Effects of fluoroquinolones on HERG currents.

abstract：:The bisquaternary compound dequalinium has been tested for its ability to inhibit the loss of K+ which angiotensin II causes in guinea-pig hepatocytes and which occurs through apamin-sensitive Ca(2+)-activated K+ (SKCa) channels. Dequalinium blocked angiotensin II-evoked K+ loss with an IC50 of 1.5 +/- 0.1 microM and ...

journal_title：European journal of pharmacology

authors： Castle NA,Haylett DG,Morgan JM,Jenkinson DH

更新日期：1993-05-19 00:00:00

abstract：:UP 269-6, 5-methyl-7-propyl-8(-)[2'-(1H-tetrazol-5-yl)biphenyl-4- yl)methyl]-1,2,4-triazolo]1,5-c]pyrimidin-2(3H)-one is a novel nonpeptide angiotensin II receptor antagonist. In vivo studies were performed to evaluate UP 269-6 for its angiotensin II antagonistic action. In pithed rats, i.v. administration of UP 269-6...

journal_title：European journal of pharmacology

authors： Cazes M,Provost D,Versigny A,Cloarec A

更新日期：1995-09-15 00:00:00

abstract：:The functional characteristics of purinoceptors in Chinese hamster ovary (CHO) cells were investigated using a microphysiometer which detects small metabolic changes to living cells in real-time as variations of pH in the extracellular microenvironment. Uridine 5'-triphosphate (UTP) increased the extracellular acidifi...

journal_title：European journal of pharmacology

authors： Okada Y,Taniguchi T,Akagi Y,Muramatsu I

更新日期：2002-11-22 00:00:00

abstract：:We found that pergolide, a dopamine D1/D2 receptor agonist used in the clinical therapy of Parkinson's disease, protects SH-SY5Y neuroblastoma cells from cell death induced by a brief pulse (15 min) of 1 mM H(2)O(2). Neuroprotection was found when pergolide was added to the culture medium either simultaneously with (E...

journal_title：European journal of pharmacology

authors： Uberti D,Piccioni L,Colzi A,Bravi D,Canonico PL,Memo M

更新日期：2002-01-02 00:00:00

abstract：:The binding of [3H]LSD to serotonergic sites in human brain was studied. The pharmacological profile of [3H]LSD binding in frontal cortex differed to that in hippocampus. Analysis of the inhibition of [3H]LSD binding by serotonin and spiperone was consistent with the presence of two binding sites, which differed in ph...

journal_title：European journal of pharmacology

authors： Cross AJ

更新日期：1982-08-13 00:00:00

abstract：:Blockade of sodium channels located in the sinoatrial node can slow diastolic depolarisation rate, recorded in vitro. The objective was therefore to determine whether these blockers could slow heart rate in vivo. The heart rate was firstly measured in spontaneously beating, isolated rat heart atria in the presence of ...

journal_title：European journal of pharmacology

authors： Létienne R,Vié B,Le Grand B

更新日期：2006-01-20 00:00:00

abstract：UNLABELLED:The influence of different nonsteroidal anti-inflammatory drugs (NSAIDs) and of a proton pump inhibitor on the healing parameters of a chronic gastric ulcer was evaluated. Wistar rats were used after the induction of a chronic acetic acid ulcer. The animals were treated orally for 8 and 15 days, twice daily,...

journal_title：European journal of pharmacology

authors： Berenguer B,Alarcón de la Lastra C,Moreno FJ,Martín MJ

更新日期：2002-05-03 00:00:00

abstract：:The in vitro biological effect of various opiates was studied in the guinea pig ileum bioassay. Besides their direct, immediate effect, certain opiates induced sensitivity changes which persisted after their removal and the complete recovery of the preparation. These specific, asymmetrical interactions may represent l...

journal_title：European journal of pharmacology

authors： Sarne Y,Gothilf Y,Weissman BA

更新日期：1980-03-07 00:00:00

abstract：:Chronic restraint stress (CRS) is known to cause metabolic and neurological complications in a number of ways. Prolonged exposure to stress evident by increased corticosterone level led to impaired altered insulin signaling and oxidative stress in mice, in the present study. Impaired insulin signaling or insulin resis...

journal_title：European journal of pharmacology

authors： Mourya A,Akhtar A,Ahuja S,Sah SP,Kumar A

更新日期：2018-09-15 00:00:00

abstract：:Annexin A1 (ANXA1)-formyl peptide receptor (Fpr) system is potent effective mediators in the control of the inflammatory response. In this study, we evaluate the potential involvement of the Fpr family in the protective effect of the mimetic peptide of ANXA1 (ANXA12-26) using an experimental allergic conjunctivitis (A...

