当前位置： SCI文献检索 > BRITISH JOURNAL OF PHARMACOLOGY期刊下所有文献 > The role of the PDE4D cAMP phosphodiesterase in the regulation of glucagon-like peptide-1 release.

The role of the PDE4D cAMP phosphodiesterase in the regulation of glucagon-like peptide-1 release.

Abstract：

BACKGROUND AND PURPOSE:Increases in intracellular cyclic AMP (cAMP) augment the release/secretion of glucagon-like peptide-1 (GLP-1). As cAMP is hydrolysed by cAMP phosphodiesterases (PDEs), we determined the role of PDEs and particularly PDE4 in regulating GLP-1 release. EXPERIMENTAL APPROACH:GLP-1 release, PDE expression and activity were investigated using rats and GLUTag cells, a GLP-1-releasing cell line. The effects of rolipram, a selective PDE4 inhibitor both in vivo and in vitro and stably overexpressed catalytically inactive PDE4D5 (D556A-PDE4D5) mutant in vitro on GLP-1 release were investigated. KEY RESULTS:Rolipram (1.5 mg x kg(-1) i.v.) increased plasma GLP-1 concentrations approximately twofold above controls in anaesthetized rats and enhanced glucose-induced GLP-1 release in GLUTag cells (EC(50) approximately 1.2 nmol x L(-1)). PDE4D mRNA transcript and protein were detected in GLUTag cells using RT-PCR with gene-specific primers and Western blotting with a specific PDE4D antibody respectively. Moreover, significant PDE activity was inhibited by rolipram in GLUTag cells. A GLUTag cell clone (C1) stably overexpressing the D556A-PDE4D5 mutant, exhibited elevated intracellular cAMP levels and increased basal and glucose-induced GLP-1 release compared with vector-transfected control cells. A role for intracellular cAMP/PKA in enhancing GLP-1 release in response to overexpression of D556A-PDE4D5 mutant was demonstrated by the finding that the PKA inhibitor H89 reduced both basal and glucose-induced GLP-1 release by 37% and 39%, respectively, from C1 GLUTag cells. CONCLUSIONS AND IMPLICATIONS:PDE4D may play an important role in regulating intracellular cAMP linked to the regulation of GLP-1 release.

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Ong WK,Gribble FM,Reimann F,Lynch MJ,Houslay MD,Baillie GS,Furman BL,Pyne NJ

doi

10.1111/j.1476-5381.2009.00194.x

subject

Has Abstract

pub_date

2009-06-01 00:00:00

pages

633-44

issue

4

eissn

0007-1188

issn

1476-5381

pii

BPH194

journal_volume

157

pub_type

杂志文章

相关文献

BRITISH JOURNAL OF PHARMACOLOGY文献大全
  • Adenosine-induced secretion in the canine trachea: modification by methylxanthines and adenosine derivatives.

    abstract：:Adenosine alone at 0.1 and 1.0 mg per tracheal segment stimulated mucus secretion by 52% and 88%, respectively, compared to baseline (P less than 0.0001). The site of the potent secretagogue effect of adenosine in canine trachea was consistent with A2 activation. A2 site activation and enhanced secretion were also ind...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1985.tb09435.x

    authors： Johnson HG,McNee ML

    更新日期：1985-09-01 00:00:00

  • Low concentrations of amitriptyline inhibit nicotinic receptors in unmyelinated axons of human peripheral nerve.

    abstract：BACKGROUND AND PURPOSE:Amitriptyline is often prescribed as a first-line treatment for neuropathic pain but its precise mode of analgesic action remains uncertain. Amitriptyline is known to inhibit voltage-dependent ion channels and also to act as an antagonist at ligand-gated ion channels, such as nicotinic acetylchol...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2009.00347.x

    authors： Freysoldt A,Fleckenstein J,Lang PM,Irnich D,Grafe P,Carr RW

    更新日期：2009-10-01 00:00:00

  • Delta-opioid receptors mediate inhibition of fast excitatory postsynaptic potentials in cat parasympathetic colonic ganglia.

