Formation of 6-keto prostaglandin E1 in mammalian kidneys.

abstract：BACKGROUND AND PURPOSE:Quercetin is a natural polyphenolic flavonoid that displays anti-diabetic properties in vivo. Its mechanism of action on insulin-secreting beta cells is poorly documented. In this work, we have analysed the effects of quercetin both on insulin secretion and on the intracellular calcium concentrat...

journal_title：British journal of pharmacology

authors： Bardy G,Virsolvy A,Quignard JF,Ravier MA,Bertrand G,Dalle S,Cros G,Magous R,Richard S,Oiry C

更新日期：2013-07-01 00:00:00

abstract：:1 New 2H-1,4-benzoxazine derivatives were synthesized and tested for their agonist properties on the ATP-sensitive K(+) channels (K(ATP)) of native rat skeletal muscle fibres by using the patch-clamp technique. The novel modifications involved the introduction at position 2 of the benzoxazine ring of alkyl substituent...

journal_title：British journal of pharmacology

authors： Tricarico D,Barbieri M,Antonio L,Tortorella P,Loiodice F,Camerino DC

更新日期：2003-05-01 00:00:00

abstract：:1 Neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) differentially activate three Y receptors (Y(1), Y(2) and Y(4)) in mouse and human isolated colon. 2 The aim of this study was to characterise Y(2) receptor-mediated responses in colon mucosa and longitudinal smooth muscle preparations from wild ...

journal_title：British journal of pharmacology

authors： Hyland NP,Sjöberg F,Tough IR,Herzog H,Cox HM

更新日期：2003-06-01 00:00:00

abstract：:1 Vasoactive intestinal polypeptide (VIP, 0.01- MicroM) produced dose-related relaxations of the mouse anococcygeus muscle. 2 Following incubation with indomethacin (2.8 microM 1 h) adenosine 5'-triphosphate (ATP, 0.5-10 mM) produced dose-related relaxations of the mouse anococcygeus. 3 Haemolysed blood reduced inhibi...

journal_title：British journal of pharmacology

authors： Gibson A,Tucker JF

更新日期：1982-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Rho kinase (ROCK) activation is involved in neuroinflammatory processes leading to progression of neurodegenerative diseases such as Parkinson's disease. Furthermore, ROCK plays a major role in angiogenesis. Neuroinflammation and angiogenesis are mechanisms involved in developing l-DOPA-induced d...

journal_title：British journal of pharmacology

authors： Lopez-Lopez A,Labandeira CM,Labandeira-Garcia JL,Muñoz A

更新日期：2020-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Melanin-concentrating hormone receptor 1 (MCH1 receptor) antagonists are being considered as anti-obesity agents. The present study reports a new class of MCH1 receptor antagonists with an 8-methylquinoline scaffold. The molecular mechanism of MCH1 receptor blockade by these antagonists was exami...

journal_title：British journal of pharmacology

authors： Sakurai T,Ogawa K,Ishihara Y,Kasai S,Nakayama M

更新日期：2014-03-01 00:00:00

abstract：:1. Human mast cell tryptase appears to display considerable variation in activating proteinase-activated receptor 2 (PAR(2)). We found tryptase to be an inefficient activator of wild-type rat-PAR(2) (wt-rPAR(2)) and therefore decided to explore the factors that may influence tryptase activation of PAR(2). 2. Using a 2...

journal_title：British journal of pharmacology

authors： Compton SJ,Renaux B,Wijesuriya SJ,Hollenberg MD

更新日期：2001-10-01 00:00:00

abstract：:The alpha2-adrenoceptor function in mesenteric arteries of spontaneously hypertensive rats (SHR) was investigated by comparing membrane potential changes in response to adrenergic agonists in preparations from female SHR, Wistar-Kyoto (WKY) and normotensive Wistar rats (NWR). Resting membrane potential was found to be...

journal_title：British journal of pharmacology

authors： Feres T,Borges AC,Silva EG,Paiva AC,Paiva TB

更新日期：1998-11-01 00:00:00

abstract：:1. Sabcomeline (SB-202026, 0.03 mg kg(-1), p.o.), a potent and functionally selective M1 receptor partial agonist, caused a statistically significant improvement in the performance of a visual object discrimination task by marmosets. No such improvement was seen after RS86 (0.1 mg kg(-1), p.o.). 2. Initial learning, w...

journal_title：British journal of pharmacology

authors： Harries MH,Samson NA,Cilia J,Hunter AJ

更新日期：1998-05-01 00:00:00

abstract：:Cholesterol and oxysterol sulfates are important regulators of lipid metabolism, inflammation, cell apoptosis, and cell survival. Among the sulfate-based lipids, cholesterol sulfate (CS) is the most studied lipid both quantitatively and functionally. Despite the importance, very few studies have analysed and linked th...