journal_title：European journal of pharmacology

authors： Marmorato MP,Gimenes AD,Andrade FEC,Oliani SM,Gil CD

更新日期：2019-01-05 00:00:00

abstract：:The endogenous release of adenosine 5'-triphosphate (ATP) from strips of guinea-pig gallbladder during transmural stimulation (TS) was measured with a firefly luciferine-luciferase reaction. TS (15V, 1 ms, 0.5-5 Hz, for 1 min) caused a rapid and marked increase of ATP release in a frequency-dependent manner. Both ATP ...

journal_title：European journal of pharmacology

authors： Takahashi T,Kusunoki M,Ishikawa Y,Kantoh M,Yamamura T,Utsunomiya J

更新日期：1987-01-28 00:00:00

abstract：:Protons and capsaicin activate overlapping subsets of sensory nerves by opening ion conductances of similar properties. We have used the [3H]resiniferatoxin binding assay utilizing rat spinal cord membranes to elucidate the possible interaction of protons at the vanilloid (capsaicin) receptor. Using low pH (pH 6.0 and...

journal_title：European journal of pharmacology

authors： Szallasi A,Blumberg PM,Lundberg JM

更新日期：1995-04-28 00:00:00

abstract：:Transporter-mediated release of dopamine and the parkinsonism-inducing neurotoxin 1-methyl-4-phenylpyridinium (MPP+) was examined in COS cells, a cell line derived from monkey kidney, expressing the rat dopamine transporter. The release of preloaded [3H]MPP+ but not [3H]dopamine was dose-dependently inhibited by cocai...

journal_title：European journal of pharmacology

authors： Kitayama S,Morita K,Dohi T

更新日期：1996-08-01 00:00:00

abstract：:The aim of the study was to determine the influence of N-(ortho-carboxyanilinomethyl)-p-isopropoxyphenylsuccinimide [o-CAMIPPS], N-(meta-carboxyanilinomethyl)-p-isopropoxyphenylsuccinimide [m-CAMIPPS], and N-(para-carboxyanilinomethyl)-p-isopropoxyphenylsuccinimide [p-CAMIPPS] on the protective activity of four classi...

journal_title：European journal of pharmacology

authors： Luszczki JJ,Cioczek JD,Kocharov SL,Andres-Mach M,Kominek M,Zolkowska D

更新日期：2010-12-01 00:00:00

abstract：:Cutaneous arteries are known to constrict in response to cooling via α2C-adrenoceptors. The involvement of α1-adrenoceptors in the cooling response has also recently been suggested by in vivo studies in mice. The present study was thus aimed to confirm it in the isolated mouse cutaneous plantar artery. Changes in vess...

journal_title：European journal of pharmacology

authors： Goto K,Saito SY,Ishikawa T

更新日期：2014-11-05 00:00:00

abstract：:A microdialysis/smallbore chromatographic system was used to monitor changes in extracellular dopamine concentration in the striatum of the rat following administration of drugs that block catecholamine uptake. Analysis of 0.5 microliter of dialysate every 5 min showed dose-dependent elevations in extracellular dopami...

journal_title：European journal of pharmacology

authors： Church WH,Justice JB Jr,Byrd LD

更新日期：1987-07-23 00:00:00

abstract：:Prior studies demonstrated that guanabenz reduces systemic blood pressure by inhibiting central sympathetic outflow as well as by adrenergic neuron blockade. Potential mechanisms responsible for the reduction of efferent sympathetic activity were examined in the present series. Guanabenz failed to modify carotid sinus...

journal_title：European journal of pharmacology

authors： Baum T,Shropshire AT

更新日期：1976-05-01 00:00:00

abstract：:Two novel 8 alpha-amino ergolines (CH 29-717 and CU 32-085) have been shown to inhibit secretion of prolactin in rats in vivo. However, when tested for dopaminomimetic potency on pituitary cell culture preparations in vitro, CH 29-717 inhibited prolactin release with an IC50 = 4 X 10(-9) M. In the same model the 1-met...

journal_title：European journal of pharmacology

authors： Markó M

更新日期：1984-06-01 00:00:00

abstract：:The effects of pentobarbital on heart rate, reflexly mediated vagal activity and the automaticity (intrinsic rate) of the sinoatrial (SA) node were investigated in rabbits. When administered in three cumulative doses (10 mg/kg i.v. each) at 15 min intervals, each dose produced transient hypotension which was not modif...

journal_title：European journal of pharmacology

authors： Murthy VS,Zagar ME,Vollmer RR,Schmidt DH

更新日期：1982-10-15 00:00:00

abstract：:Five different muscarinic receptor subtypes can be distinguished by the differences in their amino acid sequence, the coupled signal transduction system, pharmacological binding properties and activation of ionic fluxes. The present study served to characterize the binding profile of muscarinic receptors in human colo...

