当前位置： SCI文献检索 > BRITISH JOURNAL OF PHARMACOLOGY期刊下所有文献 > A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AV nodal conduction in guinea-pig.

A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AV nodal conduction in guinea-pig.

Abstract：

:1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-510), and the prototypical calcium channel blocker diltiazem. 2. In the atrial-paced isolated heart, CVT-510 was approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50 = 41 nM) than to increase coronary conductance (EC50 = 200 nM). At concentrations of CVT-510 (40 nM) and diltiazem (1 microM) that caused equal prolongation of S-H interval (approximately 10 ms), diltiazem, but not CVT-510, significantly reduced left ventricular developed pressure (LVP) and markedly increased coronary conductance. CVT-510 shortened atrial (EC50 = 73 nM) but not the ventricular monophasic action potentials (MAP). 3. In atrial-paced anaesthetized guinea-pigs, intravenous infusions of CVT-510 and diltiazem caused nearly equal prolongations of P-R interval. However, diltiazem, but not CVT-510, significantly reduced mean arterial blood pressure. 4. Both CVT-510 and diltiazem prolonged S-H interval, i.e., slowed AV nodal conduction. However, the A1 receptor-selective agonist CVT-510 did so without causing the negative inotropic, vasodilator, and hypotensive effects associated with diltiazem. Because CVT-510 did not affect the ventricular action potential, it is unlikely that this agonist will have a proarrythmic action in ventricular myocardium.

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Snowdy S,Liang HX,Blackburn B,Lum R,Nelson M,Wang L,Pfister J,Sharma BP,Wolff A,Belardinelli L

doi

10.1038/sj.bjp.0702287

subject

Has Abstract

pub_date

1999-01-01 00:00:00

pages

137-46

issue

1

eissn

0007-1188

issn

1476-5381

journal_volume

126

pub_type

杂志文章

相关文献

BRITISH JOURNAL OF PHARMACOLOGY文献大全
  • Excessive stimulation of poly(ADP-ribosyl)ation contributes to endothelial dysfunction in pre-eclampsia.

    abstract：:1. Pre-eclampsia is a serious pregnancy disorder associated with widespread activation of the maternal vascular endothelium. Recent evidence implicates a role for oxidative stress in the aetiology of this condition. 2. Reactive oxygen species, particularly superoxide anions, invokes endothelial cell activation through...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0706055

    authors： Crocker IP,Kenny LC,Thornton WA,Szabo C,Baker PN

    更新日期：2005-03-01 00:00:00

  • The electromechanical window is no better than QT prolongation to assess risk of Torsade de Pointes in the complete atrioventricular block model in dogs.

    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

    pub_type： 杂志文章

    doi：10.1111/bph.12483

    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

  • Voltage-dependent block of normal and mutant muscle sodium channels by 4-Chloro-m-Cresol.

    abstract：:1 The effects of 4-Chloro-m-Cresol (4-CmC) were examined on heterologously expressed wild type (WT), Paramyotonia Congenita (R1448H) and Hyperkalemic Periodic Paralysis (M1360V) mutant alpha-subunits of human muscle sodium channels. 2 Block of rested sodium channels caused by 4-CmC was concentration-dependent with an ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702896

    authors： Haeseler G,Leuwer M,Kavan J,Würz A,Dengler R,Piepenbrock S

    更新日期：1999-11-01 00:00:00

  • Oxidative and non-oxidative mechanisms of neuronal cell death and apoptosis by L-3,4-dihydroxyphenylalanine (L-DOPA) and dopamine.

    abstract：:1. The present study was designed to evaluate the nature of intervening agents in L-DOPA- and dopamine-induced neurotoxicity in Neuro-2A cells. 2. In the absence of cells and in conditions of light protection, at 37 degrees C, L-DOPA or dopamine (1 mM) in culture medium degraded spontaneously in a time-dependent manne...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704982

    authors： Pedrosa R,Soares-da-Silva P

    更新日期：2002-12-01 00:00:00

  • Improvement of exercise capacity of rats with chronic heart failure by long-term treatment with trandolapril.

    abstract：:1. The effects of long-term treatment with trandolapril, an angiotensin I-converting enzyme inhibitor, on exercise capacity of rats with chronic heart failure (CHF) following coronary artery ligation were examined. CHF was developed by 8 weeks after the coronary artery ligation. 2. The running time of rats with CHF in...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0702471

    authors： Yamaguchi F,Kawana K,Tanonaka K,Kamano I,Igarashi T,Gen E,Fujimoto Y,Maki T,Sanbe A,Nasa Y,Takeo S

