Hexahydrobenzo[a]phenanthridines: novel dopamine D3 receptor ligands.

abstract：:Airway remodeling in asthma is difficult to treat because of its complex pathophysiology that involves proinflammatory cytokines, as well as the arachidonic acid cytochrome P-450 (CYP) pathway; however, it has received little attention. In this study, we assessed the efficacy of a soluble epoxide hydrolase (sEH) on ai...

journal_title：European journal of pharmacology

authors： Jiang JX,Guan Y,Shen HJ,Jia YL,Shen J,Zhang LH,Liu Q,Zhu YL,Xie QM

更新日期：2020-02-05 00:00:00

abstract：:Many of the physiological responses to nitric oxide (NO) are mediated by cyclic 5'-guanosine monophosphate (cGMP), the intracellular levels of which are regulated by phosphodiesterase type 5 (PDE5). In situations of reduced NO formation, the inhibition of PDE5 by selective inhibitors such as sildenafil could be benefi...

journal_title：European journal of pharmacology

authors： Ferreira-Melo SE,Yugar-Toledo JC,Coelho OR,De Luca IM,Tanus-Santos JE,Hyslop S,Irigoyen MC,Moreno H Jr

更新日期：2006-08-07 00:00:00

abstract：:The aim of the present study was to investigate the contribution of extracellular signal regulated kinase-1/2 (ERK1/2) to pulmonary artery contraction in response to 4-aminopyridione (4-AP), an inhibitor of a voltage-gated K(+) channels that regulate pulmonary vascular tone. Pulmonary artery rings 1-1.5 mm in diameter...

journal_title：European journal of pharmacology

authors： Han W,Tang X,Wu H,Liu Y,Zhu D

更新日期：2007-08-13 00:00:00

abstract：:Edaravone is a potent scavenger of hydroxyl radicals and attenuates oxidative damage-related neurodegenerative diseases. Previous studies suggest that oxidative stress plays a key role in the pathogenesis of diabetes. The present study examined the effect of edaravone on diabetes in multiple low-dose streptozotocin-tr...

journal_title：European journal of pharmacology

authors： Fukudome D,Matsuda M,Kawasaki T,Ago Y,Matsuda T

更新日期：2008-03-31 00:00:00

abstract：:3H-Glycine was released by 50 mM K+ in a calcium-dependent manner from rat substantia nigra slices. This release was abolished by GABA (0.1-1 mM) and muscimol (0.1 mM). Taurine and beta-alanine were without effect on evoked 3H-glycine release. The effect of GABA (0.5 mM) was reversed picrotoxin (50 micro M). These res...

journal_title：European journal of pharmacology

authors： Kerwin R,Pycock C

更新日期：1980-06-13 00:00:00

abstract：:Our laboratory recently reported that a group of novel indole quinuclidine analogs bind with nanomolar affinity to cannabinoid type-1 and type-2 receptors. This study characterized the intrinsic activity of these compounds by determining whether they exhibit agonist, antagonist, or inverse agonist activity at cannabin...

journal_title：European journal of pharmacology

authors： Franks LN,Ford BM,Madadi NR,Penthala NR,Crooks PA,Prather PL

更新日期：2014-08-15 00:00:00

abstract：:The present investigation was designed to study the cardioprotective effects of nicorandil and pioglitazone preconditioning in myocardial ischemia/reperfusion-induced hemodynamic, biochemical and histological changes in rats. Oral doses of nicorandil (3 or 6 mg/kg) and pioglitazone (10 or 20mg/kg) were administered on...

journal_title：European journal of pharmacology

authors： Ahmed LA,Salem HA,Attia AS,Agha AM

更新日期：2011-08-01 00:00:00

abstract：:3H-angiotensin binding sites have been studied in a particulate fraction prepared from rat adrenal glands. This binding is rapid and reversible, of high affinity (KD29 degrees C = 3-5 X 10(-9) M) and with demonstrable specificity for the angiotensin II octapeptide. The number of binding sites varies with endogenous an...

journal_title：European journal of pharmacology

authors： Pernollet MG,Devynck MA,Matthews PG,Meyer P

更新日期：1977-06-15 00:00:00

abstract：:N-Methyl-D-aspartate (NMDA)-induced pial artery dilation is reversed to vasoconstriction following fluid percussion brain injury (FPI). This study investigated the contribution of activation of protein tyrosine kinase (PTK) and the extracellular signal-regulated kinase (ERK) and p38 isoforms of mitogen-activated prote...