    abstract：:1 The effects of opioids on synaptic transmission in cat sacral parasympathetic colonic ganglia were studied in vitro, using intracellular electrophysiological techniques. Electrical stimulation of the pelvic nerve evoked fast excitatory postsynaptic potentials (e.p.s.ps), which were blocked by hexamethonium and tetro...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1987.tb11340.x

    authors： Kennedy C,Krier J

    更新日期：1987-10-01 00:00:00

  • Biochemical and molecular analysis of carboxylesterase-mediated hydrolysis of cocaine and heroin.

    abstract：BACKGROUND AND PURPOSE:Carboxylesterases (CEs) metabolize a wide range of xenobiotic substrates including heroin, cocaine, meperidine and the anticancer agent CPT-11. In this study, we have purified to homogeneity human liver and intestinal CEs and compared their ability with hydrolyse heroin, cocaine and CPT-11. EXPE...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2010.00700.x

    authors： Hatfield MJ,Tsurkan L,Hyatt JL,Yu X,Edwards CC,Hicks LD,Wadkins RM,Potter PM

    更新日期：2010-08-01 00:00:00

  • Investigating interactions between epicardial adipose tissue and cardiac myocytes: what can we learn from different approaches?

    abstract：:Heart disease is a major cause of morbidity and mortality throughout the world. Some cardiovascular conditions can be modulated by lifestyle factors such as increased exercise or a healthier diet, but many require surgical or pharmacological interventions for their management. More targeted and less invasive therapies...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/bph.13678

    authors： Rietdorf K,MacQueen H

    更新日期：2017-10-01 00:00:00

  • Ergosterol peroxide from an edible mushroom suppresses inflammatory responses in RAW264.7 macrophages and growth of HT29 colon adenocarcinoma cells.

    abstract：BACKGROUND AND PURPOSE:5alpha,8alpha-Epidioxy-22E-ergosta-6, 22-dien-3beta-ol (ergosterol peroxide) is a major antitumour sterol produced by edible or medicinal mushrooms. However, its molecular mechanism of action has yet to be determined. Here, we examine the anticancer and anti-inflammatory effects of ergosterol per...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0706972

    authors： Kobori M,Yoshida M,Ohnishi-Kameyama M,Shinmoto H

    更新日期：2007-01-01 00:00:00

  • Anaphylactic bronchoconstriction in BP2 mice: interactions between serotonin and acetylcholine.

    abstract：:1. Immunized BP2 mice developed an acute bronchoconstriction in vivo and airway muscle contraction in vitro in response to ovalbumin (OA) and these contractions were dose dependent. 2. Methysergide or atropine inhibited OA-induced bronchoconstriction in vivo and airway muscle contraction in vitro. 3. Neostigmine poten...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702304

    authors： Eum SY,Norel X,Lefort J,Labat C,Vargaftig BB,Brink C

    更新日期：1999-01-01 00:00:00

  • New insights into human prostacyclin receptor structure and function through natural and synthetic mutations of transmembrane charged residues.

    abstract：BACKGROUND AND PURPOSE:The human prostacyclin receptor (hIP), a G-protein coupled receptor (GPCR) expressed mainly on platelets and vascular smooth muscle cells, plays important protective roles in the cardiovascular system. We hypothesized that significant insights could be gained into the structure and function of th...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0707413

    authors： Stitham J,Arehart E,Gleim SR,Li N,Douville K,Hwa J

    更新日期：2007-10-01 00:00:00

  • Rilmenidine and reflex renal sympathetic nerve activation in Wistar and hypertensive rats.

    abstract：:1. This study sets out to examine the effect of rilmenidine administered systemically on basal and reflexly activated renal nerve activity in Wistar and stroke prone spontaneously hypertensive rats (SHRSP). 2. Animals were anaesthetized with chloralose/urethane, stimulating electrodes were placed on the brachial plexi...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb16029.x

    authors： Zhang T,Johns EJ

    更新日期：1996-11-01 00:00:00

  • CXCR3 antagonist VUF10085 binds to an intrahelical site distinct from that of the broad spectrum antagonist TAK-779.

