The action of glucosulphone [N,N'-di (glucose sodium sulphonate) of 4,4'-diaminodiphenyl sulphone] on pancreatic kallikrein.

abstract：:1. Measurements were made of the uptake, metabolism and release of [(3)H]-adrenaline by human platelets in citrated plasma or in an artificial medium.2. Radioactive adrenaline was not taken up at 0-2 degrees C. At 37 degrees C there was a slow uptake which continued for at least 5 hours.3. About half of the radioactiv...

journal_title：British journal of pharmacology

authors： Born GV,Smith JB

更新日期：1970-08-01 00:00:00

abstract：:1. To see if arachidonic acid (AA) plays a role in the sustained suppression of voltage-gated calcium channel currents produced by muscarinic receptor stimulation by carbachol (CCh), the effects of AA on membrane currents were examined in whole-cell voltage-clamped smooth muscle cells of the guinea-pig ileum. 2. In ce...

journal_title：British journal of pharmacology

authors： Unno T,Komori S,Ohashi H

更新日期：1996-09-01 00:00:00

abstract：:BACKGROUND AND PURPOSE Selective hyperpolarization activated, cyclic nucleotide-gated channel (HCN) blockers represent an important therapeutic goal due to the wide distribution and multiple functions of these proteins, representing the molecular correlate of f- and h-current (I(f) or I(h) ). Recently, new compounds ...

journal_title：British journal of pharmacology

authors： Del Lungo M,Melchiorre M,Guandalini L,Sartiani L,Mugelli A,Koncz I,Szel T,Varro A,Romanelli MN,Cerbai E

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Cannabidiol has been reported to act as an antagonist at cannabinoid CB1 receptors. We hypothesized that cannabidiol would inhibit cannabinoid agonist activity through negative allosteric modulation of CB1 receptors. EXPERIMENTAL APPROACH:Internalization of CB1 receptors, arrestin2 recruitment, ...

journal_title：British journal of pharmacology

authors： Laprairie RB,Bagher AM,Kelly ME,Denovan-Wright EM

更新日期：2015-10-01 00:00:00

abstract：:1. Functional GABA-gated chloride channels are formed when cRNA encoding the Drosophila melanogaster GABA receptor subunit RDL is injected into the cytoplasm of Xenopus oocytes. Two-electrode voltage-clamp was used to investigate allosteric modulation of GABA-induced currents recorded from the expressed, bicuculline-i...

journal_title：British journal of pharmacology

authors： Hosie AM,Sattelle DB

更新日期：1996-03-01 00:00:00

abstract：:1. The chemically novel acetohydroxamic acids, BW A4C, BW A137C and BW A797C, are potent inhibitors of the synthesis of leukotriene B4 (LTB4) from arachidonic acid by human leucocyte homogenates: the concentrations required for 50% inhibition (IC50) were 0.1 microM, 0.8 microM and 0.5 microM respectively. Inhibition w...

journal_title：British journal of pharmacology

authors： Tateson JE,Randall RW,Reynolds CH,Jackson WP,Bhattacherjee P,Salmon JA,Garland LG

更新日期：1988-06-01 00:00:00

abstract：:1. Alprenolol, a beta-adrenoceptor blocking drug reported to have the same potency as propranolol in vitro and in vivo, was found to be four times more active than procaine as a local anaesthetic on frog sciatic nerve.2. At doses of 0.125 mg/kg and above alprenolol protected anaesthetized guinea-pigs against ouabain-i...

journal_title：British journal of pharmacology

authors： Singh BN,Williams EM

更新日期：1970-04-01 00:00:00

abstract：:1. In this study, we investigated the effects of different drugs (a kappa-opioid receptor agonist U-50,488, a vasopressin receptor antagonist dPTyr(Me)AVP or an N-methyl-D-aspartate (NMDA) receptor antagonist MK-801) on the development of morphine tolerance in rat hippocampal slices. 2. Hippocampal slices (450 microm)...

journal_title：British journal of pharmacology

authors： Su MT,Lin WB,Lue WM,Cheng CY,Tao PL

更新日期：1998-02-01 00:00:00

abstract：:1. Histamine and carbachol produced concentration-related increases in the accumulation of 3H-inositol phosphates in slices of bovine tracheal smooth muscle. 2. Noradrenaline alone produced a small stimulation of 3H-inositol phosphate accumulation which was inhibited by the alpha-adrenoceptor antagonist phentolamine. ...

journal_title：British journal of pharmacology

authors： Hall IP,Hill SJ

更新日期：1988-12-01 00:00:00

abstract：:1. gamma-Aminobutyric acid (GABA) was applied by the 'concentration clamp' technique to isolated neurones of Aplysia. GABA induced a chloride current (ICl) due to activation of a single class of chloride-channel. 2. The concentration-response curve for the peak ICl gave an apparent dissociation constant of 6.4 X 10(-5...

