Differential inhibition of tumour cell-induced platelet aggregation by the nicotinate aspirin prodrug (ST0702) and aspirin.

abstract：BACKGROUND AND PURPOSE:We have developed a strategy to target the permanently charged lidocaine derivative lidocaine N-ethyl bromide (QX-314) selectively into nociceptive sensory neurons through the large-pore transient receptor potential cation channel subfamily V (TRPV1) noxious heat detector channel. This involves c...

journal_title：British journal of pharmacology

authors： Roberson DP,Binshtok AM,Blasl F,Bean BP,Woolf CJ

更新日期：2011-09-01 00:00:00

abstract：:1. alpha 1-Adrenoceptor subtypes in rabbit thoracic aorta have been examined in binding and functional experiments. 2. [3H]-prazosin bound to two distinct populations of alpha 1-adrenoceptors (pKD,high = 9.94, Rhigh = 79.2 fmol mg-1 protein; pKD,low = 8.59, Rlow = 215 fmol mg-1 protein). Pretreatment with chloroethylc...

journal_title：British journal of pharmacology

authors： Oshita M,Kigoshi S,Muramatsu I

更新日期：1993-04-01 00:00:00

abstract：BACKGROUND:Macrophage elastase (MMP-12) is involved in the inflammatory process of chronic obstructive pulmonary disease (COPD). The aim of this study was to investigate in mice the effect of MMP-12 inhibition on the inflammatory process induced by cigarette smoke (CS) or by lipopolysaccharide (LPS) exposure of the air...

journal_title：British journal of pharmacology

authors： Le Quément C,Guénon I,Gillon JY,Valença S,Cayron-Elizondo V,Lagente V,Boichot E

更新日期：2008-07-01 00:00:00

abstract：:1. The possible mechanisms of action of the inhibitory effect of gomisin C on the respiratory burst of rat neutrophils in vitro was investigated. 2. The peptide formyl-Met-Leu-Phe (FMLP) induced superoxide anion (O2-) formation and O2 consumption, which was inhibited by gomisin C in a concentration-dependent manner (I...

journal_title：British journal of pharmacology

authors： Wang JP,Raung SL,Hsu MF,Chen CC

更新日期：1994-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-HT receptor agonists have variable nociceptive effects within the spinal cord. While there is some evidence for 5-HT(1A) spinally-mediated analgesia, the role of other 5-HT(1) receptor subtypes remains unclear. In the present study, we examined the spinal actions of a range of 5-HT(1) agonists,...

journal_title：British journal of pharmacology

authors： Jeong HJ,Mitchell VA,Vaughan CW

更新日期：2012-03-01 00:00:00

abstract：:1. A series of GABAB receptor antagonists were tested against (+/-)-baclofen for activity on the presynaptic GABAB receptor in the rat vas deferens. 2. All the antagonists tested caused a rightward shift in the concentration-response curve to (+/-)-baclofen. 3. pA2 values calculated from full Schild analysis were as f...

journal_title：British journal of pharmacology

authors： Hills JM,Larkin MM,Howson W

更新日期：1991-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Rhythmical transient constrictions of the lymphatic vessels provide the means for efficient lymph drainage and interstitial tissue fluid balance. This activity is critical during inflammation, to avoid or limit oedema resulting from increased vascular permeability, mediated by the release of vari...

journal_title：British journal of pharmacology

authors： Rehal S,Blanckaert P,Roizes S,von der Weid PY

更新日期：2009-12-01 00:00:00

abstract：:1. We investigated the nitric oxide (NO) dependence of vasorelaxation in response to different calcium channel blockers (CCB), in rabbit femoral artery in vivo. 2. Anaesthetized rabbits underwent femoral artery ligation, and blood from the proximal artery was returned distal to the ligature through a constant infusion...

journal_title：British journal of pharmacology

authors： Xu B,Xiao-hong L,Lin G,Queen L,Ferro A

更新日期：2002-06-01 00:00:00

abstract：:1. TRPM2 is a Ca2+ -permeable nonselective cation channel activated by intracellular ADP-ribose (ADPR) and by hydrogen peroxide (H2O2). We investigated the modulation of TRPM2 activity by N-(p-amylcinnamoyl)anthranilic acid (ACA). ACA has previously been reported to inhibit phospholipase A2 (PLA2). 2. Using patch-clam...

