An EP receptor with a novel pharmacological profile in the T-cell line Jurkat.

Abstract:

:1. Comparison of the rank order of potency of the natural prostanoids prostaglandin E2 (PGE2), PGD2, PGF2 alpha and carbaprostacyclin in stimulating cyclic AMP in Jurkat cells is consistent with the presence of an EP receptor. 2. Lack of responsiveness to the EP1/EP3 selective agonist, sulprostone, and the EP2 agonists, butaprost and AH 13205, indicates that this receptor is not of the EP1, EP2 or EP3 subtypes. 3. Inhibition of PGE2-stimulated cyclic AMP by the EP4 antagonist, AH 23848 is non-competitive, unlike the competitive antagonism reported in the pig saphenous vein EP4 preparation. Furthermore, 16,16-dimethyl PGE2 is 100 fold less potent than PGE2 in Jurkat cells, while these agonists are equipotent in the rabbit jugular vein purported EP4 preparation. In addition, 1-OH PGE1, which also is active in the rabbit jugular vein preparation, is inactive in Jurkat cells at concentrations up to 1 x 10(-4) M. These data are not wholly consistent with any adenylate cyclase coupled EP receptor described to date. 4. It is postulated that an EP receptor, positively coupled to adenylate cyclase, with a unique pharmacological profile is present in Jurkat cells.

journal_name

Br J Pharmacol

authors

De Vries GW,Guarino P,McLaughlin A,Chen J,Andrews S,Woodward DF

doi

10.1111/j.1476-5381.1995.tb15030.x

subject

Has Abstract

pub_date

1995-08-01 00:00:00

pages

1231-4

issue

7

eissn

0007-1188

issn

1476-5381

journal_volume

115

pub_type

杂志文章
  • Interactions between angiotensin II, sympathetic nerve-mediated pressor response and cyclo-oxygenase products in the pithed rat.

    abstract::1. The influence of angiotensin II (AII) on resting blood pressure and on sympathetic nerve-mediated pressor responses in the pithed rat was investigated either by inhibiting the renin-angiotensin system or by infusing AII. 2. Plasma AII levels in the pithed rat were approximately 20 fold higher than in normotensive r...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1988.tb11759.x

    authors: Grant TL,McGrath JC

    更新日期:1988-12-01 00:00:00

  • Potentiation by nitric oxide of the ATP-sensitive K+ current induced by K+ channel openers in guinea-pig ventricular cells.

    abstract::1. Modulation by nitric oxide (NO) of the ATP-sensitive K+ channel (KATP) current (IK(ATP)) was investigated in single ventricular cells dissociated from guinea-pig hearts. IK(ATP) was induced by 5-amino-N-[2-(2-chlorophenyl)ethyl]-N'-cyano-3-pyridinecarboxamidine+ ++ (KRN4884) and cromakalim. 2. In the whole-cell pat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701069

    authors: Shinbo A,Iijima T

    更新日期:1997-04-01 00:00:00

  • Effective suppression of pro-inflammatory molecules by DHCA via IKK-NF-κB pathway, in vitro and in vivo.

    abstract:BACKGROUND AND PURPOSE:Dehydrodiconiferyl alcohol (DHCA), a lignan compound isolated from Cucurbita moschata, has previously been shown to contain anti-adipogenic and antilipogenic effects on 3T3-L1 cells and mouse embryonic fibroblasts. As some of phytochemicals derived from natural plants show anti-inflammatory or an...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13137

    authors: Lee J,Choi J,Kim S

    更新日期:2015-07-01 00:00:00

  • Cholinoceptor regulation of cyclic AMP levels in bovine adrenal medullary cells.