journal_title：British journal of pharmacology

authors： Ikemoto Y,Akaike N,Kijima H

更新日期：1988-11-01 00:00:00

abstract：:Prostate cancer is the second most common malignancy in men and androgen deprivation therapy is the first-line therapy. However, most cases will eventually develop castration-resistant prostate cancer after androgen deprivation therapy treatment. Enzalutamide is a second-generation androgen receptor antagonist approve...

journal_title：British journal of pharmacology

authors： Wang Y,Chen J,Wu Z,Ding W,Gao S,Gao Y,Xu C

更新日期：2020-11-05 00:00:00

abstract：:1 Human luteal tissue slices from days 18, 21 and 25 of the menstrual cycle were superfused in vitro with Medium 199 alone or containing cloprostenol (1 microgram/ml). Concentrations of progesterone, oestradiol-17beta and prostaglandins F2alpha and E2 were determined in the superfusate samples. 2 Secretion of steroids...

journal_title：British journal of pharmacology

authors： McDougall AN,Walker FM,Watson J

更新日期：1977-07-01 00:00:00

abstract：:Recent advances have improved our understanding of the renin-angiotensin system (RAS). These have included the recognition that angiotensin (Ang)-(1-7) is a biologically active product of the RAS cascade. The identification of the ACE homologue ACE2, which forms Ang-(1-7) from Ang II, and the GPCR Mas as an Ang-(1-7) ...

journal_title：British journal of pharmacology

authors： Simões e Silva AC,Silveira KD,Ferreira AJ,Teixeira MM

更新日期：2013-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:GABAA receptors mediate neuronal inhibition in the brain. They are the primary targets for benzodiazepines, which are widely used to treat neurological disorders including anxiety, epilepsy and insomnia. The mechanism by which benzodiazepines enhance GABAA receptor activity has been extensively s...

journal_title：British journal of pharmacology

authors： Dixon CL,Harrison NL,Lynch JW,Keramidas A

更新日期：2015-07-01 00:00:00

abstract：:1. The affinity of the alpha 1-adrenoceptor antagonist SB 216469 (also known as REC 15/2739) has been determined at native and cloned alpha 1-adrenoceptor subtypes by radioligand binding and at functional alpha 1-adrenoceptor subtypes in isolated tissues. 2. In radioligand binding studies with [3H]-prazosin, SB 216469...

journal_title：British journal of pharmacology

authors： Chess-Williams R,Chapple CR,Verfurth F,Noble AJ,Couldwell CJ,Michel MC

更新日期：1996-11-01 00:00:00

abstract：:Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonar...

journal_title：British journal of pharmacology

authors： Marsango S,Barki N,Jenkins L,Tobin AB,Milligan G

更新日期：2020-09-01 00:00:00

abstract：:1. The effects of inhibiting endogenous Cu/Zn superoxide dismutase (SOD) with diethyldithiocarbamate (DETCA) were examined on the ability of hydroquinone, hydroxocobalamin and carboxy-PTIO to block nitrergic relaxation in the bovine retractor penis (BRP) muscle. 2. Incubation of strips of BRP with DETCA (3 mM) for 2 h...

journal_title：British journal of pharmacology

authors： Paisley K,Martin W

更新日期：1996-04-01 00:00:00

abstract：:1. The effect of bradykinin on the Na+-K+ pump of airway smooth muscle was investigated by measuring ouabain-sensitive (86)Rb(+) uptake in cultured guinea-pig tracheal smooth muscle cells. 2. Bradykinin induced a concentration-dependent increase in ouabain-sensitive (86)Rb(+) uptake, with an EC(50) of 3 nM (pD(2) = 8....

journal_title：British journal of pharmacology

authors： Dodson AM,Rhoden KJ

更新日期：2001-08-01 00:00:00

abstract：:1. Taxanes are antineoplastic drugs which have cardiovascular side effects of unknown mechanism. We investigated their influence on blood viscosity and erythrocyte morphology. 2. Whole blood was incubated in vitro with increasing concentrations of Taxol, Taxotere, paclitaxel (0-100 microM) and the vehicles Cremophor-E...

journal_title：British journal of pharmacology

authors： Mark M,Walter R,Meredith DO,Reinhart WH

更新日期：2001-11-01 00:00:00

abstract：:1. The present study addressed the role of neuropeptide (NPY) Y2 receptors in neurogenic contraction of mesenteric resistance arteries from female spontaneously hypertensive rats (SHR). Arteries were suspended in microvascular myographs, electrical field stimulation (EFS) was performed, and protein evaluated by Wester...

