当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Relaxing effects induced by the soluble guanylyl cyclase stimulator BAY 41-2272 in human and rabbit corpus cavernosum.

Relaxing effects induced by the soluble guanylyl cyclase stimulator BAY 41-2272 in human and rabbit corpus cavernosum.

Abstract：

:5-Cyclopropyl-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-pyrimidin-4-ylamine (BAY 41-2272) is a potent soluble guanylyl cyclase stimulator in a nitric oxide (NO)-independent manner. The relaxant effect of BAY 41-2272 was investigated in rabbit and human corpus cavernosum in vitro. BAY 41-2272 (0.01-10 microM) relaxed both rabbit (pEC(50)=6.82+/-0.06) and human (pEC(50)=6.12+/-0.10) precontracted cavernosal strips. The guanylyl cyclase inhibitor (ODQ, 10 microM) caused significant rightward shifts in the concentration-response curves for BAY 41-2272 in rabbit (4.7-fold) and human (2.3-fold) tissues. The NO synthesis inhibitor (N-nitro-L-arginine methyl ester (L-NAME), 100 microM) also produced similar rightward shifts, revealing that BAY 41-2272 acts synergistically with endogenous NO to elicit its relaxant effect. The results also indicate that ODQ is selective for the NO-stimulated enzyme, since relaxations evoked by BAY 41-2272 were only partly attenuated by ODQ. The present study shows that both BAY 41-2272 and sildenafil evoke relaxations independent of inhibition of haem in soluble guanylate cyclase. Moreover, there is no synergistic effect of the two compounds in corpus cavernosum.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Baracat JS,Teixeira CE,Okuyama CE,Priviero FB,Faro R,Antunes E,De Nucci G

doi

10.1016/j.ejphar.2003.08.012

keywords:

subject

Has Abstract

pub_date

2003-09-12 00:00:00

pages

163-9

issue

2

eissn

0014-2999

issn

1879-0712

pii

S0014299903022064

journal_volume

477

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • A direct relationship between aggressive behavior in the resident/intruder test and cell oxidative status in adult male mice.

    abstract：:Disturbances in oxidative metabolism are involved in many acute and chronic diseases, as well as in several other conditions. The objective of the present study was to examine the relationship between the level of intracellular reactive oxygen species in the peripheral blood granulocytes of mice, as evaluated by 2',7'...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2009.11.001

    authors： Rammal H,Bouayed J,Soulimani R

    更新日期：2010-02-10 00:00:00

  • Phasic activity of urinary bladder smooth muscle in the streptozotocin-induced diabetic rat: effect of potassium channel modulators.

    abstract：:Increased phasic activity in the bladder smooth muscle of animal models and patients with detrusor overactivity has been suggested to underlie the pathophysiology of overactive bladder. Potassium (K+) channels are key regulators of bladder smooth muscle tone and thus may play a role in this altered phasic activity. In...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2011.03.053

    authors： Vahabi B,Lawson K,McKay NG,Sellers DJ

    更新日期：2011-06-25 00:00:00

  • Diabetes-induced DNA damage and apoptosis are associated with poly (ADP ribose) polymerase 1 inhibition in the rat testis.

    abstract：:Molecular mechanisms responsible for diabetes-induced testicular dysfunction are not well understood. This study investigated oxidative stress, stage-dependent DNA base modification and expression of poly (ADP ribose) polymerase 1 (PARP1) in the testes of streptozotocin-induced diabetic rats. Hyperglycemia led to test...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2014.05.005

    authors： Kilarkaje N,Al-Hussaini H,Al-Bader MM

    更新日期：2014-08-15 00:00:00

  • Targeting different angiogenic pathways with combination of curcumin, leflunomide and perindopril inhibits diethylnitrosamine-induced hepatocellular carcinoma in mice.

    abstract：:No effective chemopreventive agent has been approved against hepatocellular carcinoma (HCC) to date. Since HCC is one of the hypervascular solid tumors, blocking angiogenesis represents an intriguing approach to HCC chemoprevention. The aim of the current study was to examine the combined effect of the anti-angiogenic...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2013.11.022

    authors： Nasr M,Selima E,Hamed O,Kazem A

    更新日期：2014-01-15 00:00:00

  • Ifenprodil influences changes in mouse behaviour related to acute and chronic ethanol administration.

