Temperature-sensitive transient receptor potential vanilloid channels: structural insights into ligand-dependent activation.

abstract：:An increasing number of examples in the literature suggest that the in vivo duration of drug action not only depends on macroscopic pharmacokinetic properties like plasma half-life and the time needed to equilibrate between the plasma and the effect compartments, but is also influenced by long-lasting target binding a...

journal_title：British journal of pharmacology

authors： Vauquelin G,Charlton SJ

更新日期：2010-10-01 00:00:00

abstract：:1. Heat stress (HS) is known to protect against myocardial ischaemia-reperfusion injury by improving mechanical dysfunction and decreasing necrosis. However, the mechanisms responsible for this form of cardioprotection remain to be elucidated. ATP-sensitive potassium (K(ATP)) channels have been shown to be involved in...

journal_title：British journal of pharmacology

authors： Joyeux M,Godin-Ribuot D,Ribuot C

更新日期：1998-03-01 00:00:00

abstract：:1 The effect of thiopentone, methohexitone, urethane and ketamine on the uptake and release of gamma-aminobutyric acid (GABA) and D-aspartate by rat thalamic slices has been investigated. 2 A high, supra-anaesthetic concentration of methohexitone increased the uptake of both D-aspartate and GABA. 3 None of the anaesth...

journal_title：British journal of pharmacology

authors： Kendall TJ,Minchin MC

更新日期：1982-01-01 00:00:00

abstract：:(1) Stimulation of the vanilloid receptor-1 (TRPV1) results in the activation of nociceptive and neurogenic inflammatory responses. Poor specificity and potency of TRPV1 antagonists has, however, limited the clarification of the physiological role of TRPV1. (2) Recently, iodo-resiniferatoxin (I-RTX) has been reported ...

journal_title：British journal of pharmacology

authors： Rigoni M,Trevisani M,Gazzieri D,Nadaletto R,Tognetto M,Creminon C,Davis JB,Campi B,Amadesi S,Geppetti P,Harrison S

更新日期：2003-03-01 00:00:00

abstract：:1. Adenosine 5'-triphosphate (ATP) is known to augment cardiac contractile activity and cause an increase in intracellular Ca(2+) concentration ([Ca(2+)](i)) in isolated cardiomyocytes. However, no information regarding the ATP-mediated signal transduction in the myocardium in congestive heart failure (CHF) is availab...

journal_title：British journal of pharmacology

authors： Saini HK,Shao Q,Musat S,Takeda N,Tappia PS,Dhalla NS

更新日期：2005-01-01 00:00:00

abstract：:1. Bepridil (BPD) is a pharmacological compound able to bind to the Ca2+ sensor protein troponin C (TnC), which triggers skeletal muscle contraction upon Ca2+-binding. BPD can thereby modulate the Ca2+-affinity of this protein. 2. The Ca2+-sensitizing action of bepridil was investigated on slow and fast isoforms of Tn...

journal_title：British journal of pharmacology

authors： Kischel P,Stevens L,Mounier Y

更新日期：1999-10-01 00:00:00

abstract：:1 PD 117302, a new nonpeptide opioid compound shown in in vitro studies to be a selective kappa-opioid agonist, has been evaluated in vivo for antinociceptive activity and other effects characteristic of kappa-receptor activation. 2 Dose-related long lasting antinociception was produced by PD 117302 against a mechanic...

journal_title：British journal of pharmacology

authors： Leighton GE,Johnson MA,Meecham KG,Hill RG,Hughes J

更新日期：1987-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is major evidence for the strong bi-directional interrelation of parenchymal cell apoptosis and leukocyte accumulation and inflammation in acute liver injury. Therefore, the aim of this in vivo study was to investigate the anti-apoptotic and anti-inflammatory potential of antileukoproteinas...

journal_title：British journal of pharmacology

authors： Eipel C,Kidess E,Abshagen K,Leminh K,Menger MD,Burkhardt H,Vollmar B

更新日期：2007-06-01 00:00:00

abstract：:Antigen challenge in vivo of rat peritoneal cells (enriched with monocytes and polymorphonuclear leucocytes) passively sensitized 2 h previously with homologous antibody of the IgGa class released large amounts of slow-reacting substance of anaphylaxis (SRS-A, 1739 +/- 59 u/ml) into the peritoneal fluid. This reaction...

journal_title：British journal of pharmacology

authors： Burka JF,Garland LG

更新日期：1977-12-01 00:00:00

abstract：:In the present study we tested the effects of the antihyperalgesic compound gabapentin on dorsal horn neurones in adult spinal cord. Slices were taken from control and hyperalgesic animals suffering from streptozocin-induced diabetic neuropathy. At concentrations up to 100 microM, bath application failed to affect the...

