A new method for estimating dissociation constants of competitive and non-competitive antagonists with no prior knowledge of agonist concentrations.

abstract：BACKGROUND AND PURPOSE:7-Ketocholesterol, an oxysterol present in atherosclerotic lesions, induces smooth muscle cell (SMC) death, thereby destabilizing plaques. Statins protect patients from myocardial infarction, though they induce SMC apoptosis. We investigated whether statins and 7-ketocholesterol exerted additive ...

journal_title：British journal of pharmacology

authors： Martinet W,Schrijvers DM,Timmermans JP,Bult H

更新日期：2008-07-01 00:00:00

abstract：:Muscularis mucosa of the distal oesophagus of the opossum contains nerves which release acetylcholine and substance P(SP)-like material on field stimulation. The release of SP-like material appeared to be inhibited by the presence of exogenous muscarinic agonists and potentiated by muscarinic antagonists. Analysis of ...

journal_title：British journal of pharmacology

authors： Daniel EE,Jury J,Robotham KH

更新日期：1986-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tumour cell migration and adhesion constitute essential features of metastasis. G-protein coupled receptor 55 (GPR55), a lysophospholipid receptor, has been shown to play an important role in carcinogenesis. Here, we investigated the involvement of GPR55 in migration and metastasis of colon cance...

journal_title：British journal of pharmacology

authors： Kargl J,Andersen L,Hasenöhrl C,Feuersinger D,Stančić A,Fauland A,Magnes C,El-Heliebi A,Lax S,Uranitsch S,Haybaeck J,Heinemann A,Schicho R

更新日期：2016-01-01 00:00:00

abstract：:(1) Increased oxidative stress plays a significant role in the etiology of cardiovascular disease. Lipid peroxidation, initiated in the presence of hydroxy radicals resulting in the production of malondialdehyde, directly produces oxidative stress. This study was designed to examine the direct impact of malondialdehyd...

journal_title：British journal of pharmacology

authors： Folden DV,Gupta A,Sharma AC,Li SY,Saari JT,Ren J

更新日期：2003-08-01 00:00:00

abstract：:1 The effect of clonidine on the 3H-purine release evoked by KCl or (-)-adrenaline was assessed in the superfused helical strip of the rabbit pulmonary artery pretreated with [3H]-adenosine. 2 Clonidine (3 x 10(-5) M to 10(-4) M) significantly enhanced the 3H-purine efflux evoked by 50 mM KCl but not by 3 x 10(-6) M) ...

journal_title：British journal of pharmacology

authors： Katsuragi T,Su C

更新日期：1981-11-01 00:00:00

abstract：:1. The administration of an analgesic dose (10 mg/kg, s.c.) of morphine increased the concentrations of the dopamine metabolites, 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in the brains of normal mice, and the time course of the change in the DOPAC concentration corresponded approximately to t...

journal_title：British journal of pharmacology

authors： Fukui K,Takagi H

更新日期：1972-01-01 00:00:00

abstract：:1 The influence of dopamine receptor agonists on gastric acid secretion stimulated by thyrotropin-releasing hormone (TRH) was studied in the perfused stomach of anaesthetized rats. 2 Intraventricular TRH produced a dose-dependent stimulation of basal gastric acid secretion. 3 Pretreatment with apomorphine, bromocripti...

journal_title：British journal of pharmacology

authors： Maeda-Hagiwara M,Watanabe K

更新日期：1983-05-01 00:00:00

abstract：:1. Incubation of bovine adrenal chromaffin cells with veratridine (10-100 microM) during 24 h, caused a concentration-dependent release of the cytosolic lactate dehydrogenase (LDH) into the bathing medium, an indicator of cell death. Lubeluzole or its R(-) enantiomer, R91154, did not enhance LDH release. Both lubeluzo...

journal_title：British journal of pharmacology

authors： Cano-Abad MF,López MG,Hernández-Guijo JM,Zapater P,Gandía L,Sánchez-García P,García AG

更新日期：1998-07-01 00:00:00

abstract：:1. Non-steroidal anti-inflammatory drugs (NSAIDs) are effective anti-inflammatory and analgesic drugs although they also induce unwanted side effects due to the inhibition of the physiological effects regulated by prostaglandins. This has led to the search for new compounds with fewer side effects, such as the nitro-N...

journal_title：British journal of pharmacology

authors： Romero-Sandoval EA,Mazario J,Howat D,Herrero JF

更新日期：2002-03-01 00:00:00

abstract：:1. The effects of 5-hydroxytryptamine (5-HT) uptake inhibitors, agonists and antagonists have been evaluated on mouse marble-burying behaviour, a putative test for anxiolytic agents. The high levels of locomotor activity occurring on first exposure to a circular runway (runway were used as a separate test of non-speci...

