BIIE0246: a selective and high affinity neuropeptide Y Y(2) receptor antagonist.

abstract：:The vasoinhibitory effects of MCI-154 (MCI), a new pyridazione derivative, on contractile responses to alpha 1- and alpha 2-adrenoceptor agonists were examined in isolated rabbit aorta. MCI (10(-8)-10(-5) M) inhibited the maximum contractile responses to clonidine and BHT-920 (BHT) in a concentration-dependent manner,...

journal_title：European journal of pharmacology

authors： Shibata S,Satake N,Hester RK,Kurahashi K,Ito M

更新日期：1988-01-12 00:00:00

abstract：:The number of prolactin (PRL) receptors in the hypothalamus and substantia nigra of aged rabbits is significantly lower than the number measured in young animals. The treatment of aged rabbits for 30 days with S-adenosyl-L-methionine (SAM) restored the number of PRL binding sites to levels found in the hypothalamus an...

journal_title：European journal of pharmacology

authors： Muccioli G,Di Carlo R

更新日期：1989-07-18 00:00:00

abstract：:The effects of treatment with anxiogenic or anxiolytic agents and exposure to acute restraint stress on emotional behavior in mice were examined using an automatic hole-board apparatus. Changes in the emotional state of mice were evaluated in terms of changes in exploratory activity, i.e., total locomotor activity, nu...

journal_title：European journal of pharmacology

authors： Takeda H,Tsuji M,Matsumiya T

更新日期：1998-05-29 00:00:00

abstract：:The calcium sensitivity of ouabain-induced contractions of aortic strips from spontaneously hypertensive rat (SHR) was examined using several drugs which affect Na+ and Ca2+ movements across the cell membrane, and the results were compared with those obtained with age-matched Wistar-Kyoto rat (WKY). The Ca2+ concentra...

journal_title：European journal of pharmacology

authors： Shibata R,Morita S,Nagai K,Miyata S,Iwasaki T

更新日期：1990-11-06 00:00:00

abstract：:This study was undertaken to define some of the cellular mechanisms of action of serotonin on cerebral vascular muscle. Application of serotonin to cat basilar artery resulted in a dose dependent depolarization and contraction beginning at 10(-8) M. The correlation coefficient relating the degree of force development ...

journal_title：European journal of pharmacology

authors： Harder DR,Waters A

更新日期：1983-09-16 00:00:00

abstract：:The possibility of a role of hypothalamic growth hormone (GH)-releasing factor (GRF) in GH secretion induced by centrally administered galanin was investigated in freely moving male rats. Intracerebroventricular (i.c.v.) injection of synthetic galanin (0.4 or 2 micrograms/rat) elicited a dose-related increase in plasm...

journal_title：European journal of pharmacology

authors： Murakami Y,Kato Y,Koshiyama H,Inoue T,Yanaihara N,Imura H

更新日期：1987-04-29 00:00:00

abstract：:Agelanthus dodoneifolius is one of the medicinal plants used in African pharmacopeia and traditional medicine for the treatment of cardiovascular diseases. A chemical analysis has identified one of the active principles: Dodoneine (Ddn). It is a new dihydropyranone which exerts hypotensive and vasorelaxant effects on ...

journal_title：European journal of pharmacology

authors： Carré G,Carreyre H,Ouedraogo M,Becq F,Bois P,Thibaudeau S,Vandebrouck C,Bescond J

更新日期：2014-04-05 00:00:00

abstract：:The aim of this study was to correlate mineralocorticoid action and steroid structure. Inasmuch as Na(+) retention follows a parabolic dose-response curve for most pregnanesteroids, the second-order coefficient of the function was used as a representative factor for this bipartite biological effect. The C(3)=O/D angle...

journal_title：European journal of pharmacology

authors： Piwien-Pilipuk G,Kanelakis KC,Galigniana MD

更新日期：2002-11-15 00:00:00

abstract：:We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Wh...

journal_title：European journal of pharmacology

authors： Bräuner-Osborne H,Hermit MB,Nielsen B,Krogsgaard-Larsen P,Johansen TN

更新日期：2000-10-06 00:00:00

abstract：:Activation of serotonergic 5-HT3 receptors by its selective agonist 2-methyl serotonin (2-Me-5-HT) induces vomiting, which is sensitive to selective antagonists of both 5-HT3 receptors (palonosetron) and L-type calcium channels (LTCC) (amlodipine or nifedipine). Previously we demonstrated that 5-HT3 receptor activatio...

journal_title：European journal of pharmacology

authors： Hutchinson TE,Zhong W,Chebolu S,Wilson SM,Darmani NA

更新日期：2015-05-15 00:00:00

abstract：:Acute administration of delta 9-tetrahydrocannabinol (THC) (50 mg/kg) at puberty (35-40 days) significantly (P less than 0.05) reduced Ca2+ ATPase activity in hypothalamic plasma membranes but increased, although not significantly, enzyme activity in hypothalamic tissue obtained from adult mice. In contrast, testicula...

