Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.

abstract：BACKGROUND AND PURPOSE:To study the importance of endothelium-derived contracting factors (EDCFs) in arteries of rats with type I diabetes. EXPERIMENTAL APPROACH:Rat femoral arteries were collected four or twelve weeks after induction of diabetes with streptozotocin. Rings, with or without endothelium, were suspended ...

journal_title：British journal of pharmacology

authors： Shi Y,Feletou M,Ku DD,Man RY,Vanhoutte PM

更新日期：2007-03-01 00:00:00

abstract：:1 Inactivation of prostaglandin E2 in the pulmonary circulation of rabbits in vivo was measured by comparing the hypotensive effects of doses given intravenously and intra-arterially. 2 Di-4-phloretin phosphate (DPP) 25-100 mug kg-1 min-1 inhibited the inactivation of prostaglandin E2 in the pulmonary circulation. 3 T...

journal_title：British journal of pharmacology

authors： Crutchley DJ,Piper PJ

更新日期：1975-07-01 00:00:00

abstract：:1. The role of smooth muscle-derived lipoprotein lipase (LPL) that translocates to the endothelium surface on vascular dysfunction during atherogenesis is unclear. Thus, the role of vascular LPL on blood vessel reactivity was assessed in transgenic mice that specifically express human LPL in the circulatory system. 2....

journal_title：British journal of pharmacology

authors： Esenabhalu VE,Cerimagic M,Malli R,Osibow K,Levak-Frank S,Frieden M,Sattler W,Kostner GM,Zechner R,Graier WF

更新日期：2002-01-01 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：BACKGROUND AND PURPOSE:The electromechanical window (EMW), the interval between the end of the T-wave and the end of the left ventricular pressure (LVP) curve, has recently been proposed as a predictor of risk of Torsade de Pointes (TdP) in healthy animals, whereby a negative EMW (mechanical relaxation earlier than rep...

journal_title：British journal of pharmacology

authors： Stams TR,Bourgonje VJ,Beekman HD,Schoenmakers M,van der Nagel R,Oosterhoff P,van Opstal JM,Vos MA

更新日期：2014-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The thiazolidine carboxylic acid, BML-241, has been proposed as a lead compound in development of selective antagonists at the sphingosine-1-phosphate receptor (S1P3), based on its inhibition of the rise in intracellular calcium concentrations ([Ca2+]i) in HeLa cells overexpressing S1P receptors....

journal_title：British journal of pharmacology

authors： Jongsma M,Hendriks-Balk MC,Michel MC,Peters SL,Alewijnse AE

更新日期：2006-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The adenosine 2B (A2B) receptor is the predominant adenosine receptor expressed in the colon. Acting through the A2B receptor, adenosine mediates chloride secretion, as well as fibronectin and interleukin (IL)-6 synthesis and secretion in intestinal epithelial cells. A2B receptor mRNA and protein...

journal_title：British journal of pharmacology

authors： Kolachala V,Ruble B,Vijay-Kumar M,Wang L,Mwangi S,Figler H,Figler R,Srinivasan S,Gewirtz A,Linden J,Merlin D,Sitaraman S

更新日期：2008-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Angiotensin II (AngII) induces migration and growth of vascular smooth muscle cell (VSMC), which is responsible for vascular remodelling in some cardiovascular diseases. Ang II also activates a Cl(-) current, but the underlying mechanism is not clear. EXPERIMENTAL APPROACH:The A10 cell line and ...

journal_title：British journal of pharmacology

authors： Ma MM,Lin CX,Liu CZ,Gao M,Sun L,Tang YB,Zhou JG,Wang GL,Guan YY

更新日期：2016-02-01 00:00:00

abstract：:1. In order to assess the role of different ionic currents in hypoxia-induced action potential shortening, we investigated the effects of blockers of voltage-dependent and ATP-sensitive K(+)-channel on the membrane potential of hypoxic rabbit hearts and papillary muscles. The response to blocking of the inward rectifi...