    更新日期：1999-04-01 00:00:00

  • Modelling prefrontal cortex deficits in schizophrenia: implications for treatment.

    abstract：:Current treatments of schizophrenia are compromised by their inability to treat all symptoms of the disease and their side-effects. Whilst existing antipsychotic drugs are effective against positive symptoms, they have negligible efficacy against the prefrontal cortex (PFC)-associated cognitive deficits and negative s...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1038/bjp.2008.24

    authors： Pratt JA,Winchester C,Egerton A,Cochran SM,Morris BJ

    更新日期：2008-03-01 00:00:00

  • Cannabidiol exerts antiepileptic effects by restoring hippocampal interneuron functions in a temporal lobe epilepsy model.

    abstract：BACKGROUND AND PURPOSE:A non-psychoactive phytocannabinoid, cannabidiol (CBD), shows promising results as an effective potential antiepileptic drug in some forms of refractory epilepsy. To elucidate the mechanisms by which CBD exerts its anti-seizure effects, we investigated its effects at synaptic connections and on t...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.14202

    authors： Khan AA,Shekh-Ahmad T,Khalil A,Walker MC,Ali AB

    更新日期：2018-06-01 00:00:00

  • Evidence for antithrombin III involvement in the anticoagulant activity of cellulose sulphate.

    abstract：:1 Cellulose sulphate, like heparin, prolonged the clotting time in partial thromboplastin time (PTT) assays, inhibited the amidolytic activity of thrombin, was without effect on amidolysis catalysed by activated coagulation factor X(Xa), and potentiated the inhibition of both thrombin and Xa by antithrombin III (AT). ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1980.tb10856.x

    authors： Kindness G,Long WF,Williamson FB

    更新日期：1980-04-01 00:00:00

  • Intimal hyperplasia in human uterine arteries accompanied by impaired synergism between prostaglandin I2 and nitric oxide.

    abstract：:1. The present experiments were designed to investigate the mechanisms causing intimal hyperplasia in connection with the impaired synergism between prostaglandin I2 (PGI2) and nitric oxide (NO) in human uterine arteries (UAs). 2. In order to assess the magnitude of intimal hyperplasia, the intima:media ratio (%) was ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb15779.x

    authors： Obayashi S,Aso T,Sato J,Hamasaki H,Azuma H

    更新日期：1996-11-01 00:00:00

  • Endothelium-dependent hyperpolarization of canine coronary smooth muscle.

    abstract：:1. Experiments were designed to determine whether endothelium-dependent relaxing factor(s) released by acetylcholine from the canine femoral artery influences the membrane potential of coronary arterial smooth muscle. 2. The membrane potential was recorded in small canine coronary arteries (internal diameter less than...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1988.tb10306.x

    authors： Feletou M,Vanhoutte PM

    更新日期：1988-03-01 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

  • The application of 'omics' to pulmonary arterial hypertension.

    abstract：:Recent genome-wide analyses of rare and common sequence variations have brought greater clarity to the genetic architecture of pulmonary arterial hypertension and implicated novel genes in disease development. Transcriptional signatures have been reported in whole lung tissue, pulmonary vascular cells and peripheral c...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/bph.15056

    authors： Harbaum L,Rhodes CJ,Otero-Núñez P,Wharton J,Wilkins MR

    更新日期：2021-01-01 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

  • The detection of differential beta-adrenoceptor blockade in the cat.

    abstract：:1. Tachycardia and bronchodilatation were produced by intravenous dimethylphenylpiperazinium iodide (DMPP) in the spinal or pithed cat. Responses other than those involving beta-adrenoceptors were minimized by appropriate blocking agents.2. With intact adrenals, both the tachycardia and bronchodilatation with 10 mug/k...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1973.tb08256.x

    authors： Parkes MW

    更新日期：1973-08-01 00:00:00

  • Differential inhibition by adenosine or by prostaglandin E1 of human platelet aggregation induced by adenosine 5'-O-(1-thiodiphosphate) and adenosine 5'-O-(2-thiodiphosphate).