journal_title：British journal of pharmacology

authors： Patel MK,Gonzalez MI,Bramwell S,Pinnock RD,Lee K

更新日期：2000-08-01 00:00:00

abstract：:The binding of a series of amide derivatives of methotrexate to Lactobacillus casei dihydrofolate reductase has been studied by inhibition constant measurements and by 1H n.m.r. spectroscopy. Amide modification of the alpha-carboxylate of methotrexate was found to prevent interaction of the gamma-carboxylate with the ...

journal_title：British journal of pharmacology

authors： Antonjuk DJ,Birdsall B,Cheung HT,Clore GM,Feeney J,Gronenborn A,Roberts GC,Tran TQ

更新日期：1984-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:JNJ-Q2, a novel broad-spectrum fluoroquinolone with anti-methicillin-resistant Staphylococcus aureus activity, was evaluated in a comprehensive set of non-clinical and clinical cardiovascular safety studies. The effect of JNJ-Q2 on different cardiovascular parameters was compared with that of mox...

journal_title：British journal of pharmacology

authors： Eichenbaum G,Pugsley MK,Gallacher DJ,Towart R,McIntyre G,Shukla U,Davenport JM,Lu HR,Rohrbacher J,Hillsamer V

更新日期：2012-07-01 00:00:00

abstract：:Chronic itch poses major health care and economic burdens worldwide. In 2013, B-type natriuretic peptide (BNP) was identified as an itch-selective neuropeptide and shown to be both necessary and sufficient to produce itch behaviour in mice. Since then, mechanistic studies of itch have increased, not only at central le...

journal_title：British journal of pharmacology

authors： Meng J,Chen W,Wang J

更新日期：2020-03-01 00:00:00

abstract：:In addition to their classical known effects, such as analgesia, impairment of cognition and learning and appetite enhancement, cannabinoids have also been related to the regulation of cardiovascular responses and implicated in cardiovascular pathology. Elevated levels of endocannabinoids have been related to the extr...

journal_title：British journal of pharmacology

authors： Mendizábal VE,Adler-Graschinsky E

更新日期：2007-06-01 00:00:00

abstract：:1. We have studied the effect of cannabinoid agonists (CP 55,940 and cannabinol) on intestinal motility in a model of intestinal inflammation (induced by oral croton oil in mice) and measured cannabinoid receptor expression, endocannabinoids (anandamide and 2-arachidonylglycerol) and anandamide amidohydrolase activity...

journal_title：British journal of pharmacology

authors： Izzo AA,Fezza F,Capasso R,Bisogno T,Pinto L,Iuvone T,Esposito G,Mascolo N,Di Marzo V,Capasso F

更新日期：2001-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Post-operative ileus (POI) is induced by intestinal inflammation. Here, we aimed to clarify the effects of 5-HT3 receptor antagonists against POI. EXPERIMENTAL APPROACH:We administered three 5-HT3 receptor antagonists, ondansetron, tropisetron and palonosetron, to a mouse model of POI induced by...

journal_title：British journal of pharmacology

authors： Maehara T,Matsumoto K,Horiguchi K,Kondo M,Iino S,Horie S,Murata T,Tsubone H,Shimada S,Ozaki H,Hori M

更新日期：2015-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pemphigus and pemphigoid diseases are characterized and caused predominantly by IgG autoantibodies targeting structural proteins of the skin. Their current treatment relies on general and prolonged immunosuppression that causes severe adverse events, including death. Hence, novel safe and more ef...

journal_title：British journal of pharmacology

authors： Kasprick A,Hofrichter M,Smith B,Ward P,Bieber K,Shock A,Ludwig RJ,Schmidt E

更新日期：2020-05-01 00:00:00

abstract：:1. Derivatization of nonsteroidal anti-inflammatory drugs, such that they release nitric oxide (NO) in small amounts, has been shown to significantly increase their anti-inflammatory activity and analgesic potency. In this study, we compared the anti-inflammatory potency of prednisolone to a nitric oxide-releasing der...

journal_title：British journal of pharmacology

authors： Turesin F,del Soldato P,Wallace JL

更新日期：2003-07-01 00:00:00

abstract：:1. An investigation was carried out to determine if the sympathoinhibition caused by urapidil is due to activation of 5-HT1A receptors by investigating whether it could be reversed by the non-selective 5-HT1A receptor antagonist spiperone. To control for the possibility of functional antagonism by spiperone, the abili...

journal_title：British journal of pharmacology

authors： Ramage AG

更新日期：1991-04-01 00:00:00

abstract：:1. Carrageenin or 5-hydroxytryptamine-induced oedema of the mouse hind paw was antagonized by catecholamines acting on both alpha- and beta-adrenoceptors.2. Increased permeability of the mouse peritoneum induced by the local injection of acetic acid or pro-inflammatory mediators was antagonized by catecholamines actin...

journal_title：British journal of pharmacology

authors： Green KL

更新日期：1972-06-01 00:00:00

abstract：:1 The effects of general anaesthetics on the responses of neurones to iontophoretically applied L-glutamate have been examined in slices of the guinea-pig olfactory cortex in vitro. 2 Concentrations of pentobarbitone, ether, methoxyflurance, trichloroethylene and alphaxalone that are known to depress synaptic transmis...

