Screening for liver X receptor modulators: Where are we and for what use?

abstract：:The effect of bath-applied luteinizing hormone-releasing factor (LHRF) was recorded in voltage-clamped bullfrog lumbar sympathetic neurones. At a holding potential of -- 30 mV, LHRF induced a steady inward (depolarizing) current and reduced membrane conductance; at -- 60 mV LHRF produced negligible inward current and ...

journal_title：British journal of pharmacology

authors： Adams PR,Brown DA

更新日期：1980-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Thromboxane A(2) and endothelial dysfunction are implicated in the development of pulmonary hypertension. The receptor-transduction pathway for U46619 (9,11-dideoxy-9 alpha, 11 alpha-methanoepoxy prostaglandin F(2 alpha))-induced contraction was examined in endothelium-intact (E+) and denuded (E-...

journal_title：British journal of pharmacology

authors： McKenzie C,MacDonald A,Shaw AM

更新日期：2009-06-01 00:00:00

abstract：:1. During the past few years it has been shown that the sympatholytic effect resulting from localized microinjection of clonidine and other imidazolines into the rostral ventrolateral medulla (RVL) results from activation of 'imidazoline' receptors (I1 receptors) rather than from an alpha 2-adrenoceptor-mediated effec...

journal_title：British journal of pharmacology

authors： Hieble JP,Kolpak DC

更新日期：1993-12-01 00:00:00

abstract：:1. The effects of nipradilol, a beta-adrenoceptor antagonist which possesses a nitroxy group, on cytosolic Ca2+ concentration ([Ca2+]i), and on tension development were simultaneously measured by front-surface fluorometry and fura-2-loaded strips in the proximal portion of pig coronary arteries. 2. Nipradilol reduced ...

journal_title：British journal of pharmacology

authors： Abe S,Nakamura M,Kanaide H

更新日期：1996-04-01 00:00:00

abstract：:1 The role of histamine H1- and H2-receptors in mediating the cutaneous inflammatory response produced by exogenous histamine and the release of endogenous histamine from mast cells has been investigated by a method which permits simultaneous, quantitative measurement of vasodilatation, vascular permeability and oedem...

journal_title：British journal of pharmacology

authors： Owen DA,Poy E,Woodward DF,Daniel D

更新日期：1980-08-01 00:00:00

abstract：:1. TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin. It belongs to the transient receptor potential (TRP) family, and therefore is related to vanilloid receptor type-1 (VR1, TRPV1). We tested whether substances which are structurally related to ment...

journal_title：British journal of pharmacology

authors： Behrendt HJ,Germann T,Gillen C,Hatt H,Jostock R

更新日期：2004-02-01 00:00:00

abstract：:1. A new series of cardiotonics based on five steroid nuclei has been evaluated for inhibition of Na-+/K-+-ATPase and Rb uptake by red blood cells, and for inotropic activity and toxicity in dogs. Structure-activity relationships are discussed. 2. The in vitro tests can be used satisfactorily to predict inotropic acti...

journal_title：British journal of pharmacology

authors： Beard NA,Rouse W,Somerville AR

更新日期：1975-05-01 00:00:00

abstract：:1 Cumulative concentration-response relationships for the chronotropic effects of histamine, oxymetazoline, clonidine and thirteen clonidine-like imidazolidine derivatives were examined in isolated spontaneously beating guinea-pig atria.2 The following compounds induced positive chronotropic effects: histamine, clonid...

journal_title：British journal of pharmacology

authors： McCulloch MW,Medgett IC,Rand MJ,Story DF

更新日期：1980-07-01 00:00:00

abstract：:The binding characteristics of the relaxin receptor in rat atria, uterus and cortex were studied using a [33P]-labelled human gene 2 relaxin (B33) and quantitative receptor autoradiography. The binding kinetics of [33P]-human gene 2 relaxin (B33) were investigated in slide-mounted rat atrial sections. The binding achi...

journal_title：British journal of pharmacology

authors： Tan YY,Wade JD,Tregear GW,Summers RJ

更新日期：1999-05-01 00:00:00

abstract：:1 The N6-2-O-dibutyryl derivative of adenosine 3',5'-monophosphate (db cyclic AMP) has been micro-injected into the third cerebral ventricle of the unanaesthetized, restrained mouse and the effects on body temperature and thermoregulatory activities observed. 2 Db cyclic AMP (4, 16 and 32 micrograms) injected intracer...