    abstract：:The aim of the present study was to examine the influence of ifenprodil (a non-competitive NMDA receptor antagonist which also blocks 5-HT3 receptors and alpha1-adrenoceptors) on the effects of ethanol in the mouse in vivo and to elucidate the role of various receptors in these actions. The ethanol (4 g/kg i.p.)-induc...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(99)00393-3

    authors： Malinowska B,Napiórkowska-Pawlak D,Pawlak R,Buczko W,Göthert M

    更新日期：1999-07-14 00:00:00

  • Oxidation by trace Cu2+ ions underlies the ability of ascorbate to induce vascular dysfunction in the rat perfused mesentery.

    abstract：:Ascorbate has both antioxidant and pro-oxidant activities. We have previously shown that plasma levels of ascorbate induce constriction and blockade of dilatation mediated by endothelium-derived hyperpolarizing factor (EDHF). In this study we sought to determine if these detrimental actions were mediated by a prooxida...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2009.04.033

    authors： Nelli S,Craig J,Martin W

    更新日期：2009-07-01 00:00:00

  • Differential effects of sulfonylurea derivatives on vascular ATP-sensitive potassium channels.

    abstract：:Sulfonylurea drugs exert their insulinotropic action by inhibiting ATP-sensitive potassium channels in the pancreas. However, these channels are also expressed in myocardial and vascular smooth muscle, implicating possible detrimental cardiovascular effects. Aim of the present study was to investigate the inhibitory p...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2012.02.006

    authors： Engbersen R,Masereeuw R,van Gestel MA,Siero HL,Moons MM,Smits P,Russel FG

    更新日期：2012-04-15 00:00:00

  • LncRNA OR3A4 participates in the angiogenesis of hepatocellular carcinoma through modulating AGGF1/akt/mTOR pathway.

    abstract：:Hepatocellular carcinoma (HCC), as the commonest type in liver cancer, is in urgent need for better treatment target due to its high mortality and poor prognosis. The involvement of angiogenesis in HCC has been identified by multiple studies, but the underlying mechanism remains unclear. Long non-coding RNAs (LncRNAs)...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2019.01.049

    authors： Li W,Fu Q,Man W,Guo H,Yang P

    更新日期：2019-04-15 00:00:00

  • Molecular cloning, developmental expression and pharmacological characterization of the CCKB/gastrin receptor in the calf pancreas.

    abstract：:We have cloned the calf predominant pancreatic cholecystokinin B (CCKB)/gastrin receptor cDNA. It encodes a 454 amino acid protein with 90% identity with the CCKB/gastrin receptor cloned in other species and tissues. However, the calf pancreatic CCKB/gastrin receptor contains a pentapeptide cassette within the third i...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00737-7

    authors： Dufresne M,Escrieut C,Clerc P,Le Huerou-Luron I,Prats H,Bertrand V,Le Meuth V,Guilloteau P,Vaysse N,Fourmy D

    更新日期：1996-02-15 00:00:00

  • Effects of adenosine receptor agonists and antagonists on audiogenic seizure-sensible DBA/2 mice.

    abstract：:We have studied the effects of selective and non-selective adenosine receptor agonists and antagonists in audiogenic-seizure-sensitive DBA/2 mice, an animal model of generalized reflex epilepsy. With the exception of the adenosine A3 receptor agonist, N6-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine (IB-MECA), all th...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(99)00132-6

    authors： De Sarro G,De Sarro A,Di Paola ED,Bertorelli R

    更新日期：1999-04-29 00:00:00

  • NMDA receptor 2C subunit is selectively decreased by MK-801 in the entorhinal cortex.

    abstract：:Administration of the non-competitive NMDA receptor antagonist MK-801 (5-methyl-10,11-dihydro-5H-dibenzo[1,d]cyclohepten-5,10-imine) produces paradoxical neurotoxicity in limbic cortical regions which includes the entorhinal cortex. The expression of NMDAR-2C but not -2A, -2B or -2D subunits was significantly decrease...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(96)00933-8

    authors： Lindén AM,Väsäinen J,Wong G,Castrén E

    更新日期：1997-01-14 00:00:00

  • Effect of propofol on calcium homeostasis in hypoxia-reoxygenated neonatal rat cardiomyocytes.

