations in intracellular Ca(2+) to initiate and maintain vasoconstriction. These oscillations are supported by the underlying cellular ultrastructure, particularly the close apposition between the plasma membrane...

journal_title：European journal of pharmacology

authors： Dai JM,Syyong H,Navarro-Dorado J,Redondo S,Alonso M,van Breemen C,Tejerina T

更新日期：2010-03-10 00:00:00

abstract：:Four analogues of Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2, a mammalian FMRFamide-like peptide with antiopiate properties, were synthesized with N-terminus modifications and were shown to have high affinity for F8Famide binding sites. The degradation rate of these analogues in mouse brain slices was 3 times lower than that...

journal_title：European journal of pharmacology

authors： Gicquel S,Mazarguil H,Allard M,Simonnet G,Zajac JM

更新日期：1992-11-03 00:00:00

abstract：:The specific binding of [3H]desipramine to various brain regions and peripheral tissues of the rat was of high affinity, rapid and reversible. It was inhibited with high affinity only by tricyclic antidepressants and noradrenaline uptake blockers. There was a highly significant correlation between the potencies of a s...

journal_title：European journal of pharmacology

authors： Raisman R,Sette M,Pimoule C,Briley M,Langer SZ

更新日期：1982-03-12 00:00:00