    abstract::1. The regulation of adenosine 3':5'-cyclic monophosphate (cyclic AMP) levels by cholinoceptors has been studied in cultured bovine adrenal medullary cells. 2. Acetylcholine (100 microM), nicotine (10 microM) and dimethylphenylpiperazinium (20 microM) each increased cellular cyclic AMP levels 2 to 4 fold over 5 min in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1992.tb14341.x

    authors: Anderson K,Robinson PJ,Marley PD

    更新日期:1992-06-01 00:00:00

  • Antipsoriatic effects of avarol-3'-thiosalicylate are mediated by inhibition of TNF-alpha generation and NF-kappaB activation in mouse skin.

    abstract:BACKGROUND AND PURPOSE:Avarol is a marine sesquiterpenoid hydroquinone with anti-inflammatory and antipsoriatic properties. The aim of this study was to evaluate the in vitro and in vivo pharmacological behaviour of the derivative avarol-3'-thiosalicylate (TA) on some inflammatory parameters related to the pathogenesis...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707394

    authors: Amigó M,Payá M,De Rosa S,Terencio MC

    更新日期:2007-10-01 00:00:00

  • Atomoxetine acts as an NMDA receptor blocker in clinically relevant concentrations.

    abstract:BACKGROUND AND PURPOSE:There is increasing evidence that not only the monoaminergic but also the glutamatergic system is involved in the pathophysiology of attention-deficit hyperactivity disorder (ADHD). Hyperactivity of glutamate metabolism might be causally related to a hypoactive state in the dopaminergic system. A...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2010.00707.x

    authors: Ludolph AG,Udvardi PT,Schaz U,Henes C,Adolph O,Weigt HU,Fegert JM,Boeckers TM,Föhr KJ

    更新日期:2010-05-01 00:00:00

  • Brain serotoninergic nervous system is involved in bombesin-induced frequent urination through brain 5-HT7 receptors in rats.

    abstract:BACKGROUND AND PURPOSE:Psychological stress exacerbates symptoms of urinary bladder dysfunction; however, the underlying brain mechanisms are unclear. We have demonstrated that centrally administered bombesin, a stress-related neuropeptide, facilitates the rat micturition reflex. Brain bombesin-like peptides modulate t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13941

    authors: Shimizu T,Shimizu S,Wada N,Takai S,Shimizu N,Higashi Y,Kadekawa K,Majima T,Saito M,Yoshimura N

    更新日期:2017-09-01 00:00:00

  • Pharmacology of nociceptin and its receptor: a novel therapeutic target.

    abstract::Nociceptin (NC), alias Orphanin FQ, has been recently identified as the endogenous ligand of the opioid receptor-like 1 receptor (OP(4)). This new NC/OP(4) receptor system belongs to the opioid family and has been characterized pharmacologically with functional and binding assays on native (mouse, rat, guinea-pig) and...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1038/sj.bjp.0703219

    authors: Calo' G,Guerrini R,Rizzi A,Salvadori S,Regoli D

    更新日期:2000-04-01 00:00:00

  • Inhibition of inositol 1,4,5-trisphosphate formation by cyclic GMP in cultured aortic endothelial cells of the pig.

    abstract::1. In cultured endothelial cells of the pig the endothelium-derived relaxing factor (EDRF) releasing agent thrombin (2 u ml-1) caused a significant increase in basal levels of both guanosine 3':5'-cyclic monophosphate (cyclic GMP) and inositol 1,4,5-trisphosphate (IP3). This increase was time dependent, with peak leve...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12166.x

    authors: Lang D,Lewis MJ

    更新日期:1991-01-01 00:00:00

  • Pharmacological characterization of nicotine-induced acetylcholine release in the rat hippocampus in vivo: evidence for a permissive dopamine synapse.

    abstract::In this study, the mechanism of nicotine-induced hippocampal acetylcholine (ACh) release in awake, freely moving rats was examined using in vivo microdialysis. Systemic administration of nicotine (0.4 mg kg(-1), s.c.) increased the levels of ACh in hippocampal dialysates. The nicotine-induced hippocampal ACh release w...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702683

    authors: Reid RT,Lloyd GK,Rao TS

    更新日期:1999-07-01 00:00:00

  • Effect of 781094, a new selective alpha-adrenoceptor antagonist, on the aggregatory responses of human blood platelets and on binding of [3H]-dihydroergocryptine to these cells.

