Snapshot: implications for melatonin in endoplasmic reticulum homeostasis.

abstract：:1. The effect on systemic haemodynamics of BQ-123, a selective endothelin A (ETA) receptor antagonist, was investigated in healthy men by giving, on separate occasions, ascending intravenous doses of 100, 300, 1000 and 3000 nmol min(-1) BQ-123, each for 15 min, in a randomized, placebo-controlled, double-blind study. ...

journal_title：British journal of pharmacology

authors： Spratt JC,Goddard J,Patel N,Strachan FE,Rankin AJ,Webb DJ

更新日期：2001-10-01 00:00:00

abstract：:Despite its long-standing reputation as a foul smelling and toxic gas that is associated with the decay of biological matter,hydrogen sulphide (H2S) has emerged as an important regulator of cardiovascular homoeostasis. H2S promotes a number of cellular signals that regulate metabolism, cardiac function and cell surviv...

journal_title：British journal of pharmacology

authors： Lefer DJ

更新日期：2008-11-01 00:00:00

abstract：:1. Inhibition of nitric oxide generation with Nw-nitro-L-arginine (nitroarginine) reduced vasodilator responses to bradykinin and acetylcholine and enhanced those to nitroprusside in the rat isolated perfused kidney, preconstricted with phenylephrine. 2. Inhibition of cyclo-oxygenase with indomethacin, decreased the v...

journal_title：British journal of pharmacology

authors： Fulton D,McGiff JC,Quilley J

更新日期：1992-11-01 00:00:00

abstract：:We have performed a systematic mutagenesis of three hydrophobic rings (17', 13' and 9') within transmembrane region (TM) 2 of the alpha9alpha10 nicotinic cholinergic receptor (nAChR) to a hydrophilic (threonine) residue and compared the properties of mutant receptors reconstituted in Xenopus laevis oocytes. Phenotypic...

journal_title：British journal of pharmacology

authors： Plazas PV,De Rosa MJ,Gomez-Casati ME,Verbitsky M,Weisstaub N,Katz E,Bouzat C,Elgoyhen AB

更新日期：2005-08-01 00:00:00

abstract：:1. S 16257 is a new bradycardic agent. Its electropharmacological profile has been compared to that of the known bradycardic compound UL-FS 49 (Zatebradine). Intracellular recordings of action potentials (APs) were performed with conventional glass microelectrodes. 2. In the rabbit isolated sino-atrial node (SAN) tiss...

journal_title：British journal of pharmacology

authors： Thollon C,Cambarrat C,Vian J,Prost JF,Peglion JL,Vilaine JP

更新日期：1994-05-01 00:00:00

abstract：:1. A comparative study was carried out to assess the regional haemodynamic effects of intravenous infusion of human alpha- and beta-calcitonin gene-related peptide (CGRP; 0.006, 0.06 and 0.6 nmol h-1) in conscious, unrestrained Wistar rats. 2. With human alpha-CGRP, tachycardia was always accompanied by a fall in mean...

journal_title：British journal of pharmacology

authors： Gardiner SM,Compton AM,Bennett T

更新日期：1989-12-01 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

abstract：:The role of extracellular signal-regulated kinase (ERK)-1 and ERK-2 in controlling histamine-induced tone in bovine trachealis was investigated. PD 098059, an inhibitor of mitogen-activated protein kinase kinase (MKK)-1, had no effect on the histamine concentration-response relationship that described contraction. How...

journal_title：British journal of pharmacology

authors： Koch A,Nasuhara Y,Barnes PJ,Lindsay MA,Giembycz MA

更新日期：2000-11-01 00:00:00

abstract：:Levetiracetam, the alpha-ethyl analogue of the nootropic piracetam, is a widely used antiepileptic drug (AED) that provides protection against partial seizures and is also effective in the treatment of primary generalized seizure syndromes including juvenile myoclonic epilepsy. Levetiracetam was discovered in 1992 thr...

journal_title：British journal of pharmacology

authors： Rogawski MA

更新日期：2008-08-01 00:00:00

abstract：:1. We investigated the role of nitric oxide (NO) in modulating spinal synaptic responses evoked by electrical and noxious sensory stimuli in the neonatal rat spinal cord in vitro. 2. Potentials were recorded extracellularly from a ventral root (L3-L5) of the isolated spinal cord preparation or spinal cord-saphenous ne...

