Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology.

abstract：:1 Peptide 401, a potent mast cell degranulating factor from bee venom, substantially inhibited the oedema provoked by subplantar injection of carrageenin or intra-articular injection of turpentine in the rat. The ED(50) of 401 was c. 0.1 mg/kg. The anti-inflammatory effect was assessed by measurement of the increased ...

journal_title：British journal of pharmacology

authors： Hanson JM,Morley J,Soria-Herrera C

更新日期：1974-03-01 00:00:00

abstract：:1. We investigated the role of adenosine 3':5'-cyclic monophosphate (cyclic AMP) in non-adrenergic non-cholinergic (NANC) contraction in guinea-pig bronchial strips. 2. Forskolin (3 nM to 1 microM) reduced NANC contraction induced by electrical field stimulation (EFS) in a concentration-dependent fashion (-log EC50 wa...

journal_title：British journal of pharmacology

authors： Aikawa T,Sekizawa K,Morikawa M,Itabashi S,Sasaki H,Takishima T

更新日期：1992-03-01 00:00:00

abstract：:Oxidized low density lipoproteins (oxLDL) are thought to play a major role in atherosclerosis. OxLDL act in part through alteration of intracellular signalling pathways in cells of the vascular wall. We recently reported that the EGF receptor (EGFR) signalling pathway is activated by lipid peroxidation products (among...

journal_title：British journal of pharmacology

authors： Vacaresse N,Vieira O,Robbesyn F,Jürgens G,Salvayre R,Negre-Salvayre A

更新日期：2001-04-01 00:00:00

abstract：:1. We aimed to determine whether there are any changes in responsiveness of the mesenteric arterial beds to phenylephrine (Phe) and KCl in exercise-trained rats, and whether vascular endothelium and/or vascular smooth muscle play a role in these changes. 2. Adult male rats were subjected to a swimming schedule every d...

journal_title：British journal of pharmacology

authors： Jansakul C,Hirunpan P

更新日期：1999-08-01 00:00:00

abstract：:1. Sarcolemmal membranes were isolated from normal and from denervated muscles and the specific binding of [125I]-alpha-bungarotoxin to the membranes was determined. 2. Cytosol prepared from either slow (soleus) or fast (extensor digitorum longus) muscle increased the toxin binding. Similar effects were seen with cyto...

journal_title：British journal of pharmacology

authors： Harborne AJ,Smith ME

更新日期：1988-07-01 00:00:00

abstract：:The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand propert...

journal_title：British journal of pharmacology

authors： Alexander SP,Peters JA,Kelly E,Marrion N,Benson HE,Faccenda E,Pawson AJ,Sharman JL,Southan C,Davies JA,CGTP Collaborators.

更新日期：2015-12-01 00:00:00

abstract：:1 Sheep were injected with either methotrexate or melphalan in an attempt to lower the numbers of neutrophil granulocytes in peripheral blood. 2 Methotrexate, 5.0 mg/kg intravenously, on three consecutive days, produced no noticeable clinical or haematological changes. 3 A single dose of melphalan, 1.0 mg/kg intraveno...

journal_title：British journal of pharmacology

authors： Greenwood B,Kerry PJ

更新日期：1978-06-01 00:00:00

abstract：:1. The serine/threonine protein phosphatase (PP) inhibitors, okadaic acid and calyculin, attenuated the IgE-mediated release of histamine from human lung mast cells (HLMC) and basophils in a dose-dependent manner whereas an alternative PP inhibitor, microcystin, was ineffective. Calyculin was more potent than okadaic ...

journal_title：British journal of pharmacology

authors： Peirce MJ,Munday MR,Peachell PT

更新日期：1998-11-01 00:00:00

abstract：:Glucagon-like peptide 1 (GLP-1) is a relatively recently discovered molecule originating in the so-called L-cells of the intestine. The peptide has insulinotrophic properties and it is this characteristic that has predominantly been investigated. This has led to the use of the GLP-1-like peptide exendin-4 (EX-4), whic...

journal_title：British journal of pharmacology

authors： Harkavyi A,Whitton PS

更新日期：2010-02-01 00:00:00

abstract：:1. Several amino-acid esters and amides have been prepared and their toxicological and pharmacological properties have been investigated. Some of the quaternary esters and amides were lethal to mice at doses below 1 mg/kg; this lethality was usually associated with high nicotinic activity. None of the compounds showed...