journal_title：British journal of pharmacology

authors： Njung'e K,Handley SL

更新日期：1991-09-01 00:00:00

abstract：:The neurotoxin MPP+ potently inhibited the striatal binding of [3H]-tyramine, a putative marker for the vesicular transporter of dopamine, and provoked a massive in vivo release of striatal dopamine. Tetrabenazine, an established ligand for the vesicular catecholamine carrier, potently inhibited [3H]-tyramine binding,...

journal_title：British journal of pharmacology

authors： Vaccari A,Del Zompo M,Melis F,Gessa GL,Rossetti ZL

更新日期：1991-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is growing evidence that inflammation plays a major role in the pathogenesis of neural damage caused by deposition of amyloid β (Aβ) in the brain. Nimodipine has received attention as a drug that might improve learning and reduce cognitive deficits in Alzheimer's disease, but the mechanism ...

journal_title：British journal of pharmacology

authors： Sanz JM,Chiozzi P,Colaianna M,Zotti M,Ferrari D,Trabace L,Zuliani G,Di Virgilio F

更新日期：2012-12-01 00:00:00

abstract：:1. Block by philanthotoxin-343 (PhTX-343), a neurotoxin from wasps, of ionic currents mediated through neuronal nicotinic acetylcholine (ACh) receptor/channels was characterized in rat phaeochromocytoma PC12 cells, by use of whole cell voltage-clamp techniques. 2. In the cells held at -60 mV, PhTX-343 at 0.1 and 1 mic...

journal_title：British journal of pharmacology

authors： Liu M,Nakazawa K,Inoue K,Ohno Y

更新日期：1997-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Picomolar concentrations of the beta3-adrenoceptor agonist BRL37344 stimulate 2-deoxyglucose uptake in soleus muscle via undefined receptors. Higher concentrations alter uptake, apparently via beta2-adrenoceptors. Effects of BRL37344 and beta2-adrenoceptor agonists are compared. EXPERIMENTAL APP...

journal_title：British journal of pharmacology

authors： Ngala RA,O'Dowd J,Wang SJ,Agarwal A,Stocker C,Cawthorne MA,Arch JR

更新日期：2008-10-01 00:00:00

abstract：:1. The vasodilator effects of arginine, nitric oxide (NO), acetylcholine (ACh) and sodium nitroprusside (NP) in the noradrenaline-preconstricted ('high tone') perfused rat kidney have been examined. 2. L-Arginine (0.6-23 mumol) caused a biphasic change in renal perfusion pressure. D-Arginine (0.6-23 mumol) was without...

journal_title：British journal of pharmacology

authors： Bhardwaj R,Moore PK

更新日期：1989-07-01 00:00:00

abstract：:1. The possibility that tachykinin NK1 receptors are involved in the plasma extravasation evoked by intradermal (i.d.) injection of Phoneutria nigriventer venom (PNV) in rat dorsal skin in vivo has been investigated. 2. Local oedema formation induced by the i.d. injection of test agents was measured by the extravascul...

journal_title：British journal of pharmacology

authors： Palframan RT,Costa SK,Wilsoncroft P,Antunes E,de Nucci G,Brain SD

更新日期：1996-05-01 00:00:00

abstract：:1 The effects of gamma-aminobutyric acid (GABA) and related substances were examined in guinea-pig ileum longitudinal muscle.2 GABA at doses ranging from 10(-7) M to 3 x 10(-6) M elicited a relaxation while at higher doses (3 x 10(-6) M - 10(-4) M), as previously described, it caused a contraction followed by relaxati...

journal_title：British journal of pharmacology

authors： Giotti A,Luzzi S,Spagnesi S,Zilletti L

更新日期：1983-03-01 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：:1. The action of adrenaline on the K(+) balance of the isolated heart was found to depend on the ionic composition and the temperature of the perfusion fluids used.2. When the perfusion fluid contained 145 mM Na(+), 1.7 mM Ca(++) and 3-9 mM K(+), adrenaline caused the hearts to gain K(+); when the K(+) concentration w...

journal_title：British journal of pharmacology

authors： Stafford A

更新日期：1969-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Skeletal muscle is the predominant site for glucose disposal and fatty acid consumption. Emerging evidence indicates that the crosstalk between adipose tissue and skeletal muscle is critical in maintaining insulin sensitivity and lipid homeostasis. The current study was designed to investigate wh...