journal_title：British journal of pharmacology

authors： Kraft R,Grimm C,Frenzel H,Harteneck C

更新日期：2006-06-01 00:00:00

abstract：:1. The effects of various inhibitors of the mitochondrial electron transport chain on the activity of ATP-sensitive K+ channels were examined in the Cambridge rat insulinoma G1 (CRI-G1) cell line using a combination of whole cell and single channel recording techniques. 2. Whole cell current clamp recordings, with 5 m...

journal_title：British journal of pharmacology

authors： Harvey J,Hardy SC,Ashford ML

更新日期：1999-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Protocatechuic acid (PCA) is plentiful in edible fruits and vegetables and is thus one anti-oxidative component of normal human diets. However, the molecular mechanisms involved in the chemopreventive activity of PCA are poorly understood. Here, we investigated the mechanism(s) underlying the ant...

journal_title：British journal of pharmacology

authors： Lin HH,Chen JH,Chou FP,Wang CJ

更新日期：2011-01-01 00:00:00

abstract：:The histamine H3 receptor, first described in 1983 as a histamine autoreceptor and later shown to also function as a heteroreceptor that regulates the release of other neurotransmitters, has been the focus of research by numerous laboratories as it represents an attractive drug target for a number of indications inclu...

journal_title：British journal of pharmacology

authors： Esbenshade TA,Browman KE,Bitner RS,Strakhova M,Cowart MD,Brioni JD

更新日期：2008-07-01 00:00:00

abstract：:1. By use of a number of analogues of adenine nucleotides, the structure-activity relationships of the human platelet receptor for adenosine 5'-diphosphate (ADP) mediating increases in intracellular calcium were investigated, and compared with the known structure-activity relationships for induction by ADP of platelet...

journal_title：British journal of pharmacology

authors： Hall DA,Hourani SM

更新日期：1993-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The use of tubulin-binding compounds, which act in part by inhibiting tumour angiogenesis, has become an integral strategy of tumour therapy. Recently, tubulysins were identified as a novel class of natural compounds of myxobacterial origin, which inhibit tubulin polymerization. As these compound...

journal_title：British journal of pharmacology

authors： Rath S,Liebl J,Fürst R,Ullrich A,Burkhart JL,Kazmaier U,Herrmann J,Müller R,Günther M,Schreiner L,Wagner E,Vollmar AM,Zahler S

更新日期：2012-11-01 00:00:00

abstract：:At nanomolar concentrations, SR141716 and AM251 act as specific and selective antagonists of the cannabinoid CB1 receptor. In the micromolar range, these compounds were shown to inhibit basal G-protein activity, and this is often interpreted to implicate constitutive activity of the CB1 receptors in native tissue. We ...

journal_title：British journal of pharmacology

authors： Savinainen JR,Saario SM,Niemi R,Järvinen T,Laitinen JT

更新日期：2003-12-01 00:00:00

abstract：:1. The sulphonylureas, tolbutamide (0.1-10 mM) and glibenclamide (0.1-100 microM) shown not to inhibit ATP-K+ channel currents when applied to inside-out membrane patches excised from rat cultured cerebral cortex or freshly-dispersed ventromedial hypothalamic nucleus (VMHN) neurones. 2. Saturable binding sites for [3H...

journal_title：British journal of pharmacology

authors： Ashford ML,Boden PR,Treherne JM

更新日期：1990-11-01 00:00:00

abstract：:1. Histamine release by compound 48/80 was substantially reduced in a time-dependent manner (maximum at 30 min) by pre-incubating mast cells in calcium-free medium at 37 degrees C but not at 2 degrees C. This effect was optimal at pH 7.0 to 7.5. 2. The re-introduction of calcium (0.1 to 3 mmol/l) restored histamine re...

journal_title：British journal of pharmacology

authors： Garland LG,Payne AN

更新日期：1979-04-01 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：:1. Release-regulating alpha 2-autoreceptors in human brain were characterized pharmacologically in cortical slices from patients undergoing neurosurgery to remove subcortical tumours; the slices were prelabelled with [3H]-noradrenaline ([3H]-NA) and stimulated electrically (3 Hz, 2 ms, 24 mA) under superfusion conditi...

journal_title：British journal of pharmacology

authors： Raiteri M,Bonanno G,Maura G,Pende M,Andrioli GC,Ruelle A

更新日期：1992-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Normal pregnancy is associated with decreased vascular resistance and increased release of vasodilators. Endothelin-1 (ET-1) causes vasoconstriction via endothelin receptor type A (ET(A)R), but could activate ET(B)R in the endothelium and release vasodilator substances. However, the roles of ET(B...