    abstract：BACKGROUND AND PURPOSE:The chemokine receptor CXCR3 is implicated in a variety of clinically important diseases, notably rheumatoid arthritis and atherosclerosis. Consequently, antagonists of CXCR3 are of therapeutic interest. In this study, we set out to characterize binding sites of the specific low MW CXCR3 antagoni...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.13027

    authors： Nedjai B,Viney JM,Li H,Hull C,Anderson CA,Horie T,Horuk R,Vaidehi N,Pease JE

    更新日期：2015-04-01 00:00:00

  • Distinct PKC isoforms mediate the activation of cPLA2 and adenylyl cyclase by phorbol ester in RAW264.7 macrophages.

    abstract：:The modulatory effects of protein kinase C (PKC) on the activation of cytosolic phospholipase A2 (cPLA2) and adenylyl cyclase (AC) have recently been described. Since the signalling cascades associated with these events play critical roles in various functions of macrophages, we set out to investigate the crosstalk be...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702219

    authors： Lin WW,Chen BC

    更新日期：1998-12-01 00:00:00

  • Effect of amlodipine on renin secretion and renin gene expression in rats.

    abstract：:1. This study was done to characterize the influence of calcium channel blockade on renin secretion and renin gene expression in normal rats and rats with renovascular hypertension. To this end we studied the effects of the 1,4-dihydropyridine derivative, amlodipine, on plasma renin activity and renal renin m-RNA leve...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb15735.x

    authors： Schricker K,Hamann M,Macher A,Krämer BK,Kaissling B,Kurtz A

    更新日期：1996-10-01 00:00:00

  • The gastric H,K-ATPase blocker lansoprazole is an inhibitor of chloride channels.

    abstract：:1. It was postulated that swelling dependent chloride channels are involved in the proton secretion of parietal cells. Since omeprazole, lansoprazole and its acid activated sulphenamide form AG2000 are structurally related to phenol derivatives known to block swelling dependent chloride channels, we set out to test, w...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703070

    authors： Schmarda A,Dinkhauser P,Gschwentner M,Ritter M,Fürst J,Scandella E,Wöll E,Laich A,Rossmann H,Seidler U,Lang F,Paulmichl M

    更新日期：2000-02-01 00:00:00

  • Drug-gut microbiota interactions: implications for neuropharmacology.

    abstract：:The fate and activity of drugs are frequently dictated not only by the host per se but also by the microorganisms present in the gastrointestinal tract. The gut microbiome is known to, both directly and indirectly, affect drug metabolism. More evidence now hints at the effects that drugs can have on the function and c...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/bph.14366

    authors： Walsh J,Griffin BT,Clarke G,Hyland NP

    更新日期：2018-12-01 00:00:00

  • Functional and ligand binding studies suggest heterogeneity of platelet prostacyclin receptors.

    abstract：:1. This study describes attempts to compare prostacyclin (IP-) receptors in human, pig, horse, rabbit and rat platelets and in circular muscle of human, rabbit and dog mesenteric and pig gastroepiploic arteries. Three stable prostacyclin analogues, iloprost, cicaprost and 6a-carba-prostacyclin (6a-carba-PGI2) and a pr...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1989.tb12001.x

    authors： Armstrong RA,Lawrence RA,Jones RL,Wilson NH,Collier A

    更新日期：1989-07-01 00:00:00

  • Respiratory actions of tachykinins in the nucleus of the solitary tract: characterization of receptors using selective agonists and antagonists.

    abstract：:1. The respiratory response to microinjection of tachykinins and analogues into the commissural nucleus of the solitary tract (cNTS) of urethane-anaesthetized rats was investigated in the presence and absence of selective tachykinin NK(1), NK(2) and NK(3) antagonists (RP 67580, SR 48968 and SR 142801, respectively). 2...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703172

    authors： Mazzone SB,Geraghty DP

    更新日期：2000-03-01 00:00:00

  • Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract.

    abstract：:1. Phenylephrine-induced contractions of rabbit isolated trigone and urethra were antagonized in a competitive manner by alfuzosin (pA2 7.44 and 7.30, respectively) and prazosin. 2. The characteristics of [3H]-prazosin binding to human prostatic adenoma tissue were evaluated. [3H]-prazosin was potently displaced by al...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1993.tb13762.x

    authors： Lefèvre-Borg F,O'Connor SE,Schoemaker H,Hicks PE,Lechaire J,Gautier E,Pierre F,Pimoule C,Manoury P,Langer SZ