journal_title：British journal of pharmacology

authors： Barrass BC,Brimblecombe RW,Parkes DC,Rich P

更新日期：1968-10-01 00:00:00

abstract：:1. The effects of cocaine, 6-hydroxydopamine (6-OHDA), reserpine and 17-beta-oestradiol on the sensitivity of the rat anococcygeus muscle to noradrenaline (NA), acetylcholine (ACh) and KCl were investigated.2. Cocaine (10(-5)M) increased the sensitivity of the anococcygeus to NA (100-fold) but not to ACh or KCl.3. 6-O...

journal_title：British journal of pharmacology

authors： Gibson A,Pollock D

更新日期：1973-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Red wine polyphenols (RWPs) inhibit the expression of vascular endothelial growth factor (VEGF), a major pro-angiogenic and pro-atherosclerotic factor, in vascular smooth muscle cells (VSMCs). The aim of this study was to identify which red wine polyphenols were inhibitory and to determine the me...

journal_title：British journal of pharmacology

authors： Oak MH,Bedoui JE,Madeira SV,Chalupsky K,Schini-Kerth VB

更新日期：2006-10-01 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：:In vitro preparations of rabbit heart were made from which measurements of effective refractory period (ERP), atrio-Hisian (A-H) and His-Purkinje (H-P) conduction times could be obtained, analogous to electrophysiological measurements customarily carried out in vivo. Intracellular potentials also were recorded from th...

journal_title：British journal of pharmacology

authors： Millar JS,Vaughan Williams EM

更新日期：1983-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The homeostatic control of arterial BP is well understood with changes in BP resulting from changes in cardiac output (CO) and/or total peripheral resistance (TPR). A mechanism-based and quantitative analysis of drug effects on this interrelationship could provide a basis for the prediction of dr...

journal_title：British journal of pharmacology

authors： Snelder N,Ploeger BA,Luttringer O,Rigel DF,Webb RL,Feldman D,Fu F,Beil M,Jin L,Stanski DR,Danhof M

更新日期：2013-08-01 00:00:00

abstract：:1. Transepithelial transport of a fluorescent derivative of octreotide (NBD-octreotide) was studied in freshly isolated, functionally intact renal proximal tubules from killifish (Fundulus heteroclitus). 2. Drug accumulation in the tubular lumen was visualized by means of confocal microscopy and was measured by image ...

journal_title：British journal of pharmacology

authors： Gutmann H,Miller DS,Droulle A,Drewe J,Fahr A,Fricker G

更新日期：2000-01-01 00:00:00

abstract：:1. Adult male rats were treated with propranolol (2.0 mg kg-1 day-1 i.p.), pindolol (0.2 mg kg-1 day-1 i.p.) or 0.9% NaCl day-1 i.p. and exposed to +4 degrees C for 42 days, or treated with 0.9% NaCl day-1 i.p. and kept at +23 degrees C for 42 days. They were weighed once a week, when a 24 h urine sample was also coll...

journal_title：British journal of pharmacology

authors： Kortelainen ML,Huttunen P,Lapinlampi T

更新日期：1990-04-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The P2X(7) receptor exhibits complex pharmacological properties. In this study, binding of a [(3)H]-labelled P2X(7) receptor antagonist to human P2X(7) receptors has been examined to further understand ligand interactions with this receptor. EXPERIMENTAL APPROACH:The P2X(7) receptor antagonist, ...

journal_title：British journal of pharmacology

authors： Michel AD,Chambers LJ,Clay WC,Condreay JP,Walter DS,Chessell IP

更新日期：2007-05-01 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:There is growing interest in the physiological functions of flavonoids, especially in their effects on cognitive function and on neurodegenerative diseases. The aim of the current investigation was to evaluate the role of the flavonoid baicalein in long-term potentiation (LTP) in the hippocampal ...

journal_title：British journal of pharmacology

authors： Wang W,Wang F,Yang YJ,Hu ZL,Long LH,Fu H,Xie N,Chen JG

更新日期：2011-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Metabolic and cardiovascular abnormalities accompanying metabolic syndrome, such as obesity, insulin resistance and hypertension, are all associated with endothelial dysfunction and are independent risk factors for erectile dysfunction. The purpose of the present study was to investigate the vasc...

journal_title：British journal of pharmacology

authors： Contreras C,Sánchez A,Martínez P,Raposo R,Climent B,García-Sacristán A,Benedito S,Prieto D