journal_title：British journal of pharmacology

authors： Sanchez LD,Pontini L,Marinozzi M,Sanchez-Aranguren LC,Reis A,Dias IHK

更新日期：2020-08-06 00:00:00

abstract：:1. We have investigated the cellular target of K(+) channel blockers responsible for the inhibition of the EDHF-mediated relaxation in the rat mesenteric artery by studying their effects on tension, smooth muscle cell (SMC) membrane potential and endothelial cell Ca(2+) signal ([Ca(2+)](endo)). 2. In arteries contract...

journal_title：British journal of pharmacology

authors： Ghisdal P,Morel N

更新日期：2001-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Sublesional osteoporosis predisposes individuals with spinal cord injury (SCI) to an increased risk of low-trauma fracture. The aim of the present work was to investigate the effect of treatment with resveratrol (RES) on sublesional bone loss in spinal cord-injured rats. EXPERIMENTAL APPROACH:Co...

journal_title：British journal of pharmacology

authors： Wang HD,Shi YM,Li L,Guo JD,Zhang YP,Hou SX

更新日期：2013-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Heat-sensitive transient receptor potential vanilloid (TRPV) channels are expressed in various epithelial tissues regulating, among else, barrier functions. Their expression is well established in the distal nephron; however, we have no data about their presence in podocytes. As podocytes are ind...

journal_title：British journal of pharmacology

authors： Ambrus L,Kelemen B,Szabó T,Bíró T,Tóth BI

更新日期：2017-12-01 00:00:00

abstract：:1. We studied the effect of bradykinin on plasma exudation in the airways of the anaesthetized guinea-pig in vivo. Tissue content of extravasated Evans blue dye was used as an index of protein exudation in the larynx, trachea, main bronchi and intrapulmonary airways (i.p.a.). 2. Bradykinin increased the content of Eva...

journal_title：British journal of pharmacology

authors： Rogers DF,Dijk S,Barnes PJ

更新日期：1990-11-01 00:00:00

abstract：:1. Modulations of Cl- responses to glycine by 5-hydroxytryptamine ligands were studied in cultured spinal neurones, by the whole-cell recording technique. 2. Three 5-HT3 antagonists were found to potentiate reversibly responses to low concentrations of glycine. Potentiations were induced by micromolar concentrations o...

journal_title：British journal of pharmacology

authors： Chesnoy-Marchais D

更新日期：1996-08-01 00:00:00

abstract：:1. Electrically-evoked contractions in different regions of the rabbit isolated pulmonary artery have been investigated using stimulation parameters generally assumed to stimulate nerves selectively. 2. In extrapulmonary artery, trains of stimuli (10 Hz; pulse width 0.1 ms) evoked monophasic contractions. In contrast,...

journal_title：British journal of pharmacology

authors： Jackson VM,Trout SJ,Cunnane TC

更新日期：2002-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:In mammalian cells, the anti-parasitic drug ivermectin is known as a positive allosteric modulator of the ATP-activated ion channel P2X4 and is used to discriminate between P2X4- and P2X7-mediated cellular responses. In this paper we provide evidence that the reported isoform selectivity of iverm...

journal_title：British journal of pharmacology

authors： Nörenberg W,Sobottka H,Hempel C,Plötz T,Fischer W,Schmalzing G,Schaefer M

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhibitors of histone deacetylase (HDAC) are emerging as a promising class of anti-cancer drugs, but a generic deregulation of transcription in neoplastic cells cannot fully explain their therapeutic effects. In this study we evaluated alternative molecular mechanisms by which HDAC inhibitors cou...

journal_title：British journal of pharmacology

authors： Condorelli F,Gnemmi I,Vallario A,Genazzani AA,Canonico PL

更新日期：2008-02-01 00:00:00

abstract：:1. The aim of this study was to investigate the relationship between airway reactivity, leukocyte influx and nitric oxide (NO), in conscious guinea-pigs after aerosolized lipopolysaccharide (LPS) exposure. 2. Inhaled histamine (1 mM, 20 s), causing no bronchoconstriction before LPS exposure (30 microg ml(-1), 1 h), ca...

journal_title：British journal of pharmacology

authors： Toward TJ,Broadley KJ

更新日期：2000-09-01 00:00:00

abstract：:1. Acetylcholine (ACh)-induced relaxation of aortic strips with endothelium and production of cyclic GMP between streptozotocin-induced diabetic and age-matched control rats were compared. 2. The concentration-response curve for ACh-induced relaxation was shifted to the right in diabetic rats. IC50 values for ACh were...

journal_title：British journal of pharmacology

authors： Kamata K,Miyata N,Kasuya Y

更新日期：1989-06-01 00:00:00

abstract：:1. The effect of mastoparan on phosphatidylcholine hydrolysis was examined in 1321N1 human astrocytoma cells. Mastoparan (3-30 microM) caused an accumulation of diacylglycerol (DG) and phosphatidic acd (PA) accompanied by choline release in a concentration- and time-dependent manner. 2. In the presence of 2% n-butanol...

