当前位置： SCI文献检索 > BRITISH JOURNAL OF PHARMACOLOGY期刊下所有文献 > Nitric oxide synthase inhibition by dimaprit and dimaprit analogues.

Nitric oxide synthase inhibition by dimaprit and dimaprit analogues.

Abstract：

:1. The similarity in molecular structure between the histamine H2-agonist dimaprit (3-dimethylamino-propyl-isothiourea) and the endogenous nitric oxide synthase (NOS) substrate L-arginine prompted us to study the effect of dimaprit and some dimaprit analogues on NOS activity. Dimaprit and some of its analogues were tested in an in vitro assay which measures the conversion of [3H]-L-arginine to [3H]-L-citrulline. Dimaprit inhibits rat brain NOS (nNOS) concentration dependently with an IC50 of 49+/-14 microM. 2. Removal of one or both of the methyl groups from the non-isothiourea nitrogen of dimaprit improved nNOS inhibitory properties. Aminopropylisothiourea is the most potent compound (IC50 = 4.1+/-0.9 microM) of the series followed by methylaminopropylisothiourea (IC50 = 7.6 +/- microM). 3. The observed effect of aminopropylisothiourea and methylaminopropyl-isothiourea are probably not due to the compounds themselves but to the corresponding mercaptoalkylguanidines, rearrangement products formed in aqueous solutions. This hypothesis is strengthened by the finding that aminobutylisothiourea is not active since a rearrangement to mercaptobutylguanidine does not occur. 4. Remarkably, nitrosylation of the isothiourea group of dimaprit decreases nNOS inhibitory activity, while nitrosylation of the guanidine analogue of dimaprit increases the inhibition of nNOS activity. 5. The pharmacological profile of dimaprit includes inhibition of nNOS. The nNOS inhibitory activity occurs in the same concentration range as the H2-agonist and H3-agonist activity of this compound.

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Paquay JB,Hoen PA,Voss HP,Bast A,Timmerman H,Haenen GR

doi

10.1038/sj.bjp.0702552

subject

Has Abstract

pub_date

1999-05-01 00:00:00

pages

331-4

issue

2

eissn

0007-1188

issn

1476-5381

journal_volume

127

pub_type

杂志文章

相关文献

BRITISH JOURNAL OF PHARMACOLOGY文献大全
  • Modification of cardiovascular responses to histamine by dithiothreitol.

    abstract：:1 Histamine produced dose-dependent contractile responses on both isolated perfused ear arteries and aortic strips of the rabbit. These responses were blocked by mepyramine and potentiated by both metiamide and dithiothreitol. 2 In the presence of maximum potentiation by metiamide, dithiothreitol still potentiated the...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1977.tb07497.x

    authors： Carroll PR,Glover WE

    更新日期：1977-02-01 00:00:00

  • Snapshot: implications for melatonin in endoplasmic reticulum homeostasis.

    abstract：:The endoplasmic reticulum (ER) is an important intracellular membranous organelle. Previous studies have demonstrated that the ER is responsible for protein folding and trafficking, lipid synthesis and the maintenance of calcium homeostasis. Interestingly, the morphology and structure of the ER were recently found to ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/bph.13651

    authors： Hu W,Ma Z,Di S,Jiang S,Li Y,Fan C,Yang Y,Wang D

    更新日期：2016-12-01 00:00:00

  • Whole cell and single channel analysis of the kinetics of glycine-sensitive N-methyl-D-aspartate receptor desensitization.

    abstract：:1. The kinetics of glycine-sensitive, N-methyl-D-aspartate (NMDA) receptor desensitization were investigated in cultured neurones with the patch clamp technique. 2. The degree of fast NMDA-receptor desensitization was inversely related to glycine concentration. Thus, increasing concentrations of glycine from 30 nM to ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1993.tb13556.x

    authors： Parsons CG,Zong X,Lux HD

    更新日期：1993-05-01 00:00:00

  • ACE2, angiotensin-(1-7) and Mas receptor axis in inflammation and fibrosis.

