Antiviral prodrugs - the development of successful prodrug strategies for antiviral chemotherapy.

abstract：:In CHO cells transfected with the rat dopamine D2 receptor (long isoform), administration of dopamine per se elicited a concentration-dependent increase in arachidonic acid (AA) release. The maximal effect was 197% of controls (EC50=25 nM). The partial D2 receptor agonist, (-)-(3-hydroxyphenyl)-N-n-propylpiperidine [(...

journal_title：British journal of pharmacology

authors： Nilsson CL,Hellstrand M,Ekman A,Eriksson E

更新日期：1998-08-01 00:00:00

abstract：:1. The role of alpha- and beta-adrenoceptor subtypes in the regulation of plasma glucose and immunoreactive insulin (IRI) levels has been investigated in normal conscious fasted rats by employing selective agonists and antagonists. 2. Adrenaline (0.2 mg kg-1)-induced hyperglycaemia was abolished by the selective alpha...

journal_title：British journal of pharmacology

authors： John GW,Doxey JC,Walter DS,Reid JL

更新日期：1990-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We previously demonstrated that paracetamol has to be metabolised in the brain by fatty acid amide hydrolase enzyme into AM404 (N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide) to activate CB1 receptors and TRPV1 channels, which mediate its analgesic effect. However, the brain mechanisms sup...

journal_title：British journal of pharmacology

authors： Barrière DA,Boumezbeur F,Dalmann R,Cadeddu R,Richard D,Pinguet J,Daulhac L,Sarret P,Whittingstall K,Keller M,Mériaux S,Eschalier A,Mallet C

更新日期：2020-04-01 00:00:00

abstract：:1. Endotoxin shock is accompanied by an increase in peripheral vascular permeability. It has been postulated that most biological activities of LPS are derived from lipid A moiety. Here we examined the effect of lipid A analogue ONO-4007 in increasing vascular permeability and the possible mediators in mouse skin by a...

journal_title：British journal of pharmacology

authors： Ishida H,Fujii E,Irie K,Yoshioka T,Muraki T,Ogawa R

更新日期：2000-07-01 00:00:00

abstract：:1. Unique among the phospholipids, phosphatidylserine depresses brain energy metabolism when injected intravenously into mice in the form of sonicated liposomes. The possibility that this effect results from a metabolic transformation of phosphatidylserine is examined in this paper. 2. A strong enhancement of the phos...

journal_title：British journal of pharmacology

authors： Bigon E,Boarato E,Bruni A,Leon A,Toffano G

更新日期：1979-12-01 00:00:00

abstract：:The last five years have witnessed a remarkable resurgence of interest in myocardial reperfusion injury. Reperfusion is absolutely essential to salvage ischaemic myocardium but experimental and clinical studies show that reperfusion-associated injury may mask the full benefits of prompt reperfusion in acute myocardial...

journal_title：British journal of pharmacology

authors： Baxter GF,Burley DS

更新日期：2008-01-01 00:00:00

abstract：:1 The effects of the putative 5-hydroxytryptamine (5-HT) receptor antagonists, methysergide, mianserin and methergoline, the dopamine receptor antagonists, haloperidol, thioridazine and clozapine, and the noradrenaline (NA) receptor antagonists, phentolamine, phenoxybenzamine and propranolol on the behavioural respons...

journal_title：British journal of pharmacology

authors： Dourish CT

更新日期：1982-09-01 00:00:00

abstract：:1. The effects of an intrathecally administered benzodiazepine receptor (BZR) agonist (midazolam, up to 50 micrograms), antagonist (flumazenil, Ro 15-1788, 5 micrograms) and inverse agonist (Ro 19-4603, 15 micrograms) on nociception and on morphine-induced antinociception were studied in rats. 2. By themselves, none o...

journal_title：British journal of pharmacology

authors： Moreau JL,Pieri L

更新日期：1988-04-01 00:00:00

abstract：:1. The ability of the putative, selective post-junctional alpha 2-adrenoceptor antagonist, SK&F 104078 to antagonize the effects of structurally-diverse agonists at pre-junctional alpha 2-adrenoceptors in the guinea-pig ileum and rat vas deferens in vitro and in the rat heart in vivo, and at post-junctional alpha 2-ad...

journal_title：British journal of pharmacology

authors： Akers I,Coates J,Drew GM,Sullivan AT

更新日期：1991-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Mitochondria possess their own source of cAMP, that is, soluble adenylyl cyclase (sAC). Activation or expression of mitochondrial sAC promotes mitochondrial function. Oestrogen receptor signalling plays an essential role in the regulation of mitochondrial function. Here we aimed to determine whet...