journal_title：European journal of pharmacology

authors： Dalterio SL,Bernard SA,Esquivel CR

更新日期：1987-05-07 00:00:00

abstract：:The 5-lipoxygenase inhibitors WY-50,295 tromethamine, A-64,077, L-663,536 and ICI-207,968 were compared in a reverse passive Arthus reaction-induced pleurisy model of eicosanoid biosynthesis in the rat. When a 1 h pretreatment schedule was employed, all four inhibitors equivalently blocked leukotriene B4 (LTB4) produc...

journal_title：European journal of pharmacology

authors： Berkenkopf JW,Weichman BM

更新日期：1991-01-25 00:00:00

abstract：:This paper presents the effect of 14-day intraperitoneal (i.p.) neuroleptic treatment on the behavioural response of Wistar rats to (-)-quinpirole hydrochloride (3 mg/kg, i.p.) administered 24 h after the last neuroleptic dose. Chlorpromazine hydrochloride (10 mg/kg), haloperidol (2 mg/kg) or (+/-)-sulpiride (100 mg/k...

journal_title：European journal of pharmacology

authors： Obuchowicz E

更新日期：1999-11-19 00:00:00

abstract：:We determined the role of high-grade inflammation on endothelial function and its association with biomarkers of endothelial dysfunction in collagen-induced arthritis. Sprague-Dawley rats were divided into a control (n = 12) or collagen-induced arthritis (CIA; n = 21) group. To induce arthritis, Bovine-type-II collage...

journal_title：European journal of pharmacology

authors： Mokotedi L,Millen AME,Mogane C,Gomes M,Woodiwiss AJ,Norton GR,Michel FS

更新日期：2019-12-15 00:00:00

abstract：:Paracetamol is one of the first rank drugs which cause hepatic damage during drug intoxications. Endothelin (ET) which is known as one of the most potent vasoactive agent has been shown to contribute in the pathophysiology of various diseases. We hypothesized that bosentan, which is a non-selective ET-1 receptor antag...

journal_title：European journal of pharmacology

authors： Yayla M,Halici Z,Unal B,Bayir Y,Akpinar E,Gocer F

更新日期：2014-03-05 00:00:00

abstract：:Dantrolene sodium (3 X 10(-4) M) exerted a biphasic effect on the mechanical and electrical activity of the isolated guinea pig left atrium. In the first phase, the drug increased the contractile force by about 200%, and prolonged the action potential duration. This transient positive inotropic effect was antagonized ...

journal_title：European journal of pharmacology

authors： Mészáros J,Kecskeméti V,Szegi J

更新日期：1981-09-11 00:00:00

abstract：:Synthesis of the vasoconstrictor peptide endothelin-1 by endothelial and epithelial cells is strongly induced by tumor necrosis factor alpha (TNF-alpha). The actions of TNF-alpha are mediated by two transmembrane receptors of approximately 55 (p55, CD120a) and 75 kDa (p75, CD120b). Reagents activating selectively thes...

journal_title：European journal of pharmacology

authors： Lees DM,Pallikaros Z,Corder R

更新日期：2000-02-25 00:00:00

abstract：:Naloxone, a competitive antagonist of opioid receptors, and placebo (dextrose 5% in water (D5W) were administered on separate days to healthy normotensive (NT) male volunteers and to male patients with essential hypertension (HT). A single-blind, placebo-controlled, cross-over design was employed. Increasing doses of ...

journal_title：European journal of pharmacology

authors： Fuenmayor N,Cubeddu L

更新日期：1986-07-31 00:00:00

abstract：:NO plays a key role in the pathological mechanisms of articular diseases. As cytoskeletal proteins are responsible for the polymerization, stabilization, and dynamics of the cytoskeleton network, we investigated whether cytoskeletal proteins are the intracellular pathological targets of NO. We aimed at clarifying whet...

journal_title：European journal of pharmacology

authors： Kao XB,Chen Q,Gao Y,Fan P,Chen JH,Wang ZL,Wang YQ,Chen YN,Yan YP

更新日期：2018-04-05 00:00:00

abstract：:Clonidine and methysergide constrict the rabbit auricular artery by activating smooth muscle alpha-adrenoceptors. Clonidine inhibits and methysergide enhances responses to stimulation of the sympathetic nerves. Both drugs sensitise the artery to a variety of vasoconstrictor stimuli, although not to potassium chloride....

journal_title：European journal of pharmacology

authors： Fozard JR

更新日期：1976-03-01 00:00:00

abstract：:The relationship between isometric tension and the increase in cyclic GMP level associated with the initial phase of drug-induced contraction of taenia coli was studied. Maximal contraction induced by 100 micrometers carbachol or 124 mM KCl occurred in 30 sec and was associated with an increase in cyclic GMP levels of...

