Localization of the central cardiovascular action of clonidine.

abstract：:1 The synthesis of several butyrophenone analogues of haloperidol is described. 2 The effects of these compounds on alpha-adrenoceptors were evaluated by examining their ability to reduce alpha 1-stimulated K+ release from rat parotid slices and to displace [3H]-phentolamine from human platelet membrane alpha 2-adreno...

journal_title：British journal of pharmacology

authors： Atlas D,Friedman Z,Litvin Y,Steer ML

更新日期：1982-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:AZ11645373 and N-{2-methyl-5-[(1R, 5S)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-ylcarbonyl]phenyl}-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide hydrochloride (compound-22) are recently described P2X(7) receptor antagonists. In this study we have further characterized these compounds to determine their mecha...

journal_title：British journal of pharmacology

authors： Michel AD,Ng SW,Roman S,Clay WC,Dean DK,Walter DS

更新日期：2009-04-01 00:00:00

abstract：:1. Optimal dipeptide and peptidomimetic drug transport across the intestinal mucosal surface is dependent upon the co-operative functional activity of the di/tripeptide transporter hPepT1 and the Na(+)/H(+) exchanger NHE3. The ability of the anti-absorptive enteric neuropeptide VIP (vasoactive intestinal peptide) to m...

journal_title：British journal of pharmacology

authors： Anderson CM,Mendoza ME,Kennedy DJ,Raldua D,Thwaites DT

更新日期：2003-02-01 00:00:00

abstract：:1. We have investigated the effects of chlorpheniramine, atropine and capsaicin pretreatment on inhaled sodium metabisulphite (MBS)-induced airway microvascular leakage and bronchoconstriction in anaesthetized guinea-pigs in order to clarify the mechanisms involved in these responses. The effects of frusemide and nedo...

journal_title：British journal of pharmacology

authors： Sakamoto T,Elwood W,Barnes PJ,Chung KF

更新日期：1992-10-01 00:00:00

abstract：:BACKGROUND AND PURPOSE The transepithelial absorption of Na(+) in the lungs is crucial for the maintenance of the volume and composition of epithelial lining fluid. The regulation of Na(+) transport is essential, because hypo- or hyperabsorption of Na(+) is associated with lung diseases such as pulmonary oedema or cys...

journal_title：British journal of pharmacology

authors： Althaus M,Urness KD,Clauss WG,Baines DL,Fronius M

更新日期：2012-07-01 00:00:00

abstract：:Idiopathic pulmonary fibrosis (IPF) is a fatal lung disease where the additional presence of pulmonary hypertension (PH) reduces survival. In particular, the presence of coexistent pulmonary vascular disease in patients with advanced lung parenchymal disease results in worse outcomes than either diagnosis alone. This ...

journal_title：British journal of pharmacology

authors： Rajagopal K,Bryant AJ,Sahay S,Wareing N,Zhou Y,Pandit LM,Karmouty-Quintana H

更新日期：2021-01-01 00:00:00

abstract：:1 Both phasic and tonic responses to KCl 160 mM were reduced by Ca2+ deprivation. After 90 min, the phasic response was abolished but 13 +/- 1.5% of the tonic response remained. This resistant component was still present if the Ca2+-free solution contained EGTA 0.1 mM. The tonic response was more resistant to deprivat...

journal_title：British journal of pharmacology

authors： Hay DW,Wadsworth RM

更新日期：1982-05-01 00:00:00

abstract：:By examination of compound action potentials in the saphenous nerve of the anaesthetized rat it has been shown that capsaicin causes a rapid, dose-dependent, failure of conduction in many C-fibres when applied directly to the nerve. A large reduction in C-fibre conduction occurs with concentrations as low as 110 micro...

journal_title：British journal of pharmacology

authors： Baranowski R,Lynn B,Pini A

更新日期：1986-10-01 00:00:00

abstract：:The effects of 15-hydroperoxy metabolites of arachidonic acid on vascular tone were evaluated in the perfused mesenteric preparation, the isolated perfused lung and segments of pulmonary arteries of the rat. In the mesenteric preparation, precontracted with phenylephrine, both 15-hydroperoxy-5,8,11,13-eicosatetraenoic...

journal_title：British journal of pharmacology

authors： d'Alarcao M,Corey EJ,Cunard C,Ramwell P,Uotila P,Vargas R,Wroblewska B

更新日期：1987-07-01 00:00:00

abstract：:The effect of propranolol, a beta-adrenoceptor blocking agent, has been investigated on gastric acid secretion in pylorus and cardiac-ligated rats. Compared to the control group, propranolol significantly diminished the gastric acid secretion, and inhibited the formation of gastric ulceration. ...