    更新日期：1993-08-01 00:00:00

  • Different pharmacological characteristics in L6 and C2C12 muscle cells and intact rat skeletal muscle for amylin, CGRP and calcitonin.

    abstract：:1. We compared the ability of rat amylin, rat calcitonin gene-related peptide (CGRP) and rat and salmon calcitonins to elevate cyclic AMP levels and to inhibit [U-14C]-glucose incorporation into glycogen in insulin-stimulated intact rat soleus muscle and in two cell lines derived from rodent skeletal muscle, L6 and C2...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb15270.x

    authors： Pittner RA,Wolfe-Lopez D,Young AA,Beaumont K

    更新日期：1996-03-01 00:00:00

  • In vitro and in vivo pharmacological characterization of the novel UT receptor ligand [Pen5,DTrp7,Dab8]urotensin II(4-11) (UFP-803).

    abstract：:The novel urotensin-II (U-II) receptor (UT) ligand, [Pen(5),DTrp(7),Dab(8)]U-II(4-11) (UFP-803), was pharmacologically evaluated and compared with urantide in in vitro and in vivo assays. In the rat isolated aorta, UFP-803 was inactive alone but, concentration dependently, displaced the contractile response to U-II to...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0706438

    authors： Camarda V,Spagnol M,Song W,Vergura R,Roth AL,Thompson JP,Rowbotham DJ,Guerrini R,Marzola E,Salvadori S,Cavanni P,Regoli D,Douglas SA,Lambert DG,Calò G

    更新日期：2006-01-01 00:00:00

  • Prominent sympathetic purinergic vasoconstriction in the rabbit splenic artery: potentiation by 2,2'-pyridylisatogen tosylate.

    abstract：:1. Vasoconstrictions induced by transmural electrical field stimulation were frequency-dependent from 2 to 32 Hz in the rabbit isolated splenic artery. All contractions were abolished in the presence of tetrodotoxin 1 microM or guanethidine 100 microM. Stimulation at a frequency of more than 32 Hz induced both neuroge...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0700933

    authors： Ren LM,Burnstock G

    更新日期：1997-02-01 00:00:00

  • Vascular pharmacology of a novel cannabinoid-like compound, 3-(5-dimethylcarbamoyl-pent-1-enyl)-N-(2-hydroxy-1-methyl-ethyl)benzamide (VSN16) in the rat.

    abstract：BACKGROUND AND PURPOSE:A putative novel cannabinoid receptor mediates vasorelaxation to anandamide and abnormal-cannabidiol and is blocked by O-1918 and by high concentrations of rimonabant. This study investigates VSN16, a novel water-soluble agonist, as a vasorelaxant potentially acting at non-CB1, non-CB2 cannabinoi...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0707470

    authors： Hoi PM,Visintin C,Okuyama M,Gardiner SM,Kaup SS,Bennett T,Baker D,Selwood DL,Hiley CR

    更新日期：2007-11-01 00:00:00

  • Effect of alpha-trinositol on interstitial fluid pressure, oedema generation and albumin extravasation in experimental frostbite in the rat.

    abstract：:1. The anti-inflammatory effect of alpha-trinositol (D-myo-inositol-1,2,6-trisphosphate) on oedema formation, microvascular protein leakage and interstitial fluid pressure (Pif) in rat skin after frostbite injury, was investigated. Alpha-trinositol (40 mg kg body weight(-1)) was administered intravenously as a bolus b...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702442

    authors： Berg A,Aas P,Gustafsson T,Reed RK

    更新日期：1999-03-01 00:00:00

  • Parallel maturation of the pancreatic secretory response to cholinergic stimulation and the muscarinic receptor population.

    abstract：:1 The appearance of pancreatic muscarinic receptors during development has been measured by use of the specific ligand [3H]-quinuclidinyl benzilate ([3H]-QNB). 2 QNB binding sites are present in foetal pancreas; their maximal concentration is attained at the age of 30 days and a significant decrease is observed in one...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1981.tb10428.x

    authors： Dumont Y,Larose L,Morisset J,Poirier GG

    更新日期：1981-06-01 00:00:00

  • Role of potassium channels in the nitrergic nerve stimulation-induced vasodilatation in the guinea-pig isolated basilar artery.