    abstract：:Recent advances have improved our understanding of the renin-angiotensin system (RAS). These have included the recognition that angiotensin (Ang)-(1-7) is a biologically active product of the RAS cascade. The identification of the ACE homologue ACE2, which forms Ang-(1-7) from Ang II, and the GPCR Mas as an Ang-(1-7) ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/bph.12159

    authors： Simões e Silva AC,Silveira KD,Ferreira AJ,Teixeira MM

    更新日期：2013-06-01 00:00:00

  • Degradation of acetylcholine in human airways: role of butyrylcholinesterase.

    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

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1993.tb13486.x

    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

  • Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.

    abstract：BACKGROUND AND PURPOSE:Strontium ranelate, a drug approved and until recently used for the treatment of osteoporosis, mediates its effects on bone at least in part via the calcium-sensing (CaS) receptor. However, it is not known whether bone-targeted CaS receptor positive allosteric modulators (PAMs; calcimimetics) rep...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.14344

    authors： Diepenhorst NA,Leach K,Keller AN,Rueda P,Cook AE,Pierce TL,Nowell C,Pastoureau P,Sabatini M,Summers RJ,Charman WN,Sexton PM,Christopoulos A,Langmead CJ

    更新日期：2018-11-01 00:00:00

  • Evaluation of the effect of azapropazone on neutrophil migration in anaesthetized swine using a multichamber blister suction technique.

    abstract：:1. The purpose of this study was to determine the in vivo inhibitory efficacy of azapropazone on neutrophil migration. The effects of azapropazone given at a dose of 100 mg kg-1 i.v. every 2 h on the neutrophil migration into skin inflammation sites (blister fluid) as well as into an autologous serum (+/- chemoattract...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1990.tb14686.x

    authors： Mousa SA,Brown R,Chan Y,Hsieh J,Smith RD

    更新日期：1990-02-01 00:00:00

  • Evidence against the unitary hypothesis of agonist and antagonist action at presynaptic adrenoceptors.

    abstract：:1 The concept that presynaptic receptors regulate noradrenergic transmitter release via a system of inhibitory receptors mediating negative feedback relies on a supposed association between increases in stimulation-induced efflux of [3H]-noradrenaline by antagonists and blockade by them of the inhibitory effects of ex...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1982.tb09308.x

    authors： Kalsner S

    更新日期：1982-10-01 00:00:00

  • Investigation of the effects of 5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) on membrane currents in rat portal vein.

    abstract：:1. The effects of 5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) were investigated on evoked and spontaneous currents in freshly-isolated cells from the rat portal vein by use of conventional whole-cell recording and perforated-patch techniques. 2. At a holding potential of -60 mV in potassium-free, caesium-conta...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb15171.x

    authors： Kirkup AJ,Edwards G,Weston AH

    更新日期：1996-01-01 00:00:00

  • Endothelium-independent relaxation of rabbit coronary artery by 17 beta-oestradiol in vitro.

    abstract：:1. We assessed the relaxant effect of 17 beta-oestradiol (10(-7), 10(-6) and 10(-5) M) on rabbit isolated coronary arteries precontracted with prostaglandin F2 alpha (3 x 10(-6) M), high extracellular potassium (30 mM) and Bay K 8644 (10(-6) M) plus high extracellular potassium (15 mM) by measuring isometric tension. ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1991.tb12545.x

    authors： Jiang CW,Sarrel PM,Lindsay DC,Poole-Wilson PA,Collins P

    更新日期：1991-12-01 00:00:00

  • Cellular target of voltage and calcium-dependent K(+) channel blockers involved in EDHF-mediated responses in rat superior mesenteric artery.