journal_title：British journal of pharmacology

authors： Shen S,Liao Q,Zhang T,Pan R,Lin L

更新日期：2019-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Leucocyte infiltration is a rate-limiting step in the pathophysiology of acute pancreatitis (AP) although the adhesive mechanisms supporting leucocyte-endothelium interactions in the pancreas remain elusive. The aim of this study was to define the role of lymphocyte function antigen-1 (LFA-1) in ...

journal_title：British journal of pharmacology

authors： Awla D,Abdulla A,Zhang S,Roller J,Menger MD,Regnér S,Thorlacius H

更新日期：2011-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Venoms are a rich source of ligands for ion channels, but very little is known about their capacity to modulate G-protein coupled receptor (GPCR) activity. We developed a strategy to identify novel toxins targeting GPCRs. EXPERIMENTAL APPROACH:We studied the interactions of mamba venom fractions...

journal_title：British journal of pharmacology

authors： Quinton L,Girard E,Maiga A,Rekik M,Lluel P,Masuyer G,Larregola M,Marquer C,Ciolek J,Magnin T,Wagner R,Molgó J,Thai R,Fruchart-Gaillard C,Mourier G,Chamot-Rooke J,Ménez A,Palea S,Servent D,Gilles N

更新日期：2010-01-01 00:00:00

abstract：:1. This study examined beta-adrenoceptor signalling in cardiac tissues following infusion of isoprenaline (400 microg kg(-1) h(-1)) or vehicle to rats for 14 days. 2. Isoprenaline infusion caused marked hypertrophy of atria and ventricles and reduced the resting rate of spontaneously beating right atria and the basal ...

journal_title：British journal of pharmacology

authors： McMartin L,Summers RJ

更新日期：1999-06-01 00:00:00

abstract：:1. The effects of some rapidly metabolized sympathomimetic amines, such as beta-phenylethylamine and p-tyramine, in eliciting hypertensive responses to reserpine in the anaesthetized rat, have been studied.2. Retardation of metabolism, by pretreatment with the monoamineoxidase inhibitors iproniazid or phenelzine, caus...

journal_title：British journal of pharmacology

authors： Cashin CH

更新日期：1972-02-01 00:00:00

abstract：:1. In the presence of indomethacin (IM, 10 microM) and N omega-nitro-L- arginine (L-NOARG, 0.3 mM), acetylcholine (ACh) induces an endothelium-dependent smooth muscle hyperpolarization and relaxation in the rat isolated hepatic artery. The potassium (K) channel inhibitors, tetrabutylammonium (TBA, 1 mM) and to a lesse...

journal_title：British journal of pharmacology

authors： Zygmunt PM,Högestätt ED

更新日期：1996-04-01 00:00:00

abstract：:1. Chronic benzodiazepine administration has been associated with tolerance and with downregulation of gamma-aminobutyric acidA (GABAA)-receptor binding and function. However, effects of individual benzodiazepines on brain regions have varied. 2. To compare the effects of chronic lorazepam and alprazolam, we have admi...

journal_title：British journal of pharmacology

authors： Galpern WR,Miller LG,Greenblatt DJ,Shader RI

更新日期：1990-12-01 00:00:00

abstract：:We have demonstrated previously that infusion of angiotensin II (AngII) into hyperlipidemic mice augments atherosclerosis and results in the formation of abdominal aortic aneurysms (AAA). The purpose of this study was to determine the role of aldosterone in these AngII-induced vascular pathologies. Male apolipoprotein...

journal_title：British journal of pharmacology

authors： Cassis LA,Helton MJ,Howatt DA,King VL,Daugherty A

更新日期：2005-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Positive modulators of small conductance Ca(2+)-activated K(+) channels (SK1, SK2, and SK3) exert hyperpolarizing effects that influence the activity of excitable and non-excitable cells. The prototype compound 1-EBIO or the more potent compound NS309, do not distinguish between the SK subtypes a...

journal_title：British journal of pharmacology

authors： Hougaard C,Eriksen BL,Jørgensen S,Johansen TH,Dyhring T,Madsen LS,Strøbaek D,Christophersen P

更新日期：2007-07-01 00:00:00

abstract：:The protease inhibitor ritonavir is an integral part of current antiretroviral therapy targeting human immunodeficiency virus. Recent studies demonstrate that ritonavir induces apoptotic cell death with high efficiency in lymphoblastoid cell lines. Moreover, ritonavir can suppress activation of the transcription facto...

journal_title：British journal of pharmacology

authors： Mühl H,Paulukat J,Höfler S,Hellmuth M,Franzen R,Pfeilschifter J

更新日期：2004-12-01 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