journal_title：British journal of pharmacology

authors： Kurihara T,Yoshioka K

更新日期：1996-08-01 00:00:00

abstract：:Tyrosine sulfation is a post-translational modification of secreted and transmembrane proteins, including many GPCRs such as chemokine receptors. Most chemokine receptors contain several potentially sulfated tyrosine residues in their extracellular N-terminal regions, the initial binding site for chemokine ligands. Su...

journal_title：British journal of pharmacology

authors： Ludeman JP,Stone MJ

更新日期：2014-03-01 00:00:00

abstract：:1. Neostigmine and BW284C51 induced concentration-dependent contractions in human isolated bronchial preparations whereas tetraisopropylpyrophosphoramide (iso-OMPA) was inactive on airway resting tone. 2. Neostigmine (0.1 microM) or iso-OMPA (100 microM) increased acetylcholine sensitivity in human isolated bronchial ...

journal_title：British journal of pharmacology

authors： Norel X,Angrisani M,Labat C,Gorenne I,Dulmet E,Rossi F,Brink C

更新日期：1993-04-01 00:00:00

abstract：:The interaction of a new nonribose ligand (LUF5831) with the human adenosine A1 receptor was investigated in the present study. Radioligand binding experiments were performed in the absence and presence of diverse allosteric modulators on both wild-type (wt) and mutant (T277A) adenosine A1 receptors. Thermodynamic dat...

journal_title：British journal of pharmacology

authors： Heitman LH,Mulder-Krieger T,Spanjersberg RF,von Frijtag Drabbe Künzel JK,Dalpiaz A,IJzerman AP

更新日期：2006-03-01 00:00:00

abstract：:Pulmonary hypertension (PH) is a rare, progressive pulmonary vasculopathy characterized by increased mean pulmonary arterial pressure, pulmonary vascular remodelling and right ventricular failure. Current treatments are not curative, and new therapeutic strategies are urgently required. Clinical and preclinical eviden...

journal_title：British journal of pharmacology

authors： Scott TE,Kemp-Harper BK,Hobbs AJ

更新日期：2019-06-01 00:00:00

abstract：:1. Chronic inhibition of nitric oxide synthase (NOS) provokes a hypertensive state which has been shown to be angiotensin II (Ang-II) dependent. In addition to raising blood pressure, NOS inhibition also causes leukocyte adhesion. The present study was designed to define the role of Ang-II in hypertension and in the l...

journal_title：British journal of pharmacology

authors： Alvarez A,Piqueras L,Bello R,Canet A,Moreno L,Kubes P,Sanz MJ

更新日期：2001-02-01 00:00:00

abstract：:Mitochondrial permeability transition pore (mPTP) opening plays a critical role in cardiac reperfusion injury and its prevention is cardioprotective. Tumour cell mitochondria usually have high levels of hexokinase isoform 2 (HK2) bound to their outer mitochondrial membranes (OMM) and HK2 binding to heart mitochondria ...

journal_title：British journal of pharmacology

authors： Halestrap AP,Pereira GC,Pasdois P

更新日期：2015-04-01 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：:We investigated the action of the phenylalkylamines verapamil and N-methyl-verapamil on the Kv1.3 potassium channel using the whole-cell configuration of the patch-clamp technique. Our goal was to identify their binding as a prerequisite for using the phenylalkylamines as small, well-defined molecular probes, not only...

journal_title：British journal of pharmacology

authors： Rauer H,Grissmer S

更新日期：1999-07-01 00:00:00

abstract：:1. We have studied the mechanical response of circular strips of the guinea-pig ileum to tachykinins and characterized the receptors involved by means of receptor-selective agonists. 2. The strips responded to both substance P (SP) and neurokinin A (NKA), as well as to [Pro9]-SP sulphone (selective NK1-receptor agonis...

journal_title：British journal of pharmacology

authors： Maggi CA,Patacchini R,Giachetti A,Meli A

更新日期：1990-12-01 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：:1. The present study was designed to investigate tolerance to several pharmacological effects of apomorphine. 2. Changes in blood pressure, heart rate, plasma noradrenaline levels, rectal temperature, respiratory rate and retching plus vomiting were compared after administration of apomorphine (200 micrograms kg-1, i....