journal_title：European journal of pharmacology

authors： Armstead WM

更新日期：2003-08-08 00:00:00

abstract：:Endothelins, 21-amino acid peptides involved in the pathogenesis of various diseases, bind to endothelin ET(A) and ET(B) receptors to initiate their effects. Here, we characterize the pharmacology of A-216546 ([2S-(2,2-dimethylpentyl)-4S-(7-methoxy-1,3-benzodioxol-5-yl )-1-(N,N-di(n-butyl) aminocarbonylmethyl)-pyrroli...

journal_title：European journal of pharmacology

authors： Wu-Wong JR,Dixon DB,Chiou WJ,Dayton BD,Novosad EI,Adler AL,Wessale JL,Calzadilla SV,Hernandez L,Marsh KC,Liu G,Szczepankiewicz B,von Geldern TW,Opgenorth TJ

更新日期：1999-02-05 00:00:00

abstract：:The therapeutic efficacy of antidepressant drugs that inhibit the reuptake of serotonin (5-hydroxytryptamine, 5-HT) may be enhanced by blocking their indirect activation of 5-HT(1A) autoreceptors, which mediate feedback inhibition of serotonergic neuronal activity. In this study, we examined the effects of venlafaxine...

journal_title：European journal of pharmacology

authors： Bjorvatn B,Fornal CA,Martín FJ,Metzler CW,Jacobs BL

更新日期：2000-09-15 00:00:00

abstract：:Dexmedetomidine (DMED) is a potent and highly selective α2-adrenergic receptor agonist and is widely used for short-term sedation. However, the mechanism of DMED-induced sedation has not been deciphered. In the present study, we investigated the mechanism of Gαi and Gβγ subunits on DMED-induced sedation. An ED50 of DM...

journal_title：European journal of pharmacology

authors： Liu M,Yang Y,Tan B,Li Y,Zhou P,Su R

更新日期：2018-07-15 00:00:00

abstract：:Venenum Bufonis, a traditional Chinese medicine, is widely used in the treatment of liver cancer in modern Chinese medical practices. In our search for anti-hepatoma constituents in Venenum Bufonis, bufotalin, bufalin, telocinobufagin and cinobufagin were obtained. Bufotalin was the most potent active compound among t...

journal_title：European journal of pharmacology

authors： Zhang DM,Liu JS,Tang MK,Yiu A,Cao HH,Jiang L,Chan JY,Tian HY,Fung KP,Ye WC

更新日期：2012-10-05 00:00:00

abstract：:It is well documented that cannabinoid receptor agonist WIN 55,212-2 had protective effect against cerebral ischemic injury. Our previous study indicated that WIN 55,212-2 pretreatment induced ischemic tolerance to focal cerebral ischemia in a dose-dependent manner. The aim of the present study was to investigate the ...

journal_title：European journal of pharmacology

authors： Hu B,Wang Q,Chen Y,Du J,Zhu X,Lu Y,Xiong L,Chen S

更新日期：2010-10-25 00:00:00

abstract：:The anticancer drugs camptothecin (CPT) and topotecan (TPT) are known DNA topoisomerase I inhibitors which cause DNA damage and lead to cell death. In this study we provide evidence that CPT and TPT also interfere with the elements of cytoskeleton - microtubules and actin filaments which could be partly responsible fo...

journal_title：European journal of pharmacology

authors： Wang X,Tanaka M,Krstin S,Peixoto HS,Moura CCM,Wink M

更新日期：2016-10-15 00:00:00

abstract：:Increased motor activity and poor performance in the active avoidance test were observed in the offspring of rats treated with dl-propranolol or sotalol during pregnancy, but not with atenolol and d-propranolol. All substances were administered in drinking water from days 8-22 of gestation. A significant increase in t...

journal_title：European journal of pharmacology

authors： Speiser Z,Gordon I,Rehavi M,Gitter S

更新日期：1991-03-19 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 efficacy of a novel, nonpeptidic, caspase 3/7-selective inhibitor, (S)-(+)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin (MMPSI) for reducing ischemic injury in isolated rabbit hearts or cardiomyocytes was evaluated. MMPSI (0.1-10 microM) evoked a concentration-dependent reduction in infarct size (up to 56% vs...

journal_title：European journal of pharmacology

authors： Chapman JG,Magee WP,Stukenbrok HA,Beckius GE,Milici AJ,Tracey WR

更新日期：2002-12-05 00:00:00

abstract：:The mesolimbic dopaminergic innervation is supposed to be involved in the mechanisms of central effects exerted by various classes of psychotropic drugs. Antidepressants have been found to interact with the brain dopaminergic system as well, although the precise central location of this interaction is unknown. Some da...

journal_title：European journal of pharmacology

authors： Plaznik A,Kostowski W

更新日期：1987-03-31 00:00:00

abstract：:In the present study, the development of tolerance to the motor impairing effects of gamma-hydroxybutyric acid (GHBA) and ethanol was compared (Experiment 1). Rats were required to perform a motor coordination task daily shortly after ethanol (3.5 g/kg) and GHBA (1.0 g/kg) administration for 9 consecutive days. Tolera...