    abstract：:1. We studied the effects of various K+ channel blockers on the vasodilator responses of guinea-pig isolated basilar arteries to nitrergic nerve stimulation, the nitric oxide (NO) donor sodium nitroprusside (SNP), and the membrane permeable guanosine-3',5'-cyclic monophosphate (cyclic GMP) analogue 8-bromo-cyclic GMP ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0701552

    authors： Jiang F,Li CG,Rand MJ

    更新日期：1998-01-01 00:00:00

  • Novel cAMP signalling paradigms: therapeutic implications for airway disease.

    abstract：:Since its discovery over 50 years ago, cAMP has been the archetypal second messenger introducing students to the concept of cell signalling at the simplest level. As explored in this review, however, there are many more facets to cAMP signalling than the path from Gs-coupled receptor to adenylyl cyclase (AC) to cAMP t...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/j.1476-5381.2011.01719.x

    authors： Billington CK,Hall IP

    更新日期：2012-05-01 00:00:00

  • Human vascular to cardiac tissue selectivity of L- and T-type calcium channel antagonists.

    abstract：:1. Voltage-operated calcium channel (VOCC) antagonists are effective antihypertensive and antianginal agents but they also depress myocardial contractility. 2. We compared four L-type calcium channel antagonists, felodipine, nifedipine, amlodipine and verapamil and a relatively T-type selective calcium channel antagon...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702045

    authors： Sarsero D,Fujiwara T,Molenaar P,Angus JA

    更新日期：1998-09-01 00:00:00

  • Inhibition by simvastatin, but not pravastatin, of glucose-induced cytosolic Ca2+ signalling and insulin secretion due to blockade of L-type Ca2+ channels in rat islet beta-cells.

    abstract：:1. Hypercholesterolaemia often occurs in patients with type 2 diabetes, who therefore encounter administration of HMG-CoA reductase inhibitors. Alteration of pancreatic beta-cell function leading to an impaired insulin secretory response to glucose plays a crucial role in the pathogenesis of type 2 diabetes. Therefore...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702397

    authors： Yada T,Nakata M,Shiraishi T,Kakei M

    更新日期：1999-03-01 00:00:00

  • Effects of vinblastine on noradrenergic axons.

    abstract：:1 The effects of vinblastine and 6-hydroxydopamine (6-OHDA) on various parameters of adrenergic neurone functions in the rat were examined and compared.2 During the first 12 h after injection of vinblastine, although the concentration of cardiac noradrenaline was unaltered, the turnover rate of the catecholamine in th...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1974.tb08564.x

    authors： Hanbauer I,Jacobowitz DM,Kopin IJ

    更新日期：1974-02-01 00:00:00

  • Potentiation of chloride responses to glycine by three 5-HT3 antagonists in rat spinal neurones.

    abstract：:1. Modulations of Cl- responses to glycine by 5-hydroxytryptamine ligands were studied in cultured spinal neurones, by the whole-cell recording technique. 2. Three 5-HT3 antagonists were found to potentiate reversibly responses to low concentrations of glycine. Potentiations were induced by micromolar concentrations o...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb15651.x

    authors： Chesnoy-Marchais D

    更新日期：1996-08-01 00:00:00

  • Orexin A activates hypoglossal motoneurons and enhances genioglossus muscle activity in rats.

    abstract：BACKGROUND AND PURPOSE:Orexins have been demonstrated to play important roles in many physiological processes. However, it is not known how orexin A affects the activity of the hypoglossal motoneuron (HMN) and genioglossus (GG) muscle. EXPERIMENTAL APPROACH:GG muscle electromyograms (GG-EMG) were recorded in anaesthet...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.12784

    authors： Zhang GH,Liu ZL,Zhang BJ,Geng WY,Song NN,Zhou W,Cao YX,Li SQ,Huang ZL,Shen LL

    更新日期：2014-09-01 00:00:00