journal_title：British journal of pharmacology

authors： Gradin KA,Buus CL,Li JY,Frøbert O,Simonsen U

更新日期：2006-07-01 00:00:00

abstract：:The effects of the angiotensin-converting-enzyme inhibitor (ACEI) ramiprilat, the angiotensin II type 1 receptor antagonist (AT(1)A) candesartan, and the combination of both drugs on infarct size (IS) resulting from regional myocardial ischaemia were studied in pigs. Both ACEI and AT(1)A reduce myocardial IS by a brad...

journal_title：British journal of pharmacology

authors： Weidenbach R,Schulz R,Gres P,Behrends M,Post H,Heusch G

更新日期：2000-09-01 00:00:00

abstract：:1. The purpose of this study was to develop and validate an integrated pharmacokinetic-pharmacodynamic model for the anti-lipolytic effects of the adenosine A1-receptor agonist N6-(p-sulphophenyl)adenosine (SPA). Tissue selectivity of SPA was investigated by quantification of haemodynamic and anti-lipolytic effects in...

journal_title：British journal of pharmacology

authors： van Schaick EA,de Greef HJ,Langemeijer MW,Sheehan MJ,IJzerman AP,Danhof M

更新日期：1997-10-01 00:00:00

abstract：:Peroxisome proliferator activated receptors (PPAR)s are nuclear transcription factors of the steroid receptor super-family. One member, PPARgamma, a critical transcription factor in adipogenesis, is expressed in ECV304 cells, and when activated participates in the induction of cell death by apoptosis. Here we describe...

journal_title：British journal of pharmacology

authors： Bishop-Bailey D,Hla T,Warner TD

更新日期：2000-10-01 00:00:00

abstract：:The human distal gut is home to a rich and dense microbial community with representatives of all three domains of life which are intricately connected with our physiology and health. The combined genomes of these microbes, collectively called the human microbiome, vastly expand the metabolic capacities of our own geno...

journal_title：British journal of pharmacology

authors： Bik EM,Ugalde JA,Cousins J,Goddard AD,Richman J,Apte ZS

更新日期：2018-12-01 00:00:00

abstract：:1 Palmitaldehyde, olealdehyde and linolealdehyde acetal phosphatidic acids induced rapid shape change and dose-dependent biphasic aggregation of human platelets in platelet-rich plasma; aggregation was reversible at low doses and irreversible at high doses of the acetal phosphatidic acids. The palmitaldehyde congener ...

journal_title：British journal of pharmacology

authors： Brammer JP,Maguire MH,Walaszek EJ,Wiley RA

更新日期：1983-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Nitric oxide (NO) is known to activate NO-sensitive guanylyl cyclase (NO-GC) and to elicit cGMP production. However, NO has also been proposed to induce cGMP-independent effects. It is accepted practice to use specific NO-GC inhibitors, such as ODQ or NS2028, to assess cGMP-dependent NO effects. ...

journal_title：British journal of pharmacology

authors： Lies B,Groneberg D,Gambaryan S,Friebe A

更新日期：2013-09-01 00:00:00

abstract：:Nicotine and dimethyl-phenylpiperazinium (DMPP) increased intravesicular pressure and then transiently depressed the spontaneous activity of the urinary bladder in chloralose anaesthetized cats. Adrenaline (5-10 micrograms kg-1), noradrenaline (5-20 micrograms kg-1) and isoprenaline (40-50 micrograms kg-1) which depre...

journal_title：British journal of pharmacology

authors： Koley B,Koley J,Saha JK

更新日期：1984-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Some neurosteroids, notably 3alpha-hydroxysteroids, positively modulate GABA(A) receptors, but sulphated steroids negatively modulate these receptors. Recently, other lipophilic amphiphiles have been suggested to positively modulate GABA receptors. We examined whether there was similarity among t...

journal_title：British journal of pharmacology

authors： Chisari M,Shu HJ,Taylor A,Steinbach JH,Zorumski CF,Mennerick S

更新日期：2010-05-01 00:00:00

abstract：:1. We studied the effect of intracellular angiotensin II (Ang II) and related peptides on rat aortic contraction, whether this effect is pharmacologically distinguishable from that induced by extracellular stimulation, and determined the Ca2+ source involved. 2. Compounds were delivered into the cytoplasm of de-endoth...

journal_title：British journal of pharmacology

authors： Brailoiu E,Filipeanu CM,Tica A,Toma CP,de Zeeuw D,Nelemans SA

更新日期：1999-03-01 00:00:00

abstract：:1. The rat isolated superior mesenteric bed, perfused with Krebs-Henseleit solution containing 10 microM indomethacin and precontracted with 100 microM methoxamine, was used to study the vasorelaxation produced by some fragments of endothelin-1, by two alanyl-substituted analogues, and by human and porcine proendothel...

journal_title：British journal of pharmacology

authors： Douglas SA,Hiley CR

更新日期：1991-10-01 00:00:00