journal_title：British journal of pharmacology

authors： Mizuno K,Nakahata N,Ohizumi Y

更新日期：1995-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Aucubin, the predominant component of Eucommia ulmoides Oliv., has been shown to have profound effects on oxidative stress. As oxidative stress has previously been demonstrated to contribute to acute and chronic myocardial injury, we tested the effects of aucubin on cardiac remodelling and heart ...

journal_title：British journal of pharmacology

authors： Wu QQ,Xiao Y,Duan MX,Yuan Y,Jiang XH,Yang Z,Liao HH,Deng W,Tang QZ

更新日期：2018-05-01 00:00:00

abstract：:1. 8-Hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), gepirone, buspirone and ipsapirone dose-dependently antagonized the head-shakes induced by 1-(2,5-dimethoxy 4-iodophenyl)-2-amino propane hydrochloride (DOI) (1.0 mg kg-1) in mice, when these agents were given i.p. 10 min beforehand. 2. para-Chlorophenylalanine (...

journal_title：British journal of pharmacology

authors： Dursun SM,Handley SL

更新日期：1993-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The passage of drugs across the blood-brain barrier (BBB) limits the efficacy of chemotherapy in brain tumours. For instance, the anticancer drug doxorubicin, which is effective against glioblastoma in vitro, has poor efficacy in vivo, because it is extruded by P-glycoprotein (Pgp/ABCB1), multidr...

journal_title：British journal of pharmacology

authors： Pinzón-Daza M,Garzón R,Couraud P,Romero Ia,Weksler B,Ghigo D,Bosia A,Riganti C

更新日期：2012-12-01 00:00:00

abstract：:BACKGROUND AND PURPOSE The Ca(2+) paradox is an important phenomenon associated with Ca(2+) overload-mediated cellular injury in myocardium. The present study was undertaken to elucidate molecular and cellular mechanisms for the development of the Ca(2+) paradox. EXPERIMENTAL APPROACH Fluorescence imaging was performe...

journal_title：British journal of pharmacology

authors： Kojima A,Kitagawa H,Omatsu-Kanbe M,Matsuura H,Nosaka S

更新日期：2010-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:2-Hydroxypropyl-β-cyclodextrin (HPCD) is an FDA approved vehicle for drug delivery and an efficient cholesterol-lowering agent. HPCD was proposed to lower tissue cholesterol via multiple mechanisms including those mediated by oxysterols. CYP27A1 and CYP46A1 are the major oxysterol-producing enzym...

journal_title：British journal of pharmacology

authors： El-Darzi N,Mast N,Petrov AM,Pikuleva IA

更新日期：2020-07-22 00:00:00

abstract：:The molecular mechanisms involved in veratridine-induced chromaffin cell death have been explored. We have found that exposure to veratridine (30 microM, 1 h) produces a delayed cellular death that reaches 55% of the cells 24 h after veratridine exposure. This death has the features of apoptosis as DNA fragmentation c...

journal_title：British journal of pharmacology

authors： Jordán J,Galindo MF,Calvo S,González-García C,Ceña V

更新日期：2000-08-01 00:00:00

abstract：:1. Whole-cell patch-clamp recordings were made from smooth muscle cells isolated from the longitudinal muscle layer of guinea-pig ileum. Carbachol (acting at muscarinic receptors) or histamine (acting at H1 histamine receptors) suppressed Ca2+ channel current. The effect of either agonist had an initial transient comp...

journal_title：British journal of pharmacology

authors： Unno T,Beech DJ,Komori S,Ohashi H

更新日期：1998-10-01 00:00:00

abstract：:1. The effects of ryanodine on changes in cytoplasmic Ca2+ level ([Ca2+]i) and muscle tension induced by maximum concentrations of phenylephrine (Phe; 1 microM), prostaglandin F2 alpha (PGF2 alpha, 10 microM), caffeine (Caf, 30 mM) and isoprenaline (Iso, 1 microM) were examined in rat aortic strips using fura-2. 2. In...

journal_title：British journal of pharmacology

authors： Hisayama T,Takayanagi I,Okamoto Y

更新日期：1990-08-01 00:00:00

abstract：:(1) Rapid desensitization of ligand-gated ion channel receptors can alter the apparent activity of receptor modulators, as well as make detection of fast-channel activation difficult. Investigation of the antagonist pharmacology of ATP-sensitive homomeric P2X3 receptors is limited by agonist-evoked fast-desensitizatio...

journal_title：British journal of pharmacology

authors： Neelands TR,Burgard EC,Uchic ME,McDonald HA,Niforatos W,Faltynek CR,Lynch KJ,Jarvis MF

更新日期：2003-09-01 00:00:00