journal_title：European journal of pharmacology

authors： Janis RA,Diamond J

更新日期：1981-03-12 00:00:00

abstract：:The effects of angiotensin I-converting enzyme (ACE) inhibitors and bradykinin (BK) on prostacyclin (PGI2) production in isolated arterial tissue were investigated. Rings of rat abdominal aorta were incubated in Krebs-Ringer bicarbonate buffer and PGI2 generation was assessed by the determination of its stable hydroly...

journal_title：European journal of pharmacology

authors： Hoffmann G,Pietsch R,Göbel BO,Weisser B,Bönner G,Vetter H,Düsing R

更新日期：1990-03-13 00:00:00

abstract：:Ro 40-5967 [(1S,2S)-2-[2[3-(2-benzamidopropyl]- methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl- methoxyacetate] is a new Ca2+ channel antagonist active at L-type channels. Radioligand binding studies in cardiac tissue show that Ro 40-5967 does not inhibit 1,4-dihydropyridine binding, but does in...

journal_title：European journal of pharmacology

authors： Rutledge A,Triggle DJ

更新日期：1995-07-04 00:00:00

abstract：:Apomorphine (50 micrograms/kg) induced repeated episodes of yawning, penile erection and genital grooming in rats. A dose of cycloheximide, which inhibited brain protein synthesis by 50% totally prevented apomorphine-induced yawning and reduced by approximately 50% the occurrence of episodes of penile erection and gen...

journal_title：European journal of pharmacology

authors： Serra G,Fratta W,Collu M,Napoli-Farris L,Gessa GL

更新日期：1982-12-24 00:00:00

abstract：:Dietary fish oils rich in n-3 polyunsaturated fatty acids can modulate a diverse range of factors contributing to cardiovascular disease. This study examined the relative roles of eicosapentaenoic acid (20:5 n-3; EPA) and docosahexaenoic acid (22:6 n-3; DHA) which are the principal n-3 polyunsaturated fatty acids rega...

journal_title：European journal of pharmacology

authors： McLennan P,Howe P,Abeywardena M,Muggli R,Raederstorff D,Mano M,Rayner T,Head R

更新日期：1996-04-04 00:00:00

abstract：:Intraperitoneal administration of phencyclidine (PCP, 2.5-20 mg/kg) produced a dose-related inhibition of the increase in serum PRL concentrations produced by alpha-methylparatyrosine (AMPT) or reserpine, but not morphine. Phencyclidine was more potent in antagonizing the PRL-releasing effect of reserpine than that of...

journal_title：European journal of pharmacology

authors： Meltzer HY,Simonovic M,Gudelsky GA

更新日期：1985-03-26 00:00:00

abstract：:Increased glycolysis under hypoxic stress is a fundamentally important feature of non-small cell lung cancer (NSCLC) cells, but molecular mechanisms of hypoxia on glycolysis remain elusive. Herein, we aimed to explore whether lncRNAs and miRNAs are involved in the glycolytic reprogramming under hypoxic conditions. The...

journal_title：European journal of pharmacology

authors： Shi J,Wang H,Feng W,Huang S,An J,Qiu Y,Wu K

更新日期：2019-11-05 00:00:00

abstract：:The present study was carried out to clarify the role of nonselective cation channels as a Ca2+ entry pathway in the contraction and the increase in [Ca2+]i induced by endothelin- in endothelium-denuded rat thoracic aorta rings, and their suppression by nitric oxide (NO). In Ca2+-free medium, the endothelin-1-induced ...

journal_title：European journal of pharmacology

authors： Zhang XF,Komuro T,Miwa S,Minowa T,Iwamuro Y,Okamoto Y,Ninomiya H,Sawamura T,Masaki T

更新日期：1998-07-10 00:00:00

abstract：:Forskolin inhibited the response to electrical field stimulation (0.1 Hz) and antagonised contractile responses to noradrenaline in the isolated rat vas deferens. The inhibition of the response to electrical stimulation (IC50 0.1 microM) was not affected by either propranolol or yohimbine. Both isoprenaline and forsko...

journal_title：European journal of pharmacology

authors： Hovevei-Sion D,Finberg JP,Bomzon A,Youdim MB

更新日期：1983-11-25 00:00:00

abstract：:Transient receptor potential melastatin 2 (TRPM2) is an oxidative stress-sensitive Ca2+-permeable channel. The activation of TRPM2 by H2O2 causes cell death in various types of cells. 5-Fluorouracil (5-FU) is an important anticancer drug, but myelosuppression is one of the most frequent adverse effects. The involvemen...

journal_title：European journal of pharmacology

authors： Ishibashi M,Ishii M,Yamamoto S,Mori Y,Shimizu S

更新日期：2021-01-15 00:00:00