    abstract::781094 (2-(2(1, 4-benzodioxanyl))-2-imidazoline hydrochloride) is a potent competitive inhibitor of the aggregatory responses of human platelets induced by adrenaline (pA2 = 7.3) and UK-14304. 781094 is a more potent inhibitor of the pro-aggregatory response to clonidine than of that to methoxamine. The alpha 2/alpha ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1983.tb11012.x

    authors: Kerry R,Scrutton MC

    更新日期:1983-06-01 00:00:00

  • Inhibition of [3H]-(+)-MK 801 binding to rat brain sections by CPP and 7-chlorokynurenic acid: an autoradiographic analysis.

    abstract::1. The regional binding of [3H]-(+)-5-methyl-10,11-dihydro-5H-dibenzo (a,d)cyclohepten-5,10-imine maleate ([3H]-(+)-MK 801) to sections of rat brain was measured by an in vitro quantitative autoradiographic technique. A heterogeneous distribution of binding sites was observed. 2. High values of binding were detected i...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb12845.x

    authors: Tacconi S,Ratti E,Marien MR,Gaviraghi G,Bowery NG

    更新日期:1993-03-01 00:00:00

  • Effect of oral administration of zanapezil (TAK-147) for 21 days on acetylcholine and monoamines levels in the ventral hippocampus of freely moving rats.

    abstract::Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment. In this study, the effects of TAK-147 at 2 mg kg(-1) p.o. for 21 days, compared t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0706288

    authors: Hatip-Al-Khatib I,Iwasaki K,Yoshimitsu Y,Arai T,Egashira N,Mishima K,Ikeda T,Fujiwara M

    更新日期:2005-08-01 00:00:00

  • Sedative activity of cannabis in relation to its delta'-trans-tetrahydrocannabinol and cannabidiol content.

    abstract::1. The oral sedative potencies of cannabis herb, crude ethanolic and petroleum-ether fractions, were assayed against delta'-trans-tetrahydrocannabinol (THC) administered orally to mice, by measuring spontaneous motor activity over 30 min periods, at selected times, up to 6 h. 2. The THC contents of the extracts were d...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1981.tb09145.x

    authors: Pickens JT

    更新日期:1981-04-01 00:00:00

  • Necessity of divalent cations for recovery from carbachol-induced nicotinic acetylcholine receptor inactivation at snake twitch fibre endplates.

    abstract::1. Previous studies demonstrated that elevation of the extracellular calcium concentration during a prolonged exposure to a high concentration of carbachol reverses the staurosporine-induced decrease in the extent of endplate resensitization in voltage-clamped snake twitch fibres. The present studies were designed to ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13896.x

    authors: Hardwick JC,Parsons RL

    更新日期:1993-10-01 00:00:00

  • Histamine H1-receptor-mediated inositol phospholipid hydrolysis in DDT1MF-2 cells: agonist and antagonist properties.

    abstract::1. The effect of histamine H1-receptor stimulation on inositol phospholipid hydrolysis has been investigated in the hamster vas deferens smooth muscle cell line, DDT1MF-2. 2. Histamine (EC50 = 27 microM) stimulated the accumulation of [3H]-inositol phosphates in DDT1MF-2 cells prelabelled with [3H]-myo-inositol. 2-Thi...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13462.x

    authors: White TE,Dickenson JM,Hill SJ

    更新日期:1993-01-01 00:00:00

  • Can non-clinical repolarization assays predict the results of clinical thorough QT studies? Results from a research consortium.