journal_title：British journal of pharmacology

authors： Mazzuca MQ,Dang Y,Khalil RA

更新日期：2013-07-01 00:00:00

abstract：:Perivascular adipose tissue (PVAT) is now recognized as an active player in vascular homeostasis. The expansion of PVAT in obesity and its possible role in vascular dysfunction have attracted much interest. In terms of the regulation of vascular tone and blood pressure, PVAT has been shown to release vasoactive mediat...

journal_title：British journal of pharmacology

authors： Ramirez JG,O'Malley EJ,Ho WSV

更新日期：2017-10-01 00:00:00

abstract：:Aspirin at therapeutic concentrations does not inhibit the uptake of 5-hydroxytryptamine (5-HT) by blood platelets nor induce release of 5-HT from platelets, although platelet aggregation responses to collagen and arachidonic acid (which are dependent on platelet prostaglandin synthesis) are abolished. This does not s...

journal_title：British journal of pharmacology

authors： Drummond AH,MacIntyre DE,Olverman HJ

更新日期：1977-04-01 00:00:00

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：:1 alpha-Monofluoromethyldopa (MFMD, RMI 71963), a potent and selective enzyme-activated irreversible inhibitor of aromatic L-amino acid decarboxylase produces a substantial and long-lasting decrease in the catecholamine content of mouse brain, heart and kidney. 2 Single doses of MFMD reduce the 5-hydroxytryptamine con...

journal_title：British journal of pharmacology

authors： Bey P,Jung MJ,Koch-Weser J,Palfreyman MG,Sjoerdsma A,Wagner J,Zraïka M

更新日期：1980-12-01 00:00:00

abstract：:1 The actions of prostaglandin F2 alpha (PGF2 alpha) and noradrenaline on contraction and 45Ca exchange have been studied in rat mesenteric arteries. 2 PGF2 alpha and noradrenaline contracted rat isolated mesenteric artery preparations to about the same extent. The PGF2 alpha-stimulated contractions, unlike those prod...

journal_title：British journal of pharmacology

authors： Godfraind T,Miller RC

更新日期：1982-01-01 00:00:00

abstract：:1. Metolazone, a new diuretic, was found to be excreted by glomerular filtration and renal tubular secretion.2. The secretory mechanism was antagonized by probenecid but this did not affect the diuretic action of metolazone. ...

journal_title：British journal of pharmacology

authors： Belair EJ,Cohen AI,Yelnosky J

更新日期：1972-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The human prostacyclin receptor (hIP), a G-protein coupled receptor (GPCR) expressed mainly on platelets and vascular smooth muscle cells, plays important protective roles in the cardiovascular system. We hypothesized that significant insights could be gained into the structure and function of th...

journal_title：British journal of pharmacology

authors： Stitham J,Arehart E,Gleim SR,Li N,Douville K,Hwa J

更新日期：2007-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The development of subtype-selective ligands to inhibit voltage-sensitive sodium channels (VSSCs) has been attempted with the aim of developing therapeutic compounds. Tetrodotoxin (TTX) is a toxin from pufferfish that strongly inhibits VSSCs. Many TTX analogues have been identified from marine an...

journal_title：British journal of pharmacology

authors： Tsukamoto T,Chiba Y,Wakamori M,Yamada T,Tsunogae S,Cho Y,Sakakibara R,Imazu T,Tokoro S,Satake Y,Adachi M,Nishikawa T,Yotsu-Yamashita M,Konoki K

更新日期：2017-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Memantine and ketamine are clinically used, open-channel blockers of NMDA receptors exhibiting remarkable pharmacodynamic similarities despite strikingly different clinical profiles. Although NMDA channel gating constitutes an important difference between memantine and ketamine, it is unclear how...

journal_title：British journal of pharmacology

authors： Emnett CM,Eisenman LN,Mohan J,Taylor AA,Doherty JJ,Paul SM,Zorumski CF,Mennerick S

更新日期：2015-03-01 00:00:00

abstract：:1 The mechanism underlying the enhancement by superoxide dismutase (SOD) of endothelium-dependent relaxation was investigated in rabbit mesenteric resistance arteries. 2 SOD (200 U ml(-1)) increased the production of H(2)O(2) in smooth muscle cells (as indicated by the use of an H(2)O(2)-sensitive fluorescent dye). 3 ...

journal_title：British journal of pharmacology

authors： Itoh T,Kajikuri J,Hattori T,Kusama N,Yamamoto T

更新日期：2003-05-01 00:00:00