journal_title：European journal of pharmacology

authors： Kopp R,Lambrecht G,Mutschler E,Moser U,Tacke R,Pfeiffer A

更新日期：1989-10-17 00:00:00

abstract：:Given the differences in the dopamine neurotransmission between the shell and the core of the nucleus accumbens, as well as the differential involvement of these two domains in oral behaviour of rats, it was decided to determine whether or not dopamine D1 and/or dopamine D2 receptors differentially direct oral behavio...

journal_title：European journal of pharmacology

authors： Cools AR,Miwa Y,Koshikawa N

更新日期：1995-11-03 00:00:00

abstract：:N(G)-(Nitro-L-arginine (L-NOARG), an inhibitor of nitric oxide synthase, induces catalepsy in mice. The objective of the present work was to investigate if serotonergic drugs are able to modulate this effect. Results showed that the cataleptogenic effect of L-NOARG (40 mg/kg) in male albino-Swiss mice was enhanced by ...

journal_title：European journal of pharmacology

authors： Nucci-da-Silva LP,Guimarães FS,Del Bel EA

更新日期：1999-08-20 00:00:00

abstract：:Donor-specific antibodies (DSA) are a major risk factor for antibody-mediated rejection (ABMR) in solid organ transplantation, and ABMR remains a medical challenge. Therefore, effective anti-ABMR therapies are needed to improve overall graft survival. Cathepsin S (Cat S) is an essential protease for antigen peptide lo...

journal_title：European journal of pharmacology

authors： Kubo K,Kawato Y,Nakamura K,Nakajima Y,Nakagawa TY,Hanaoka K,Oshima S,Fukahori H,Inami M,Morokata T,Higashi Y

更新日期：2018-11-05 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：:We aimed to determine the presence of oxidative stress in rhinitis medicamentosa (RM) and to evaluate the effect of erdosteine (ED) on mucosal changes in a rat model. Twenty-four male rats were used in this experimental study. Three groups were created. Group 1 (n=8) was the control group. Two puffs of 0.05% oxymetazo...

journal_title：European journal of pharmacology

authors： Dokuyucu R,Cevik C,Ozler GS,Ozgur T,Arli C,Sefil F,Yonden Z

更新日期：2014-11-05 00:00:00

abstract：:Clinical evidence indicates an antiarrhythmic effect of sulfonylureas, which might be blunted by their vascular action. We wanted to investigate the effect of glibenclamide and the new sulfonylthiourea compound 1-[[5-[2-(5-chloro-o-anisamido)ethyl]-2-methoxyphenyl]-sulfonyl]-3 -me thylthiourea (HMR1883) on cardiac ele...

journal_title：European journal of pharmacology

authors： Dhein S,Pejman P,Krüsemann K

更新日期：2000-06-16 00:00:00

abstract：:The effect of dimethyl sulfoxide (DMSO) on the slow ventral root potential, which is related to nociceptive transmission, was investigated in the isolated spinal cord of a newborn rat. DMSO at 0.3-1% (v/v) enhanced the slow ventral root potential, but not mono- and polysynaptic reflex discharges. DMSO at 1% also enhan...

journal_title：European journal of pharmacology

authors： Kubota K,Fujibayashi K,Saito K

更新日期：1998-06-19 00:00:00

abstract：:Lipopolysaccharide (LPS) administration in rats induces a characteristic syndrome termed 'sickness behavior', including profound changes on locomotor activity and circulating stress and inflammatory mediators. The aim of the present investigation was to evaluate whether the behavioral and the peripheral biomarker resp...

journal_title：European journal of pharmacology

authors： Bison S,Razzoli M,Arban R,Michielin F,Bertani S,Carboni L

更新日期：2011-07-01 00:00:00

abstract：:T-type Ca(2+) currents were recorded in 2 mM Ca(2+) from HEK293 cells stably expressing the low voltage-activated Ca(2+) channel sub-unit alpha(1I). These currents were inhibited by the known Ca(2+) channel antagonist mibefradil with an IC(50) close to 1 microM. SB-209712 (1,6,bis¿1-[4-(3-phenylpropyl)piperidinyl]¿hex...

journal_title：European journal of pharmacology

authors： McNaughton NC,Warre R,Cooper DG,Nasir S,Ranson JL,Randall A

更新日期：2000-10-27 00:00:00

abstract：:The protective potency of ischemic preconditioning decreases with increasing age. A key step in ischemic preconditioning is the opening of mitochondrial Ca(2+) sensitive K(+) (mK(Ca)) channels, which causes mild uncoupling of mitochondrial respiration. We hypothesized that aging reduces the effects of mK(Ca) channel o...

journal_title：European journal of pharmacology

authors： Heinen A,Winning A,Schlack W,Hollmann MW,Preckel B,Frässdorf J,Weber NC

更新日期：2008-01-14 00:00:00