    abstract:BACKGROUND AND PURPOSE:Translation of non-clinical markers of delayed ventricular repolarization to clinical prolongation of the QT interval corrected for heart rate (QTc) (a biomarker for torsades de pointes proarrhythmia) remains an issue in drug discovery and regulatory evaluations. We retrospectively analysed 150 d...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14101

    authors: Park E,Gintant GA,Bi D,Kozeli D,Pettit SD,Pierson JB,Skinner M,Willard J,Wisialowski T,Koerner J,Valentin JP

    更新日期:2018-02-01 00:00:00

  • Characterization of nociceptin hyperalgesia and allodynia in conscious mice.

    abstract::1. Intrathecal (i.t.) administration of nociceptin and high doses of morphine induced allodynia in response to innocuous tactile stimuli, and i.t. nociceptin evoked hyperalgesia in response to noxious thermal stimuli in conscious mice. Here we have characterized the nociceptin-induced allodynia and compared it with th...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701146

    authors: Hara N,Minami T,Okuda-Ashitaka E,Sugimoto T,Sakai M,Onaka M,Mori H,Imanishi T,Shingu K,Ito S

    更新日期:1997-06-01 00:00:00

  • Dualistic actions of cromakalim and new potent 2H-1,4-benzoxazine derivatives on the native skeletal muscle K ATP channel.

    abstract::1 New 2H-1,4-benzoxazine derivatives were synthesized and tested for their agonist properties on the ATP-sensitive K(+) channels (K(ATP)) of native rat skeletal muscle fibres by using the patch-clamp technique. The novel modifications involved the introduction at position 2 of the benzoxazine ring of alkyl substituent...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705233

    authors: Tricarico D,Barbieri M,Antonio L,Tortorella P,Loiodice F,Camerino DC

    更新日期:2003-05-01 00:00:00

  • The antiarrhythmic compound efsevin directly modulates voltage-dependent anion channel 2 by binding to its inner wall and enhancing mitochondrial Ca2+ uptake.

    abstract:BACKGROUND AND PURPOSE:The synthetic compound efsevin was recently identified to suppress arrhythmogenesis in models of cardiac arrhythmia, making it a promising candidate for antiarrhythmic therapy. Its activity was shown to be dependent on the voltage-dependent anion channel 2 (VDAC2) in the outer mitochondrial membr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.15022

    authors: Wilting F,Kopp R,Gurnev PA,Schedel A,Dupper NJ,Kwon O,Nicke A,Gudermann T,Schredelseker J

    更新日期:2020-07-01 00:00:00

  • Hypoxia modulates the activity of a series of clinically approved tyrosine kinase inhibitors.

    abstract:BACKGROUND AND PURPOSE:Hypoxia in tumours is known to cause resistance to conventional chemotherapeutic drugs. In contrast, little is known about the effects of hypoxia on targeted anti-cancer drugs. This study evaluated the effect of hypoxia on a series of clinically approved tyrosine kinase inhibitors (TKIs). EXPERI...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12438

    authors: Ahmadi M,Ahmadihosseini Z,Allison SJ,Begum S,Rockley K,Sadiq M,Chintamaneni S,Lokwani R,Hughes N,Phillips RM

    更新日期:2014-01-01 00:00:00

  • Adrenal origin of plasma catecholamines after decapitation: a study in normal and diabetic rats.

    abstract::The concentrations of catecholamines and the activities of dopamine-beta-hydroxylase were measured in blood obtained from decapitated diabetic and aged-matched control rats. The activity of dopamine-beta-hydroxylase in blood from diabetic rats was much greater (5 fold) than that seen for control rats. For both diabeti...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1978.tb08632.x

    authors: Berkowitz BA,Head RJ

    更新日期:1978-09-01 00:00:00

  • Salmeterol, a novel, long-acting beta 2-adrenoceptor agonist: characterization of pharmacological activity in vitro and in vivo.