journal_title：British journal of pharmacology

authors： Danhof IE,Geumei A

更新日期：1972-09-01 00:00:00

abstract：:1. Simultaneous computer modelling of control and guanfacine-masked [3H]-MK 912 saturation curves as well as guanfacine competition curves revealed that the drugs bound to two alpha 2-adrenoceptor subtypes in the rat cerebral cortex with very different selectivities. These alpha 2-adrenoceptor subtypes were designated...

journal_title：British journal of pharmacology

authors： Uhlén S,Xia Y,Chhajlani V,Felder CC,Wikberg JE

更新日期：1992-08-01 00:00:00

abstract：:1. We examined the gastric mucosal blood flow (GMBF) and ulcerogenic responses following barrier disruption induced by sodium taurocholate (TC) in diabetic rats and investigated the role of capsaicin-sensitive sensory neurons in these responses. 2. Animals were injected streptozotocin (STZ: 70 mg kg(-1), i.p.) and use...

journal_title：British journal of pharmacology

authors： Tashima K,Korolkiewicz R,Kubomi M,Takeuchi K

更新日期：1998-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We previously reported that NCX 2057, a compound comprising a nitric oxide (NO)-releasing moiety and the natural antioxidant, ferulic acid (FA), inhibits pro-inflammatory mediators through NO-mediated gene regulation. Here, we have assessed the activities of NCX 2057 in models of inflammatory and...

journal_title：British journal of pharmacology

authors： Ronchetti D,Borghi V,Gaitan G,Herrero JF,Impagnatiello F

更新日期：2009-09-01 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：:This paper is intended to assist pharmacologists to make the most of statistical analysis and avoid common errors. A scenario, in which an experimenter performed an experiment in two separate stages, combined the control groups for analysis and found some surprising results, is presented. The consequences of combined ...

journal_title：British journal of pharmacology

authors： Lew MJ

更新日期：2008-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Alcohol exposure in utero may lead to a wide range of long-lasting morphological and behavioural deficiencies known as fetal alcohol spectrum disorders (FASD), associated with a higher risk of later developing neuropsychiatric disorders. However, little is known about the long-term consequences o...

journal_title：British journal of pharmacology

authors： Cantacorps L,Montagud-Romero S,Luján MÁ,Valverde O

更新日期：2020-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Small molecule glucokinase activators (GKAs) have been associated with potent antidiabetic efficacy and hepatic steatosis in rodents. This study reports the discovery of S 50131 and S 51434, two novel GKAs with an original scaffold and an atypical pharmacological profile. EXPERIMENTAL APPROACH:A...

journal_title：British journal of pharmacology

authors： De Ceuninck F,Kargar C,Charton Y,Goldstein S,Perron-Sierra F,Ilic C,Caliez A,Rolin JO,Sadlo M,Harley E,Vinson C,Ktorza A

更新日期：2013-07-01 00:00:00

abstract：:1. This study describes the effects of hypoxia on relaxing responses and cAMP production induced by the known vasodilator peptides: alphaCGRP, amylin (AMY) and adrenomedullin (AM) on isolated pig coronary arteries in vitro. 2. Hypoxic incubation increased the vasorelaxant effect of alphaCGRP (four-fold; P<0.05), AMY (...

journal_title：British journal of pharmacology

authors： Hasbak P,Eskesen K,Schifter S,Edvinsson L

更新日期：2005-07-01 00:00:00

abstract：:1. An investigation into the effects of cholecystokinin octapeptide (CCK-8S) and its pentapeptide analogue, pentagastrin, on neurones located in ventromedial nuclei of rat hypothalamic slices maintained in vitro has been undertaken. 2. CCK-8S (0.01-1.0 microM) applied in the perfusion medium produced a concentration-d...

journal_title：British journal of pharmacology

authors： Boden P,Hill RG

更新日期：1988-05-01 00:00:00

abstract：BACKGROUND & PURPOSE:The therapeutically available quinolone antibiotic moxifloxacin has been used as a positive control for prolonging the QT interval in both clinical and non-clinical studies designed to assess the potential of new drugs to delay cardiac repolarization. Despite moxifloxacin prolonging QT, it has not ...

journal_title：British journal of pharmacology

authors： Thomsen MB,Beekman JD,Attevelt NJ,Takahara A,Sugiyama A,Chiba K,Vos MA

更新日期：2006-12-01 00:00:00

abstract：:1. We studied the ability of nitric oxide (NO) to physiologically antagonize endothelin-1 (ET-1) induced constrictions in human internal mammary artery (IMA). We also investigated the hypothesis that NO interacts directly with ET-receptor binding in human heart and aorta. 2. ET-1 potently contracted IMA (EC(50) 6.86 n...