    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

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704348

    authors： Ghisdal P,Morel N

    更新日期：2001-11-01 00:00:00

  • Effects of glyceryl trinitrate and SIN-1A on musculature and vasculature of the dog trachea in situ.

    abstract：:In dog trachea in situ, perfused arterially with blood, isoprenaline, glyceryl trinitrate and N-nitroso-N-morpholinoamino-acetonitrile (SIN-1A) given intra-arterially, decreased tracheal tone which had been elevated by neostigmine and increased tracheal blood flow. Glyceryl trinitrate and SIN-1A were more effective on...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1981.tb16764.x

    authors： Maruyama M,Satoh K,Taira N

    更新日期：1981-05-01 00:00:00

  • Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding.

    abstract：BACKGROUND AND PURPOSE:The P2X(7) receptor exhibits complex pharmacological properties. In this study, binding of a [(3)H]-labelled P2X(7) receptor antagonist to human P2X(7) receptors has been examined to further understand ligand interactions with this receptor. EXPERIMENTAL APPROACH:The P2X(7) receptor antagonist, ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0707196

    authors： Michel AD,Chambers LJ,Clay WC,Condreay JP,Walter DS,Chessell IP

    更新日期：2007-05-01 00:00:00

  • Guidelines for reporting experiments involving animals: the ARRIVE guidelines.

    abstract：:British Journal of Pharmacology (BJP) is pleased to publish a new set of guidelines for reporting research involving animals, simultaneously with several other journals; the 'ARRIVE' guidelines (Animals in Research: Reporting In Vivo Experiments). This editorial summarizes the background to the guidelines, gives our v...

    journal_title：British journal of pharmacology

    pub_type： 社论

    doi：10.1111/j.1476-5381.2010.00873.x

    authors： McGrath JC,Drummond GB,McLachlan EM,Kilkenny C,Wainwright CL

    更新日期：2010-08-01 00:00:00

  • Protective effect of propranolol on mitochondrial function in the ischaemic heart.

    abstract：:1. The present study was aimed to determine whether propranolol improves contractile function of the ischaemic/reperfused heart through protection of the mitochondrial function during ischaemia. 2. Isolated perfused rat hearts were subjected to 35-min ischaemia followed by 60-min reperfusion. Pre-treatment with propra...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704724

    authors： Iwai T,Tanonaka K,Kasahara S,Inoue R,Takeo S

    更新日期：2002-06-01 00:00:00

  • Targeting of sodium channel blockers into nociceptors to produce long-duration analgesia: a systematic study and review.

    abstract：BACKGROUND AND PURPOSE:We have developed a strategy to target the permanently charged lidocaine derivative lidocaine N-ethyl bromide (QX-314) selectively into nociceptive sensory neurons through the large-pore transient receptor potential cation channel subfamily V (TRPV1) noxious heat detector channel. This involves c...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2011.01391.x

    authors： Roberson DP,Binshtok AM,Blasl F,Bean BP,Woolf CJ

    更新日期：2011-09-01 00:00:00

  • Indomethacin-induced alterations in corticosteroid and prostaglandin release by isolated adrenocortical cells of the cat.

    abstract：:1 The effects of purported prostaglandin synthesis inhibitors on steroid and prostaglandin (E and F) release from trypsin-dispersed cat adrenocortical cells were investigated. 2 Low indomethacin concentrations potentiated adrenocorticotrophin (ACTH)-evoked prostaglandin and steroid release, whereas higher concentratio...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1976.tb07477.x

    authors： Laychock SG,Rubin RP

    更新日期：1976-06-01 00:00:00

  • NCX 4016, a nitric oxide-releasing aspirin, modulates adrenergic vasoconstriction in the perfused rat tail artery.

    abstract：:1. The ability of the nitric oxide (NO)-releasing aspirin, NCX 4016, to control vasoconstrictor responses induced by electrical field stimulation (TNS) or by exogenous norepinephrine (NE) was investigated in perfused rat tail artery with intact endothelium. 2. NCX 4016 (25, 50 and 100 microM) dose-dependently antagoni...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704869

    authors： Rossoni G,Manfredi B,Del Soldato P,Berti F

    更新日期：2002-09-01 00:00:00

  • Presynaptic alpha-adrenoceptors: do exogenous and neuronally released noradrenaline act at different sites?