    abstract::1. Salmeterol, a novel, long-acting beta-adrenoceptor agonist, has been compared with isoprenaline and salbutamol for activity in vitro on a range of beta-adrenoceptor containing preparations from laboratory animals and man, and in vivo for bronchodilator activity in the conscious guinea-pig. 2. Salmeterol, like isopr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12486.x

    authors: Ball DI,Brittain RT,Coleman RA,Denyer LH,Jack D,Johnson M,Lunts LH,Nials AT,Sheldrick KE,Skidmore IF

    更新日期:1991-11-01 00:00:00

  • Mechanisms of the protective effects of urocortin on coronary endothelial function during ischemia-reperfusion in rat isolated hearts.

    abstract::1 Urocortin is a vasodilator peptide related to corticotrophin-releasing factor, which may protect endothelial function during coronary ischemia-reperfusion (I-R). The aim of this study was to study the mechanisms of this protective effect. 2 Hearts from Sprague-Dawley rats were isolated and perfused at constant flow ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0706208

    authors: García-Villalón AL,Amezquita YM,Monge L,Fernández N,Climent B,Sánchez A,Diéguez G

    更新日期:2005-06-01 00:00:00

  • Prevention of arterial stiffening by pyridoxamine in diabetes is associated with inhibition of the pathogenic glycation on aortic collagen.

    abstract:BACKGROUND AND PURPOSE:Our team previously demonstrated that diabetes induces a deterioration in vascular dynamics, in parallel with the enhanced formation of advanced glycation end products. The aim of this study was to determine whether prevention of the arterial stiffening by pyridoxamine in diabetes is associated w...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00309.x

    authors: Chang KC,Liang JT,Tsai PS,Wu MS,Hsu KL

    更新日期:2009-08-01 00:00:00

  • Characteristic changes in coronary artery at the early hyperglycaemic stage in a rat type 2 diabetes model and the effects of pravastatin.

    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

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00348.x

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

    更新日期:2009-09-01 00:00:00

  • The effect of p-chloromercuribenzoate on structure-binding relationships of muscarinic receptors in the rat cerebral cortex.

    abstract::Muscarinic receptors in the rat cerebral cortex, reacted with p-chloromercuribenzoate (PCMB) under different conditions (Phase I and II), have modified binding sites. These exhibit remarkable changes in the structural dependence of the binding of drugs. In Phase I, the structure-binding profile of agonists for both th...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1983.tb11066.x

    authors: Birdsall NJ,Burgen AS,Hulme EC,Wong EH

    更新日期:1983-09-01 00:00:00

  • Effects of K+ channel blockers on the action potential of hypoxic rabbit myocardium.

    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

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1992.tb14436.x

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

    更新日期:1992-08-01 00:00:00

  • Gallium modulates osteoclastic bone resorption in vitro without affecting osteoblasts.

    abstract:BACKGROUND AND PURPOSE:Gallium (Ga) has been shown to be effective in the treatment of disorders associated with accelerated bone loss, including cancer-related hypercalcemia and Paget's disease. These clinical applications suggest that Ga could reduce bone resorption. However, few studies have studied the effects of G...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2010.00665.x

    authors: Verron E,Masson M,Khoshniat S,Duplomb L,Wittrant Y,Baud'huin M,Badran Z,Bujoli B,Janvier P,Scimeca JC,Bouler JM,Guicheux J

    更新日期:2010-04-01 00:00:00

  • Superoxide anions enhance platelet adhesion and aggregation.

    abstract::1. Superoxide dismutase (SOD, 60 u ml-1) or ferricytochrome c (70 microM) significantly inhibited thrombin-stimulated platelet adhesion to gelatin-coated plastic, whereas catalase (1000 u ml-1) or mannitol (1 mM) had no effect. 2. The platelet aggregation induced by low concentrations of thrombin (causing less than 45...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1989.tb12572.x

    authors: Salvemini D,de Nucci G,Sneddon JM,Vane JR

    更新日期:1989-08-01 00:00:00