journal_title：British journal of pharmacology

authors： Wiley KE,Davenport AP

更新日期：2001-01-01 00:00:00

abstract：:1. The effects of long-term treatment with trandolapril, an angiotensin I-converting enzyme inhibitor, on exercise capacity of rats with chronic heart failure (CHF) following coronary artery ligation were examined. CHF was developed by 8 weeks after the coronary artery ligation. 2. The running time of rats with CHF in...

journal_title：British journal of pharmacology

authors： Yamaguchi F,Kawana K,Tanonaka K,Kamano I,Igarashi T,Gen E,Fujimoto Y,Maki T,Sanbe A,Nasa Y,Takeo S

更新日期：1999-04-01 00:00:00

abstract：:1. The ability of the nitric oxide (NO)-releasing aspirin, NCX 4016, to control vasoconstrictor responses induced by electrical field stimulation (TNS) or by exogenous norepinephrine (NE) was investigated in perfused rat tail artery with intact endothelium. 2. NCX 4016 (25, 50 and 100 microM) dose-dependently antagoni...

journal_title：British journal of pharmacology

authors： Rossoni G,Manfredi B,Del Soldato P,Berti F

更新日期：2002-09-01 00:00:00

abstract：:Ouabain was administered at a loading dose of 3 mug/kg followed by an infusion at a rate of 1 mug/kg-1 min-1 in order to produce severe dysrhythmia in dogs within 60 minutes. Similarly, digitoxin at a loading dose of 9 mug/kg followed by an infusion at a rate of 3 mug kg-1 min-1 was administered to compare its effect ...

journal_title：British journal of pharmacology

authors： Dutta S,Marks BH,Schoener EP

更新日期：1977-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Preclinical cardiovascular safety studies (CVS) have been compared between facilities with respect to their sensitivity to detect drug-induced QTc prolongation (ΔQTc). Little is known about the consistency of quantitative ΔQTc predictions that are relevant for translation to humans. EXPERIMENTAL...

journal_title：British journal of pharmacology

authors： Gotta V,Cools F,van Ammel K,Gallacher DJ,Visser SA,Sannajust F,Morissette P,Danhof M,van der Graaf PH

更新日期：2015-09-01 00:00:00

abstract：:1. Systemic infusion of neuropeptide Y (NPY) reduces renal blood flow and can concomitantly increase diuresis, natriuresis and calciuresis in anaesthetized rats. The present study was designed to investigate whether the apparently contradictory NPY effects on renal blood flow and urine formation and composition are me...

journal_title：British journal of pharmacology

authors： Bischoff A,Avramidis P,Erdbrügger W,Münter K,Michel MC

更新日期：1997-04-01 00:00:00

abstract：:1. Intracellular recordings were made from neurones in vitro in the rat substantia nigra zona compacta and ventral tegmental area; the neurones had the characteristic properties of dopamine-containing cells, and fired action potentials spontaneously. 2. Cocaine (1-10 microM) inhibited spontaneous firing, hyperpolarize...

journal_title：British journal of pharmacology

authors： Lacey MG,Mercuri NB,North RA

更新日期：1990-04-01 00:00:00

abstract：:1. Intrathecal (i.t.) administration of nociceptin and high doses of morphine induced allodynia in response to innocuous tactile stimuli, and i.t. nociceptin evoked hyperalgesia in response to noxious thermal stimuli in conscious mice. Here we have characterized the nociceptin-induced allodynia and compared it with th...

journal_title：British journal of pharmacology

authors： Hara N,Minami T,Okuda-Ashitaka E,Sugimoto T,Sakai M,Onaka M,Mori H,Imanishi T,Shingu K,Ito S

更新日期：1997-06-01 00:00:00

abstract：:1 The metabolism of extracellular nucleotides plays an important role in nucleotide signalling mediated by P2 receptors. The nucleotide sequence encoding a putative human ecto-ATPase named CD39L1 was reported recently. However, the biological activity of this protein has not been established. 2 Based on the sequence o...

journal_title：British journal of pharmacology

authors： Mateo J,Harden TK,Boyer JL

更新日期：1999-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is increasing evidence that not only the monoaminergic but also the glutamatergic system is involved in the pathophysiology of attention-deficit hyperactivity disorder (ADHD). Hyperactivity of glutamate metabolism might be causally related to a hypoactive state in the dopaminergic system. A...

journal_title：British journal of pharmacology

authors： Ludolph AG,Udvardi PT,Schaz U,Henes C,Adolph O,Weigt HU,Fegert JM,Boeckers TM,Föhr KJ

更新日期：2010-05-01 00:00:00