journal_title：British journal of pharmacology

authors： Dascombe MJ,Milton AS,Nyemitei-Addo I,Pertwee RG

更新日期：1980-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Tolerance induced by morphine and other opiates remains a major unresolved problem in the clinical management of pain. There is now good evidence for the importance of MAPKs in morphine-induced antinociceptive tolerance. A member of the MAPK kinase kinase family, TGF-β activated kinase 1 (TAK1) i...

journal_title：British journal of pharmacology

authors： Xu H,Xu T,Ma X,Jiang W

更新日期：2015-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:An ever-growing wealth of information on current drugs and their pharmacological effects is available from online databases. As our understanding of systems biology increases, we have the opportunity to predict, model and quantify how drug combinations can be introduced that outperform convention...

journal_title：British journal of pharmacology

authors： Benson HE,Watterson S,Sharman JL,Mpamhanga CP,Parton A,Southan C,Harmar AJ,Ghazal P

更新日期：2017-12-01 00:00:00

abstract：:Class A1 scavenger receptors (SR-A1) are membrane glycoproteins that can form homotrimers. This receptor was originally defined by its ability to mediate the accumulation of lipids in macrophages. Subsequent studies reveal that SR-A1 plays critical roles in innate immunity, cell apoptosis and proliferation. This revie...

journal_title：British journal of pharmacology

authors： Ben J,Zhu X,Zhang H,Chen Q

更新日期：2015-12-01 00:00:00

abstract：:1. The sinus node inhibitors UL FS 49 and DK-AH 269 reduce heart rate by slowing diastolic depolarization rate in the sino-atrial (SA) node, which might originate from the use-dependent blockade of a hyperpolarization-activated current If. A hyperpolarization-activated current Ih, which is present in many types of neu...

journal_title：British journal of pharmacology

authors： Raes A,Van de Vijver G,Goethals M,van Bogaert PP

更新日期：1998-10-01 00:00:00

abstract：:1. The role of vasoconstrictor 5-HT1-like receptors in the control of vascular reactivity in vivo has been relatively little studied, particularly with regards to venous function. Using an anaesthetized dog model, we have investigated the haemodynamic profile of the selective 5-HT1-like agonist, sumatriptan, focussing...

journal_title：British journal of pharmacology

authors： Drieu la Rochelle C,O'Connor SE

更新日期：1995-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The histamine H4 receptor is widely expressed in cells of immune origin and has been shown to play a role in a variety of inflammatory processes mediated by histamine. In this report, we describe the in vitro and in vivo anti-inflammatory properties of a potent histamine H4 receptor antagonist, A...

journal_title：British journal of pharmacology

authors： Strakhova MI,Cuff CA,Manelli AM,Carr TL,Witte DG,Baranowski JL,Vortherms TA,Miller TR,Rundell L,McPherson MJ,Adair RM,Brito AA,Bettencourt BM,Yao BB,Wetter JM,Marsh KC,Liu H,Cowart MD,Brioni JD,Esbenshade TA

更新日期：2009-05-01 00:00:00

abstract：:1. The effects of suramin on an adenosine 5'-triphosphate (ATP)-activated inward current were investigated in PC12 phaeochromocytoma cells with whole-cell voltage-clamp techniques. 2. Suramin (30 to 300 microM) inhibited the ATP-activated current in a dose-dependent manner. The inhibitory effects were reversible and c...

journal_title：British journal of pharmacology

authors： Nakazawa K,Fujimori K,Takanaka A,Inoue K

更新日期：1990-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Diabetes is a risk factor for the development of coronary artery disease but it is not known whether the functions of endothelium-derived nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) in coronary arteries are altered in the early stage of diabetes. Such alterations and t...

journal_title：British journal of pharmacology

authors： Kajikuri J,Watanabe Y,Ito Y,Ito R,Yamamoto T,Itoh T

更新日期：2009-09-01 00:00:00

abstract：:1. The effects of some chloride channel antagonists were studied on the calcium-activated chloride current (ICl(Ca)) in smooth muscle cells from the rabbit portal vein with the perforated patch technique. 2. 4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulphonic acid (SITS) and 4,4'-diisothiocyanato-stilbene-2,2'-disu...

journal_title：British journal of pharmacology

authors： Hogg RC,Wang Q,Large WA

更新日期：1994-04-01 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 iodine-containing contrast medium iopanoic acid induces alterations of thyroid hormone metabolism comparable to those observed with the iodine-containing antiarrhythmic drug amiodarone. Both compounds inhibit the intracellular conversion of thyroxine (T4) to triiodothyronine (T3). Using iopanoic acid, the question...