更新日期：2010-09-01 00:00:00

abstract：:Photorelaxation of vascular smooth muscle (VSM) is caused by the release of nitric oxide (NO) from a finite molecular store that can be depleted by irradiating pre-contracted arteries with visible light. The ability of an 'exhausted' vessel to respond to a further period of illumination is lost temporarily but then re...

journal_title：British journal of pharmacology

authors： Megson IL,Holmes SA,Magid KS,Pritchard RJ,Flitney FW

更新日期：2000-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tetracyclines were recently found to induce tumour cell death, but the early processes involved in this cytotoxic effect remain unclear. EXPERIMENTAL APPROACH:Viability of human and mouse melanoma cells was determined by MTT assay and flow cytometry. Kinase/protein/caspase activation was measure...

journal_title：British journal of pharmacology

authors： Shieh JM,Huang TF,Hung CF,Chou KH,Tsai YJ,Wu WB

更新日期：2010-07-01 00:00:00

abstract：:1. To elucidate whether K+ channels play a role in the action of epithelium-dependent bronchodilatation, we studied responses in human bronchial strips in the presence of indomethacin and NG-nitro-L-arginine methylester under isometric conditions, in vitro. 2. Mechanical removal of the epithelium increased the contrac...

journal_title：British journal of pharmacology

authors： Tamaoki J,Tagaya E,Isono K,Kondo M,Konno K

更新日期：1997-06-01 00:00:00

abstract：:1. The ability of a range of substituted imidazole compounds to inhibit mouse cerebellar neuronal nitric oxide synthase (nNOS), bovine aortic endothelial NOS (eNOS) and inducible NOS (iNOS) from lungs of endotoxin-pretreated rats was investigated. In each case the substrate (L-arginine) concentration employed was 120 ...

journal_title：British journal of pharmacology

authors： Handy RL,Harb HL,Wallace P,Gaffen Z,Whitehead KJ,Moore PK

更新日期：1996-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We sought to understand why (-)-cannabidiol (CBD) and (-)-cannabidiol-dimethylheptyl (CBD-DMH) exhibit distinct pharmacology, despite near identical structures. EXPERIMENTAL APPROACH:HEK293A cells expressing either human type 1 cannabinoid (CB1 ) receptors or CB2 receptors were treated with CBD ...

journal_title：British journal of pharmacology

authors： Tham M,Yilmaz O,Alaverdashvili M,Kelly MEM,Denovan-Wright EM,Laprairie RB

更新日期：2019-05-01 00:00:00

abstract：:Three neurotoxin homologues (CM10 and CM12 from Naja haje annulifera and S5C10 from Dendroaspis jamesoni kaimosae) and two short neurotoxins (CM14 from Naja haje annulifera and erabutoxin b from Laticauda semifasciata) were examined by circular dichroism (c.d.) and tested for neuromuscular activity on chick biventer c...

journal_title：British journal of pharmacology

authors： Harvey AL,Hider RC,Hodges SJ,Joubert FJ

更新日期：1984-07-01 00:00:00

abstract：:1. The effects of paracetamol and lysine acetylsalicylate (L-AS) on high-threshold mechanonociceptors have been investigated by recording neural activity from the inflamed ankle joint in anaesthetized rats with mild adjuvant-induced monoarthritis. 2. Paracetamol (50 mg kg-1, i.v.) and L-AS (100 mg kg-1, i.v., equivale...

journal_title：British journal of pharmacology

authors： McQueen DS,Iggo A,Birrell GJ,Grubb BD

更新日期：1991-09-01 00:00:00

abstract：:1. Vasorelaxant properties of three nitric oxide (NO) donor drugs (glyceryl trinitrate, sodium nitroprusside and spermine NONOate) in mouse aorta (phenylephrine pre-contracted) were compared with those of endothelium-derived NO (generated with acetylcholine), NO free radical (NO*; NO gas solution) and nitroxyl ion (NO...

journal_title：British journal of pharmacology

authors： Wanstall JC,Jeffery TK,Gambino A,Lovren F,Triggle CR

更新日期：2001-10-01 00:00:00

abstract：:1. Microvascular permeability in the mesentery and consequent leakage of protein into the peritoneum of spontaneously hypertensive rats (SHR) and normotensive rats (NTR) was measured in vivo by the extravasation of Evans blue dye. 2. In sensitized NTR, challenge with antigen produced extensive increases in dye extrava...

journal_title：British journal of pharmacology

authors： Kwasniewski FH,Tavares de Lima W,Bakhle YS,Jancar S

更新日期：1998-06-01 00:00:00