    abstract：:The effects of dopamine receptor and alpha-adrenoceptor agonists and antagonists on the stimulation-evoked overflow of radioactivity from strips of dog saphenous vein previously loaded with [3H]-noradrenaline have been examined alone and in combination. In the presence of neuronal and extraneuronal catecholamine uptak...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1984.tb10098.x

    authors： Baker DJ,Drew GM,Hilditch A

    更新日期：1984-03-01 00:00:00

  • Mechanisms involved in the regulation of mRNA for M2 muscarinic acetylcholine receptors and endothelial and neuronal NO synthases in rat atria.

    abstract：BACKGROUND AND PURPOSE:Agonists of the M(2) muscarinic acetylcholine receptor (mAChR) increase mRNA for this receptor and mRNA for endothelial and neuronal isoforms of NO synthase (eNOS or nNOS). Here we examine the different signalling pathways involved in such events in rat cardiac atria. EXPERIMENTAL APPROACH:In is...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0707180

    authors： Ganzinelli S,Joensen L,Borda E,Bernabeo G,Sterin-Borda L

    更新日期：2007-05-01 00:00:00

  • Structurally diverse amphiphiles exhibit biphasic modulation of GABAA receptors: similarities and differences with neurosteroid actions.

    abstract：BACKGROUND AND PURPOSE:Some neurosteroids, notably 3alpha-hydroxysteroids, positively modulate GABA(A) receptors, but sulphated steroids negatively modulate these receptors. Recently, other lipophilic amphiphiles have been suggested to positively modulate GABA receptors. We examined whether there was similarity among t...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2010.00679.x

    authors： Chisari M,Shu HJ,Taylor A,Steinbach JH,Zorumski CF,Mennerick S

    更新日期：2010-05-01 00:00:00

  • Study of NO and VIP as non-adrenergic non-cholinergic neurotransmitters in the pig gastric fundus.

    abstract：:1. The contribution of nitric oxide (NO) and vasoactive intestinal polypeptide (VIP) to non-adrenergic non-cholinergic (NANC) relaxations in the pig gastric fundus was investigated. 2. Circular and longitudinal muscle strips were mounted for isotonic registration in the presence of atropine and guanethidine; tone was ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1995.tb16406.x

    authors： Lefebvre RA,Smits GJ,Timmermans JP

    更新日期：1995-10-01 00:00:00

  • The Akt inhibitor, triciribine, ameliorates chronic hypoxia-induced vascular pruning and TGFβ-induced pulmonary fibrosis.

    abstract：BACKGROUND AND PURPOSE:Interstitial lung disease accounts for a group of chronic and progressive disorders associated with severe pulmonary vascular remodelling, peripheral vascular rarefaction and fibrosis, thus limiting lung function. We have previously shown that Akt is necessary for myofibroblast differentiation, a...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.13203

    authors： Abdalla M,Sabbineni H,Prakash R,Ergul A,Fagan SC,Somanath PR

    更新日期：2015-08-01 00:00:00

  • Haem oxygenase-1 up-regulation by rosiglitazone via ROS-dependent Nrf2-antioxidant response elements axis or PPARγ attenuates LPS-mediated lung inflammation.

    abstract：BACKGROUND AND PURPOSE:Haem oxygenase-1 (HO-1) is induced by thiazolidinediones including rosiglitazone and exerts anti-inflammatory effects in various models. However, the molecular mechanisms underlying rosiglitazone-induced HO-1 expression remain largely unknown in human pulmonary alveolar epithelial cells (HPAEpiCs...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.14465

    authors： Cho RL,Yang CC,Tseng HC,Hsiao LD,Lin CC,Yang CM

    更新日期：2018-10-01 00:00:00

  • Actions of second messengers synthesized by various spasmogenic agents and their relation to mechanical responses in dog tracheal smooth muscle.