journal_title：British journal of pharmacology

authors： Richards CD,Smaje JC

更新日期：1976-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:To determine whether there is an association between vascular NADPH oxidase (NOX), superoxide, the small GTPase Rac(1) and PDE type 5 (PDE5) in human vascular smooth muscle cell (hVSMCs). EXPERIMENTAL APPROACH:hVSMCs were incubated with xanthine-xanthine oxidase (X-XO; a superoxide generating sy...

journal_title：British journal of pharmacology

authors： Muzaffar S,Shukla N,Bond M,Sala-Newby GB,Newby AC,Angelini GD,Jeremy JY

更新日期：2008-11-01 00:00:00

abstract：:1. Perivascular nerves of the sheep middle cerebral artery show immunoreactivity for both vasoactive intestinal polypeptide (VIP) and calcitonin gene-related peptide (CGRP). 2. Rings of endothelium-denuded sheep middle cerebral artery precontracted with 5-hydroxytryptamine were relaxed by CGRP (maximum relaxation = 87...

journal_title：British journal of pharmacology

authors： Gaw AJ,Aberdeen J,Humphrey PP,Wadsworth RM,Burnstock G

更新日期：1991-03-01 00:00:00

abstract：:1. The effect of adenosine triphosphate (ATP) and its stable analogues, alpha, beta-methylene-ATP and beta, gamma-methylene-ATP, on the efferent function of capsaicin-sensitive non-adrenergic, non-cholinergic (NANC) nerves was tested in guinea-pig isolated atria. 2. Transmural nerve stimulation of atria isolated from ...

journal_title：British journal of pharmacology

authors： Rubino A,Amerini S,Ledda F,Mantelli L

更新日期：1992-03-01 00:00:00

abstract：:1 In order to address mechanistic differences between arterial vessel types, we have compared the vasorelaxant actions of anandamide in resistance (G3) and conduit (G0) mesenteric arteries. 2 Anandamide produced concentration-dependent relaxations of pre-constricted G3 arteries with a maximal response that was signifi...

journal_title：British journal of pharmacology

authors： O'Sullivan SE,Kendall DA,Randall MD

更新日期：2004-06-01 00:00:00

abstract：:1. The present study was aimed at examining P2 receptor-mediated vasodilatation in human vessels. The isometric tension was recorded in isolated segments of the human left internal mammary artery branches precontracted with 1 microM noradrenaline. 2. Endothelial denudation abolished the dilator responses. 3. The selec...

journal_title：British journal of pharmacology

authors： Wihlborg AK,Malmsjö M,Eyjolfsson A,Gustafsson R,Jacobson K,Erlinge D

更新日期：2003-04-01 00:00:00

abstract：:1 The activity and pulmonary metabolism of two peptides, 7-homo Pro-bradykinin and 8-homo Phe-bradykinin were studied in isolated systems. 2 Both analogues were about 50-70 times less active than bradykinin on the guinea-pig ileum and 70-160 times less active on isolated strips of cat terminal ileum. 3 The action of b...

journal_title：British journal of pharmacology

authors： Bakhle YS

更新日期：1977-01-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The psychostimulant cocaine induces complex molecular, cellular and behavioural responses as a consequence of inhibiting presynaptic dopamine, noradrenaline and 5-HT transporters. To elucidate 5-HT transporter (SERT)-specific contributions to cocaine action, we evaluated cocaine effects in the SE...

journal_title：British journal of pharmacology

authors： Simmler LD,Anacker AMJ,Levin MH,Vaswani NM,Gresch PJ,Nackenoff AG,Anastasio NC,Stutz SJ,Cunningham KA,Wang J,Zhang B,Henry LK,Stewart A,Veenstra-VanderWeele J,Blakely RD

更新日期：2017-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pyrazole derivatives have recently been suggested as selective blockers of transient receptor potential cation (TRPC) channels but their ability to distinguish between the TRPC and Orai pore complexes is ill-defined. This study was designed to characterize a series of pyrazole derivatives in term...

journal_title：British journal of pharmacology

authors： Schleifer H,Doleschal B,Lichtenegger M,Oppenrieder R,Derler I,Frischauf I,Glasnov TN,Kappe CO,Romanin C,Groschner K

更新日期：2012-12-01 00:00:00

abstract：:1. Relaxing effect of loop diuretics, piretanide and furosemide in comparison with acetylcholine (ACh) was investigated in guinea-pig isolated mesenteric resistance arteries. 2. Concentration-response curves to ACh (0.001 - 10 microM) and diuretics (0.0001 - 1 microM) were constructed in noradrenaline (10 - 30 microM)...

journal_title：British journal of pharmacology

authors： Pourageaud F,Bappel-Gozalbes C,Marthan R,Freslon JL

更新日期：2000-11-01 00:00:00