journal_title：European journal of pharmacology

authors： Colombo G,Agabio R,Lobina C,Reali R,Fadda F,Gessa GL

更新日期：1995-02-06 00:00:00

abstract：:D-amino acid oxidase (DAAO) is an astroglial enzyme abundantly present in the pain sensing regions including brain and spinal cord. There have been studies indicating an upregulation and increased activity of DAAO in different pain models. Furthermore, the upregulation of DAAO also results in the development of morphi...

journal_title：European journal of pharmacology

authors： Sharma J,Kulshrestha R,Singh N,Jaggi AS

更新日期：2019-07-15 00:00:00

abstract：:In the rat distal colon, 5-hydroxytryptamine (5-HT)-induced Cl- secretion is seen as a rise in short circuit current (Isc). We investigated the 5-HT receptor mediating 5-HT-induced Cl- secretion in the rat distal colon. Rat distal colon was prepared either by stripping away the muscularis propria with the neural gangl...

journal_title：European journal of pharmacology

authors： Budhoo MR,Harris RP,Kellum JM

更新日期：1996-03-07 00:00:00

abstract：:The Kd values of the multiple agonist binding sites in cardiac muscarinic receptors (mAChR) and pD2 values for negative inotropic actions were determined independently and their relation was examined. The guinea-pig cardiac mAChR is known to have three agonist binding sites (super-high (SH), high (H) and low (L) affin...

journal_title：European journal of pharmacology

authors： Mizushima A,Uchida S,Matsumoto K,Osugi T,Kagiya T,Zhou XM,Higuchi H,Yoshida H

更新日期：1985-12-17 00:00:00

abstract：:gamma-Acetylenic GABA (100 mg/kg i.p.) inhibited GABA-transaminase activity and caused a several-fold increase in the concentration of GABA in rat brain. This increased GABA concentration was associated with a decreased rate of dopamine depletion following alpha-methyl-p-tyrosine treatment and a decrease in homovanill...

journal_title：European journal of pharmacology

authors： Palfreyman MG,Huot S,Lippert B,Schechter PJ

更新日期：1978-08-15 00:00:00

abstract：:Cardiovascular and behavioral responses induced by intravenous administration of the serotonin (5-HT)1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), were studied in conscious normotensive rats either after a single administration, after repeated subcutaneous treatments (1 mg/kg daily for 3 day...

journal_title：European journal of pharmacology

authors： Kolbasa KP,McCall RB,Ludens JH

更新日期：1991-02-14 00:00:00

abstract：:High stereoselectivity was observed for the enantiomers of trihexyphenidyl and trihexyphenidyl methiodide at muscarinic M1-receptors in field-stimulated rabbit vas deferens and at M2 alpha- and M2 beta-receptors in guinea-pig atrium and ileum, respectively. Considerably higher affinities (up to 1700-fold) were found f...

journal_title：European journal of pharmacology

authors： Lambrecht G,Feifel R,Moser U,Aasen AJ,Waelbroeck M,Christophe J,Mutschler E

更新日期：1988-10-11 00:00:00

abstract：:Diabetic osteopenia can result in an increased incidence of bone fracture and a delay in fracture healing. Quercetin, one of the most widely distributed flavonoids in plants, possesses antioxidant property and beneficial effect on osteoporosis in ovariectomized mice. All these properties make quercetin a potential can...

journal_title：European journal of pharmacology

authors： Liang W,Luo Z,Ge S,Li M,Du J,Yang M,Yan M,Ye Z,Luo Z

更新日期：2011-11-16 00:00:00

abstract：:Experiments were designed to determine whether or not ketanserin (R 41 468) antagonizes the augmentation by 5-hydroxytryptamine of contractions evoked in isolated arteries by non-adrenergic vasoconstrictor substances. Rings of rabbit femoral arteries were studied under isometric conditions in organ chambers filled wit...

journal_title：European journal of pharmacology

authors： Van Nueten JM,Janssen PA,De Ridder A,Vanhoutte PM

更新日期：1982-02-05 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：:The purpose of this study was to investigate whether the selective angiotensin AT2 receptor ligands, CGP 42112B (Nic-Tyr-(N alpha-benzoyloxycarbonyl-Arg)Lys-His-Pro-Ile-OH) and PD 123319 ((s)-1-[[4-(dimethylamino)-3-methyl-phenyl]methyl]-5-(diphenylacetyl+ ++)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]-pyridine-6-carboxylic...

journal_title：European journal of pharmacology

authors： Macari D,Whitebread S,Cumin F,De Gasparo M,Levens N

更新日期：1994-06-23 00:00:00