journal_title：British journal of pharmacology

authors： Ruiz Petrich E,Leblanc N,deLorenzi F,Allard Y,Schanne OF

更新日期：1992-08-01 00:00:00

abstract：:1. We have investigated the cellular target of K(+) channel blockers responsible for the inhibition of the EDHF-mediated relaxation in the rat mesenteric artery by studying their effects on tension, smooth muscle cell (SMC) membrane potential and endothelial cell Ca(2+) signal ([Ca(2+)](endo)). 2. In arteries contract...

journal_title：British journal of pharmacology

authors： Ghisdal P,Morel N

更新日期：2001-11-01 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：BACKGROUND AND PURPOSE:The glucagon-like peptides GLP-1 and GLP-2 are secreted from enteroendocrine L-cells following nutrient ingestion. Drugs that increase activity of the GLP-1 axis are highly successful therapies for type 2 diabetes, and boosting L-cell secretion is a potential strategy for future diabetes treatmen...

journal_title：British journal of pharmacology

authors： Parker HE,Wallis K,le Roux CW,Wong KY,Reimann F,Gribble FM

更新日期：2012-01-01 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：:1 4-Aminopyridine methiodide (4-APMI), a quaternary analogue of aminopyridine (4-AP), was tested for neuromuscular facilitatory actions on the chick biventer cervicis and frog sartorius nerve-muscle preparations. 2 In the chick, 4-APMI (10(-4) to 10(-2) M) augmented indirectly elicited twitches and reversed tubocurari...

journal_title：British journal of pharmacology

authors： Horn AS,Lambert JJ,Marshall IG

更新日期：1979-01-01 00:00:00

abstract：:1. The effect of neuropeptide Y (NPY) on motor responses produced by activation of capsaicin-sensitive primary afferents in the guinea-pig isolated ileum was determined by use of capsaicin itself and electrical mesenteric nerve stimulation as stimuli. 2. NPY inhibited or suppressed the cholinergic contractile response...

journal_title：British journal of pharmacology

authors： Takaki M,Nakayama S

更新日期：1991-06-01 00:00:00

abstract：:1. The pharmacological characteristics of RP 67580, a non-peptide tachykinin NK1 receptor antagonist, and its effects on a reflex response evoked by stimulation of primary afferent fibres, were examined in isolated neonatal spinal cord preparations of the rat. Potentials were recorded extracellularly from a lumbar ven...

journal_title：British journal of pharmacology

authors： Hosoki R,Yanagisawa M,Guo JZ,Yoshioka K,Maehara T,Otsuka M

更新日期：1994-12-01 00:00:00

abstract：:It has been proposed that the vagus nerve plays a role in mediating cholecystokinin-8 (CCK-8) effect on such gastric functions as motility, emptying and gastric acid secretion. To examine the contribution of the efferent pathways in realizing these effects, efferent mass activity in the ventral gastric vagal nerve in ...

journal_title：British journal of pharmacology

authors： Bucinskaite V,Kurosawa M,Lundeberg T

更新日期：2000-04-01 00:00:00

abstract：:Human skin fibroblasts incubated with arachidonic acid in culture show basal release of prostaglandins. They produce the same prostaglandins after stimulation with bradykinin. Basal release of prostaglandins I2 (6-oxo-PGF1 alpha), F2 alpha and E2 is inhibited dose-dependently by both acetylsalicylic acid (ASA) and dip...

journal_title：British journal of pharmacology

authors： Lüthy C,Multhaupt M,Oetliker O,Perisic M

更新日期：1983-08-01 00:00:00

abstract：:The mechanism of the long duration of action of salmeterol at beta(2)-adrenoceptors has long been a matter of debate, and is still unresolved. Szczuka and colleagues have both summarized the position to date and suggested a new mechanistic contender, receptor rebinding. Despite this, they still do not come to any clea...

journal_title：British journal of pharmacology

authors： Coleman RA

更新日期：2009-09-01 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：:1. We previously showed that chronic exposure to aspirin (100 mg kg-1 daily, by mouth) is effective in preventing the onset of hypertension in young (28-84 day old) spontaneously hypertensive rats (SHRs). This is contrary to what others have reported using older SHRs. 2. Renal prostaglandin F2 alpha was also reduced i...