    abstract：:1. The effects of the spasmogenic agents, carbachol (CCh), histamine, 5-hydroxytryptamine (5-HT) and 9,11-epithio-11,12-methano-thromboxane A2 (STA2) were investigated on smooth muscle tissues of the dog trachea. 2. CCh (10 microM) produced a larger contraction than high K (128 mM), 10 microM histamine, 5-HT or STA2. ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1990.tb12049.x

    authors： Katsuyama H,Suzuki S,Nishiye E

    更新日期：1990-05-01 00:00:00

  • Effects of desensitization to adenosine 5'-triphosphate and adenosine on non-adrenergic inhibitory responses in the circular muscle of rabbit colon.

    abstract：:An approximate eight fold desensitization of the circular coat of the distal rabbit colon to adenosine 5'-triphosphate (ATP) and adenosine could be achieved by repeatedly exposing the organ to relatively low concentrations (10-100 microM) of these compounds. The desensitization was specific and reversible after prolon...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1982.tb08788.x

    authors： Crema A,D'Angelo L,Frigo GM,Lecchini S,Onori L,Tonini M

    更新日期：1982-02-01 00:00:00

  • 5-HT7 receptors mediate the inhibitory effect of 5-HT on peristalsis in the isolated guinea-pig ileum.

    abstract：:The study was undertaken to investigate the 5-HT receptor mediating the inhibitory effect of 5-HT on peristalsis in the guinea-pig isolated ileum. The facilitatory and inhibitory effects were measured as the decrease and increase, respectively, in the intraluminal pressure required to trigger peristalsis. In the prese...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0705184

    authors： Tuladhar BR,Ge L,Naylor RJ

    更新日期：2003-04-01 00:00:00

  • BODIPY-conjugated neuropeptide Y ligands: new fluorescent tools to tag Y1, Y2, Y4 and Y5 receptor subtypes.

    abstract：:N-terminal labelled fluorescent BODIPY-NPY peptide analogues were tested in Y1, Y2, Y4 and Y5 receptor-binding assays performed in rat brain membrane preparations and HEK293 cells expressing the rat Y1, Y2, Y4 and Y5 receptors. BODIPY TMR/FL-[Leu31, Pro34]NPY/PYY were able to compete for specific [125][Leu31, Pro34]PY...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0706425

    authors： Dumont Y,Gaudreau P,Mazzuferi M,Langlois D,Chabot JG,Fournier A,Simonato M,Quirion R

    更新日期：2005-12-01 00:00:00

  • Subclassification of release-regulating alpha 2-autoreceptors in human brain cortex.

    abstract：:1. Release-regulating alpha 2-autoreceptors in human brain were characterized pharmacologically in cortical slices from patients undergoing neurosurgery to remove subcortical tumours; the slices were prelabelled with [3H]-noradrenaline ([3H]-NA) and stimulated electrically (3 Hz, 2 ms, 24 mA) under superfusion conditi...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb13421.x

    authors： Raiteri M,Bonanno G,Maura G,Pende M,Andrioli GC,Ruelle A

    更新日期：1992-12-01 00:00:00

  • Contribution of cytochrome P450 metabolites to bradykinin-induced vasodilation in endothelial NO synthase deficient mouse hearts.

    abstract：:We have characterized the contribution of endothelial nitric oxide synthase (eNOS), cyclo-oxygenase (COX) and cytochrome P450 (CYP450) to the bradykinin (BK)- induced vasodilation in isolated hearts from wildtype (WT) and eNOS deficient mice (eNOS-/-). The endothelium-dependent vasodilation by bradykinin (BK, 1 microM...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704472

    authors： Ding Z,Gödecke A,Schrader J

    更新日期：2002-02-01 00:00:00