journal_title：British journal of pharmacology

authors： Montastruc JL,Llau ME,Senard JM,Tran MA,Rascol O,Montastruc P

更新日期：1996-03-01 00:00:00

abstract：:1. OPC-31260, a benzazepine derivative, has been studied for its ability to antagonize the binding of arginine vasopressin (AVP) to receptors in rat liver (V1) and kidney (V2) plasma membranes, for antagonism of the antidiuretic action of AVP in alcohol-anaesthetized rats and for diuretic action in conscious normal ra...

journal_title：British journal of pharmacology

authors： Yamamura Y,Ogawa H,Yamashita H,Chihara T,Miyamoto H,Nakamura S,Onogawa T,Yamashita T,Hosokawa T,Mori T

更新日期：1992-04-01 00:00:00

abstract：:1. Glycine responses were studied under voltage clamp in Xenopus oocytes injected with cDNA encoding mammalian glycine receptor subunits and in rat medullary neurones. Bath application of glycine gave strychnine-sensitive currents which reversed close to the expected equilibrium potentials for chloride ions. The peak ...

journal_title：British journal of pharmacology

authors： Downie DL,Hall AC,Lieb WR,Franks NP

更新日期：1996-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Although CB(1) receptor activation evokes neuroprotection in response to cannabinoids, some cannabinoids have been reported to be peroxisome proliferator activated receptor (PPAR) ligands, offering an alternative protective mechanism. We have, therefore, investigated the ability of a range of can...

journal_title：British journal of pharmacology

authors： Sun Y,Alexander SP,Garle MJ,Gibson CL,Hewitt K,Murphy SP,Kendall DA,Bennett AJ

更新日期：2007-11-01 00:00:00

abstract：:The complement system plays a major role in threat recognition and in orchestrating responses to microbial intruders and accumulating debris. This immune surveillance is largely driven by lectins that sense carbohydrate signatures on foreign, diseased and healthy host cells and act as complement activators, regulators...

journal_title：British journal of pharmacology

authors： Hevey R,Pouw RB,Harris C,Ricklin D

更新日期：2020-11-03 00:00:00

abstract：:1. Fluoxetine (Prozac) is widely used as an antidepressant drug and is assumed to be a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI). Claims that its beneficial psychotropic effects extend beyond those in treatment of depression have drawn clinical and popular attention to this compound, raising the q...

journal_title：British journal of pharmacology

authors： Tytgat J,Maertens C,Daenens P

更新日期：1997-12-01 00:00:00

abstract：:If one drug, B, antagonizes another, A, by producing the opposite physiological effect, the antagonist concentration-effect curves should be affected by the recording system, which limits the range of agonist responses. With pieces of isolated guinea-pig ileum taken from adjacent parts of the same animal, one recorded...

journal_title：British journal of pharmacology

authors： Barlow RB,Bond SM,Grant C,McQueen DS,Yaqoob Z

更新日期：2001-08-01 00:00:00

abstract：:Since December 2019 SARS-Cov-2 was found responsible for the disease COVID-19, which has spread worldwide. No specific therapies/vaccines are yet available for the treatment of COVID-19. Drug repositioning may offer a strategy and a number of drugs have been repurposed, including lopinavir/ritonavir, remdesivir, favip...

journal_title：British journal of pharmacology

authors： Scavone C,Brusco S,Bertini M,Sportiello L,Rafaniello C,Zoccoli A,Berrino L,Racagni G,Rossi F,Capuano A

更新日期：2020-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Biased GPCR ligands are able to engage with their target receptor in a manner that preferentially activates distinct downstream signalling and offers potential for next generation therapeutics. However, accurate quantification of ligand bias in vitro is complex, and current best practice is not a...

journal_title：British journal of pharmacology

authors： Winpenny D,Clark M,Cawkill D

更新日期：2016-04-01 00:00:00

abstract：:5-Lipoxygenase (5-LO) is a crucial enzyme in the synthesis of the bioactive leukotrienes (LTs) from arachidonic acid (AA), and inhibitors of 5-LO are thought to prevent the untowarded pathophysiological effects of LTs. In this study, we present the molecular pharmacological profile of the novel nonredox-type 5-LO inhi...

journal_title：British journal of pharmacology

authors： Fischer L,Steinhilber D,Werz O

更新日期：2004-07-01 00:00:00