    abstract：:Adenosine 5'-diphosphate (ADP) induces human platelet aggregation and inhibits stimulated adenylate cyclase. Adenosine 5'-O-(1-thiodiphosphate) (ADP-alpha-S) and adenosine 5'-O-(2-thiodiphosphate) (ADP-beta-S) act at the ADP receptor and achieve the same maximal rate of human platelet aggregation as each other. Adenos...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1982.tb08781.x

    authors： Cusack NJ,Hourani SM

    更新日期：1982-02-01 00:00:00

  • Rhythmic relaxations of active tension in the rabbit large arteries induced by a combination of cyclopiazonic acid and Bay K 8644.

    abstract：:1. We previously demonstrated that cyclopiazonic acid (CPA), an inhibitor of Ca(2+)-ATPase in the sarcoplasmic reticulum, induced rhythmic relaxations of active tension in the endothelium-denuded small arteries of the mesentery and the ear of the rabbit, but that this agent failed to induce rhythmic responses in the e...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1996.tb15392.x

    authors： Omote M,Mizusawa H

    更新日期：1996-05-01 00:00:00

  • Prostaglandins, thromboxanes and the pregnant rat uterus at term.

    abstract：:1 Prostaglandin and thromboxane release from the term pregnant (Day 22) rat uterus in vitro has been measured by radioimmunoassay and gas chromatography combined with mass spectrometry. 2 Prostacyclin (prostaglandin I2, PGI2) and thromboxane A2 (TXA2) (measured as their metabolites, 6-oxo-PGF1 alpha and TXB2, respecti...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1981.tb16773.x

    authors： Phillips CA,Poyser NL

    更新日期：1981-05-01 00:00:00

  • Primary porcine enterocyte and hepatocyte cultures to study drug oxidation reactions.

    abstract：:1. Primary porcine hepatocytes and enterocytes were isolated and cultured in Williams' E medium for up to 10 days to investigate potential organ differences in the metabolism of the immunosuppressive compound tacrolimus (FK 506) and of two investigational drugs (KC11346 and KC12291). Using LC-MS (FK506) and HPLC-FL (K...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703062

    authors： Bader A,Hansen T,Kirchner G,Allmeling C,Haverich A,Borlak JT

    更新日期：2000-01-01 00:00:00

  • Inhibition of neutrophil and monocyte recruitment by endogenous and exogenous lipocortin 1.

    abstract：:1. The role played by endogenous lipocortin 1 in the anti-migratory action exerted by dexamethasone (Dex) on monocyte recruitment in an in vivo model of acute inflammation was investigated by use of several neutralizing polyclonal antibodies raised against lipocortin 1 or a lipocortin 1-derived N-terminus peptide (pep...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0701029

    authors： Getting SJ,Flower RJ,Perretti M

    更新日期：1997-03-01 00:00:00

  • The use of low concentrations of divalent cations to demonstrate a role for N-methyl-D-aspartate receptors in synaptic transmission in amphibian spinal cord.

    abstract：:1 Synaptic potentials and the responses of frog spinal cord to various acidic amino acids were examined by means of the sucrose gap recording technique. 2 Divalent cations (50-250 microM) specifically antagonized responses evoked at N-methyl-D-aspartate (NMDA) receptors by N-methyl D,L aspartic acid (NMDLA). The rank ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1982.tb09306.x

    authors： Smith PA

    更新日期：1982-10-01 00:00:00

  • The action of Hoe 140 on the bradykinin-induced splenic pressor reflex of the anaesthetized cat.

    abstract：:1. Intrasplenic injection of bradykinin (BK) induced a dose-dependent pressor response in the anaesthetized cat, with an ED50 of 0.98 +/- 0.43 nmol. In contrast, intrasplenic administration of desArg9bradykinin (desArg9BK) was without significant effect at doses of up to 200 nmol. 2. Intravenously administered BK indu...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1993.tb13962.x

    authors： Louttit JB,Coleman RA

    更新日期：1993-12-01 00:00:00

  • Clinical and preclinical evidence of somatosensory involvement in amyotrophic lateral sclerosis.

    abstract：:Amyotrophic lateral sclerosis (ALS) is the most common motor neuron neurodegenerative disease. Although it has been classically considered as a disease limited to the motor system, there is increasing evidence for the involvement of other neural and non-neuronal systems. In this review, we will discuss currently exist...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/bph.15202

    authors： Riancho J,Paz-Fajardo L,López de Munaín A

    更新日期：2020-07-16 00:00:00

  • Inhibitory effects of certain enantiomeric cannabinoids in the mouse vas deferens and the myenteric plexus preparation of guinea-pig small intestine.