journal_title：British journal of pharmacology

authors： Pozdniakova S,Guitart-Mampel M,Garrabou G,Di Benedetto G,Ladilov Y,Regitz-Zagrosek V

更新日期：2018-10-01 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:Down's syndrome is a common genetic cause of intellectual disability, for which there are no drug therapies. Mechanistic studies in a model of Down's syndrome [Ts65Dn (TS) mice] demonstrated that impaired cognitive function was due to excessive neuronal inhibitory tone. These deficits were normal...

journal_title：British journal of pharmacology

authors： Colas D,Chuluun B,Warrier D,Blank M,Wetmore DZ,Buckmaster P,Garner CC,Heller HC

更新日期：2013-07-01 00:00:00

abstract：:The effects of aconitine, an Aconitum alkaloid, on spontaneous inhibitory and excitatory postsynaptic currents (IPSCs and EPSCs respectively) were investigated in the mechanically dissociated rat ventromedial hypothalamic (VMH) neurons in which native presynaptic nerve terminals remained intact. Under current-clamp co...

journal_title：British journal of pharmacology

authors： Yamanaka H,Doi A,Ishibashi H,Akaike N

更新日期：2002-02-01 00:00:00

abstract：:1. Yawning was induced by subcutaneous (s.c.) injection of low doses of apomorphine to rats. This effect decreased with increasing doses of the drug. 2. Intraperitoneal (i.p.) pretreatment of animals with sulpiride (D2-receptor blocker) reduced the frequency of the yawns induced by apomorphine, while SCH 23390 (D1-rec...

journal_title：British journal of pharmacology

authors： Zarrindast MR,Poursoltan M

更新日期：1989-04-01 00:00:00

abstract：:In perfused rabbit adrenal glands, colchicine (500 muM) inhibited the catecholamine secretion evoked by acetylcholine (20 mug/ml) but not that evoked by excess potassium (60 mM). Since both stimuli are believed to release catecholamines ultimately by the same secretory process, exocytosis, it is concluded that these i...

journal_title：British journal of pharmacology

authors： Douglas WW,Sorimachi M

更新日期：1972-05-01 00:00:00

abstract：:1 The responses of excitatory junctions on locust skeletal muscle fibres to iontophoretically applied L-glutamic acid and DL-ibotenic acid, a rigidly extended analogue of glutamate, were recorded by means of intracellular microelectrodes.2 Iontophoresis of L-glutamate to junctional sites produced transient depolarizat...

journal_title：British journal of pharmacology

authors： Clark RB,Gration KA,Usherwood PN

更新日期：1979-06-01 00:00:00

abstract：:The novel urotensin-II (U-II) receptor (UT) ligand, [Pen(5),DTrp(7),Dab(8)]U-II(4-11) (UFP-803), was pharmacologically evaluated and compared with urantide in in vitro and in vivo assays. In the rat isolated aorta, UFP-803 was inactive alone but, concentration dependently, displaced the contractile response to U-II to...

journal_title：British journal of pharmacology

authors： Camarda V,Spagnol M,Song W,Vergura R,Roth AL,Thompson JP,Rowbotham DJ,Guerrini R,Marzola E,Salvadori S,Cavanni P,Regoli D,Douglas SA,Lambert DG,Calò G

更新日期：2006-01-01 00:00:00

abstract：:The effect of acute, streptozotocin-induced diabetes on the affinity (KD), density (Bmax) and selectivity of specific, high affinity binding sites for [125I]-endothelin [( 125I]-ET) in rat cardiac membrane fragments was determined. Three days after a single i.v. bolus dose of streptozotocin (60 mg kg-1), the density o...

journal_title：British journal of pharmacology

authors： Nayler WG,Liu JJ,Panagiotopoulos S,Casley DJ

更新日期：1989-08-01 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：BACKGROUND AND PURPOSE:Peptide YY (PYY) and neuropeptide Y (NPY) activate Y receptors, targets under consideration as treatments for diarrhoea and other intestinal disorders. We investigated the gastrointestinal consequences of selective PYY or NPY ablation on mucosal ion transport, smooth muscle activity and transit u...

journal_title：British journal of pharmacology

authors： Tough IR,Forbes S,Tolhurst R,Ellis M,Herzog H,Bornstein JC,Cox HM

更新日期：2011-09-01 00:00:00

abstract：:1. The alpha 2-adrenoceptor agonists TL99 (2-(N N-dimethyl)amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene) and UK14304 (5-bromo-6-[2-imidazoline-2-yl-aminol]-quinoxaline), in concentrations that are less than 1% of those producing vasoconstriction, enhance vasoconstrictor responses to noradrenaline and phenylephrin...