journal_title：British journal of pharmacology

authors： Stäubli M,Studer H

更新日期：1986-06-01 00:00:00

abstract：:Inhalation of cyclopropane in dogs, by the closed circuit method, for a fixed period, produced an emetic response during recovery from anaesthesia. Bilateral surgical ablation of the emetic chemoreceptor trigger zone of the area postrema rendered the dogs refractory to several times (3-6) the threshold emetic dose of ...

journal_title：British journal of pharmacology

authors： Badola RP,Bhargava KP,Dixit KS,Ratra CK

更新日期：1971-09-01 00:00:00

abstract：:1 Both phasic and tonic responses to KCl 160 mM were reduced by Ca2+ deprivation. After 90 min, the phasic response was abolished but 13 +/- 1.5% of the tonic response remained. This resistant component was still present if the Ca2+-free solution contained EGTA 0.1 mM. The tonic response was more resistant to deprivat...

journal_title：British journal of pharmacology

authors： Hay DW,Wadsworth RM

更新日期：1982-05-01 00:00:00

abstract：:(1) UNC-49B and UNC-49C are gamma-aminobutyric acid (GABA) receptor subunits encoded by the Caenorhabditis elegans unc-49 gene. UNC-49B forms a homomeric GABA receptor, or can co-assemble with UNC-49C to form a heteromeric receptor. The pharmacological properties of UNC-49B homomers and UNC-49B/C heteromers were inves...

journal_title：British journal of pharmacology

authors： Bamber BA,Twyman RE,Jorgensen EM

更新日期：2003-03-01 00:00:00

abstract：:The Secretin family of GPCRs are endocrine peptide hormone receptors that share a common genomic organization and are the subject of a wide variety of alternative splicing. All GPCRs contain a central seven transmembrane domain responsible for transducing signals from the outside of the cell as well as extracellular a...

journal_title：British journal of pharmacology

authors： Furness SG,Wootten D,Christopoulos A,Sexton PM

更新日期：2012-05-01 00:00:00

abstract：:1. The present study shows the effects of imipramine in a single dose (10 mg kg(-1), p.o.) or following repeated (14 days, twice a day) treatment on the level of mRNA coding for D2 dopamine receptors in the rat caudate putamen (CP). Repeated administration of imipramine resulted in the increase of the level of mRNA co...

journal_title：British journal of pharmacology

authors： Dziedzicka-Wasylewska M,Rogoz R

更新日期：1998-03-01 00:00:00

abstract：:1. Leukotriene B(4) (LTB(4)) stimulation of guinea-pig peritoneal eosinophils, induced a biphasic activation of the NADPH oxidase composed of a rapid (<3 min) phase mediated by non-adherent cells and a sustained (3 - 120 min) phase mediated by CD11b/CD18 adherent eosinophils. Studies were undertaken to compare the int...

journal_title：British journal of pharmacology

authors： Lynch OT,Giembycz MA,Barnes PJ,Lindsay MA

更新日期：2001-10-01 00:00:00

abstract：:1. LP-805, 8-tert-butyl-6,7-dihydropyrrolo-[3,2-e]-5-methylpyrazolo- [1,5a]-pyrimidine-3-carbonitrile, is a newly synthesized potent vasodilator. To investigate the cellular mechanisms of vasorelaxation induced by LP-805, we simultaneously determined the effects of LP-805 on cytosolic Ca2+ concentrations ([Ca2+]i) and...

journal_title：British journal of pharmacology

authors： Ushio-Fukai M,Hirano K,Kanaide H

更新日期：1994-12-01 00:00:00

abstract：:1. The potassium-sparing diuretic, amiloride, has been shown to inhibit the Na/Ca exchange system in various preparations. The effects of this drug have been investigated on the contractions of guinea-pig aortic strips elicited by reduction of external K, by addition of ouabain and by removal of external Na. 2. Amilor...

journal_title：British journal of pharmacology

authors： Bova S,Cargnelli G,Luciani S

更新日期：1988-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:5-Hydroxytryptamine (5-HT) has been shown to control and modulate many physiological and behavioural functions in insects. In this study, we report the cloning and pharmacological properties of a 5-HT(1) receptor of an insect model for neurobiology, physiology and pharmacology. EXPERIMENTAL APPR...

journal_title：British journal of pharmacology

authors： Troppmann B,Balfanz S,Baumann A,Blenau W

更新日期：2010-04-01 00:00:00