    abstract：:1. The psychoactive cannabinoids (-)-delta 9-tetrahydrocannabinol ((-)-delta 9-THC) and the 1,1-dimethyl-heptyl homologue of (-)-11-hydroxy-delta 8-tetrahydrocannabinol ((-)-DMH) both inhibited electrically-evoked contractions of the mouse isolated vas deferens and the myenteric plexus-longitudinal muscle preparation ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb09088.x

    authors： Pertwee RG,Stevenson LA,Elrick DB,Mechoulam R,Corbett AD

    更新日期：1992-04-01 00:00:00

  • A toxin from the spider Phoneutria nigriventer that blocks calcium channels coupled to exocytosis.

    abstract：:1. The aim of the present experiments was to investigate the pharmacological action of a toxin from the spider Phoneutria nigriventer, Tx3-3, on the function of calcium channels that control exocytosis of synaptic vesicles. 2. Tx3-3, in confirmation of previous work, diminished the intracellular calcium increase induc...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0701381

    authors： Guatimosim C,Romano-Silva MA,Cruz JS,Beirão PS,Kalapothakis E,Moraes-Santos T,Cordeiro MN,Diniz CR,Gomez MV,Prado MA

    更新日期：1997-10-01 00:00:00

  • Pro-oxidant effects of Ecstasy and its metabolites in mouse brain synaptosomes.

    abstract：BACKGROUND AND PURPOSE:3,4-Methylenedioxymethamphetamine (MDMA or 'Ecstasy') is a worldwide major drug of abuse known to elicit neurotoxic effects. The mechanisms underlying the neurotoxic effects of MDMA are not clear at present, but the metabolism of dopamine and 5-HT by monoamine oxidase (MAO), as well as the hepati...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2011.01453.x

    authors： Barbosa DJ,Capela JP,Oliveira JM,Silva R,Ferreira LM,Siopa F,Branco PS,Fernandes E,Duarte JA,de Lourdes Bastos M,Carvalho F

    更新日期：2012-02-01 00:00:00

  • Inositol phospholipid hydrolysis in human brain; adenosine inhibition of the response to histamine.

    abstract：:1. Inositol phospholipid hydrolysis was examined in human cerebral cortex slices by a [3H]-inositol prelabelling assay. 2. Enhancement of [3H]-inositol phosphates accumulation was observed in the presence of carbachol, noradrenaline, histamine, 5-hydroxytryptamine (5-HT) and depolarizing concentrations of KCl. 3. Desp...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1990.tb12048.x

    authors： Kendall DA,Firth JL

    更新日期：1990-05-01 00:00:00

  • Aspirin at therapeutic concentrations does not affect 5-hydroxytryptamine uptake by platelets.

    abstract：:Aspirin at therapeutic concentrations does not inhibit the uptake of 5-hydroxytryptamine (5-HT) by blood platelets nor induce release of 5-HT from platelets, although platelet aggregation responses to collagen and arachidonic acid (which are dependent on platelet prostaglandin synthesis) are abolished. This does not s...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1977.tb07735.x

    authors： Drummond AH,MacIntyre DE,Olverman HJ

    更新日期：1977-04-01 00:00:00

  • The effects of combined angiotensin converting enzyme inhibition and beta-adrenoceptor blockade on plasma renin activity in anaesthetized dogs.

    abstract：:1. The effects of beta-adrenoceptor blockade on the changes in plasma renin activity (PRA) following angiotensin enzyme (ACE) inhibition were investigated in pentobarbitone-chloralose anaesthetized dogs. 2. ACE-inhibition, with enalapril (2 mg kg-1), caused a significant reduction in systemic arterial blood pressure (...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb14338.x

    authors： Cambridge D,Whiting MV,Butterfield LJ,Allan G

    更新日期：1992-06-01 00:00:00

  • A cerebral nitrergic pathway modulates endotoxin-induced changes in gastric motility.

    abstract：:1. This study analyses the neural pathway involved in the modulation of gastric motor function by stress. 2. Systemic administration of low doses of endotoxin (40 microg kg(-1), i.v.) prevents the increase in gastric tone induced by 2-deoxy-D-glucose (200 mg kg(-1), i.v., 2-DG) in urethane-anaesthetized rats. 3. Funct...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704258

    authors： Quintana E,García-Zaragozá E,Martínez-Cuesta MA,Calatayud S,Esplugues JV,Barrachina MD

    更新日期：2001-09-01 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