journal_title：British journal of pharmacology

authors： Tuttle RS,Yager J,Northrup N

更新日期：1988-07-01 00:00:00

abstract：:1. The effect of a standardized mixture of beta-hydroxyethyl rutosides against oxidative damage in singlet oxygen-challenged isolated cardiac myocytes from adult rats was investigated. The morphology of the myocytes was evaluated as an indicator for cell viability (elongated, rod shaped cells vs. hypercontracted, roun...

journal_title：British journal of pharmacology

authors： Olbrich HG,Grabisch P,Grossmann A,Rinne T,Klepzig H,Mutschler E

更新日期：1996-10-01 00:00:00

abstract：:1 Hypothalamic blood flow (HBF) was measured in conscious rabbits by the 133xenon washout technique. 2 Substance P in a dose of 50 or 500 ng increases HBF while 5 ng is without effect. 3 Cholinoceptor blockade, with either atropine or mecamylamine abolishes the vasodilator effect of substance P. 4 Chemical sympathecto...

journal_title：British journal of pharmacology

authors： Klugman KP,Lembeck F,Markowitz S,Mitchell G,Rosendorff C

更新日期：1980-01-01 00:00:00

abstract：:1. In decerebrated, non-spinalized rabbits, intrathecal administration of either of the selective 5-HT1A-receptor antagonists (S)WAY-100135 or WAY-100635 resulted in dose-dependent enhancement of the reflex responses of gastrocnemius motoneurones evoked by electrical stimulation of all myelinated afferents of the sura...

journal_title：British journal of pharmacology

authors： Clarke RW,Harris J,Houghton AK

更新日期：1996-11-01 00:00:00

abstract：:1. In isolated Langendorff-perfused, electrically-paced, hearts of guinea-pigs, global low-flow-ischaemia (LFI; at 0.7 ml min-1) resulted in marked increases in the rates of release of lactate, lactate dehydrogenase (LDH) and creatine kinase (CK) over a 30 min period. At the end of the LFI period, tissue ATP content w...

journal_title：British journal of pharmacology

authors： Clarke B,Spedding M,Patmore L,McCormack JG

更新日期：1993-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Due to their potent bronchodilator properties, beta(2)-adrenoceptor agonists are a mainstay of therapy in asthma. However, the effects of beta(2)-adrenoceptor agonists on inflammation are less clear. Accordingly, we have investigated the effects of beta(2)-adrenoceptor agonists on inflammatory me...

journal_title：British journal of pharmacology

authors： Holden NS,Rider CF,Bell MJ,Velayudhan J,King EM,Kaur M,Salmon M,Giembycz MA,Newton R

更新日期：2010-05-01 00:00:00

abstract：:1. We measured the effects of agonists and antagonists of metabotropic glutamate (mGlu) receptors (types 1 and 5) on NMDA-induced depolarization of mouse cortical wedges in order to characterize the mGlu receptor type responsible for modulating NMDA responses. We also characterized a number of mGlu receptor agents by ...

journal_title：British journal of pharmacology

authors： Attucci S,Carlà V,Mannaioni G,Moroni F

更新日期：2001-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:A fluorinated derivative (2F-MT-45) of the synthetic μ-opioid receptor agonist MT-45 (1-cyclohexyl-4-(1,2-diphenylethyl)piperazine) was recently identified in a seized illicit tablet. While MT-45 is a Class A drug, banned in a number of countries, nothing is known about the pharmacology of 2F-MT-...

journal_title：British journal of pharmacology

authors： Baptista-Hon DT,Smith M,Singleton S,Antonides LH,Nic Daeid N,McKenzie C,Hales TG

更新日期：2020-08-01 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. We investigated the hypothesis that, as in some other large human arteries, 5-HT-induced contraction of the temporal artery is mediated through two co-existing receptor populations, 5-HT1-like- and 5-HT2A. Temporal arterial segments were obtained from patients undergoing brain surgery and rings prepared set up to c...

journal_title：British journal of pharmacology

authors： Verheggen R,Freudenthaler S,Meyer-Dulheuer F,Kaumann AJ

更新日期：1996-01-01 00:00:00