journal_title：British journal of pharmacology

authors： Xiao XH,Rand MJ

更新日期：1989-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although picrotoxin is a well-established antagonist of GABA(A) receptors, detailed studies of its action on inhibitory synaptic transmission have not previously been made. EXPERIMENTAL APPROACH:Electrophysiological techniques were used to study the action of picrotoxin on inhibitory postsynapti...

journal_title：British journal of pharmacology

authors： Korshoej AR,Holm MM,Jensen K,Lambert JD

更新日期：2010-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Insulin resistance is often found to be associated with high blood pressure. We propose that in insulin-resistant hypertension, endothelial dysfunction is the consequence of increased activity of vascular MMP-2. As MMP-2 proteolytically cleaves a number of extracellular matrix proteins, we hypoth...

journal_title：British journal of pharmacology

authors： Nagareddy PR,Rajput PS,Vasudevan H,McClure B,Kumar U,Macleod KM,McNeill JH

更新日期：2012-02-01 00:00:00

abstract：:Irritable bowel syndrome is characterized by visceral hyperalgesia commonly associated with stress and inflammatory processes. We investigated the role of tachykinin NK2 receptors in the ability of trinitrobenzenesulphonic acid (TNBS) and stress to enhance the sensitivity of the rat rectum to distension using a select...

journal_title：British journal of pharmacology

authors： Toulouse M,Coelho AM,Fioramonti J,Lecci A,Maggi C,Buéno L

更新日期：2000-01-01 00:00:00

abstract：:The processes underpinning post-developmental neurogenesis in the mammalian brain continue to be defined. Such processes involve the proliferation of neural stem cells and neural progenitor cells (NPCs), neuronal migration, differentiation and integration into a network of functional synapses within the brain. Both in...

journal_title：British journal of pharmacology

authors： Prenderville JA,Kelly ÁM,Downer EJ

更新日期：2015-08-01 00:00:00

abstract：:1. The present study characterizes and classifies alpha 1-adrenoceptor-mediated vasoconstriction in the isolated perfused kidney of rat using quantitative receptor pharmacology and compares the results to radioligand binding studies (made in cloned alpha 1-adrenoceptor subtypes, native alpha 1A-adrenoceptors in submax...

journal_title：British journal of pharmacology

authors： Blue DR Jr,Bonhaus DW,Ford AP,Pfister JR,Sharif NA,Shieh IA,Vimont RL,Williams TJ,Clarke DE

更新日期：1995-05-01 00:00:00

abstract：:1. We examined the effects of eprosartan, an AT(1) receptor antagonist, on the progression of left ventricular (LV) dysfunction and remodelling in dogs with heart failure (HF) produced by intracoronary microembolizations (LV ejection fraction, EF 30 to 40%). 2. Dogs were randomized to 3 months of oral therapy with low...

journal_title：British journal of pharmacology

authors： Suzuki G,Mishima T,Tanhehco EJ,Sharov VG,Todor A,Rostogi S,Gupta RC,Chaudhry PA,Anagnostopoulos PV,Nass O,Goldstein S,Sabbah HN

更新日期：2003-01-01 00:00:00

abstract：:1. Therapeutic doses of colistin sulphomethate sodium B.P. (Colomycin), pento-N sulphomethylpolymyxin B sodium (Thiosporin) and ampicillin B.P. (Penbritin) as well as normal saline have been given to volunteers with normal kidney function.2. A blind crossover technique was used and the effects of the compounds on bloo...

journal_title：British journal of pharmacology

authors： Caldwell AD,Martin AJ,Trigger DJ

更新日期：1969-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Combretastatin A-4 3-O-phosphate (CA4P) is in clinical trial as a tumour vascular disrupting agent (VDA) but the cause of blood flow disruption is unclear. We tested the hypothesis that activation of Rho/Rho kinase (ROCK) is fundamental to the effects of this drug in vivo. EXPERIMENTAL APPROACH:...

journal_title：British journal of pharmacology

authors： Williams LJ,Mukherjee D,Fisher M,Reyes-Aldasoro CC,Akerman S,Kanthou C,Tozer GM

更新日期：2014-11-01 00:00:00

abstract：:1. Inhibition of rat platelet aggregation by the nitric oxide (NO) donor MAHMA NONOate (Z-1-N-methyl-N-[6-(N-methylammoniohexyl)amino]diazen-1-ium-1,2-diolate) was investigated. The aims were to compare its anti-aggregatory effect with vasorelaxation, to determine the effects of the soluble guanylate cyclase inhibitor...

journal_title：British journal of pharmacology

authors： Homer KL,Wanstall JC

更新日期：2002-12-01 00:00:00