    abstract：:Intracellular Ca2+ overload induced by hypoxia-reoxygenation alters Ca2+ homeostasis, which plays an important role in myocardial cell injury. Even though propofol is known as a radical scavenger with Ca2+ channel blocking properties, little is known about cardioprotective effect associated with Ca2+ homeostasis in ca...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2008.07.027

    authors： Kim HS,Chang WC,Hwang KC,Choi IG,Park WK

    更新日期：2008-10-10 00:00:00

  • 5-HT7, but not 5-HT2B, receptors mediate hypotension in vagosympathectomized rats.

    abstract：:This study evaluated the possible involvement of 5-HT(2B) receptors in long-lasting hypotension to 5-hydroxytryptamine (5-HT), which is predominantly mediated by 5-HT7 receptors, in anaesthetised vagosympathectomized rats. Intravenous injections of 5-HT and 5-carboxamidotryptamine (5-CT) elicited a dose-dependent hypo...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2004.08.050

    authors： Centurión D,Glusa E,Sánchez-López A,Valdivia LF,Saxena PR,Villalón CM

    更新日期：2004-10-19 00:00:00

  • Influence of MK-801 on the anticonvulsant activity of antiepileptics.

    abstract：:MK-801 (a potent non-competitive antagonist of N-methyl-D-aspartic acid-mediated events) in subcutaneous doses of 0.1 and 0.2 mg/kg increased the threshold for electroconvulsions and in doses of 0.0031 and 0.0125 mg/kg enhanced the protective activity of valproate against maximal electroshock-induced convulsions in mi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(91)90582-b

    authors： Urbańska E,Dziki M,Kleinrok Z,Czuczwar SJ,Turski WA

    更新日期：1991-08-06 00:00:00

  • In vivo 'enkephalinase' inhibition by acetorphan in human plasma and CSF.

    abstract：:Thiorphan, the potent inhibitor of 'enkephalinase', has shown some analgesic properties in experimental animals and in man. The possibility that the intravenous infusion of acetorphan, a prodrug of thiorphan (26 micrograms/kg per min for 60 min), can inhibit plasma and cerebrospinal fluid (CSF) enkephalinase in man in...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(86)90094-4

    authors： Spillantini MG,Geppetti P,Fanciullacci M,Michelacci S,Lecomte JM,Sicuteri F

    更新日期：1986-06-05 00:00:00

  • Role of Hypothalamic-Pituitary-Adrenal axis and corticotropin-releasing factor stress system on cue-induced relapse to alcohol seeking.

    abstract：:A large body of evidence has shown that the Corticotropin Releasing Factor (CRF) system, which plays a key role in stress modulation, is deeply involved in relapse to alcohol seeking induced by exposure to stressful events such as foot shock or yohimbine injections. Exposure to environmental cues is also known to be a...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.06.020

    authors： Galesi FL,Ayanwuyi LO,Mijares MG,Cippitelli A,Cannella N,Ciccocioppo R,Ubaldi M

    更新日期：2016-10-05 00:00:00

  • Dopamine dynamics during emotional cognitive processing: Implications of the specific actions of clozapine compared with haloperidol.

    abstract：:Clozapine has improved efficacy relative to typical antipsychotics in schizophrenia treatment, particularly regarding emotional symptoms. However, the mechanisms underlying its therapeutic benefits remain unclear. Using a methamphetamine-sensitised rat model, we measured changes in dopamine levels in the amygdalae in ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.04.013

    authors： Kawano M,Oshibuchi H,Kawano T,Muraoka H,Tsutsumi T,Yamada M,Inada K,Ishigooka J

    更新日期：2016-06-15 00:00:00

  • Suppression by cetirizine of pleurisy triggered by antigen in actively sensitized rats.

    abstract：:The efficacy of cetirizine in comparison with meclizine, another piperazine H1 receptor antagonist, in rat pleurisy caused by allergen or autacoid was investigated. Sensitization was achieved by subcutaneous injection of a mixture of ovalbumin and aluminium hydroxide. Fourteen days later, the animals were challenged w...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(92)90811-h

    authors： Pasquale CP,e Silva PM,Lima MC,Diaz BL,Rihoux JP,Vargaftig BB,Cordeiro RS,Martins MA

    更新日期：1992-11-13 00:00:00

  • Species-specific binding of transformed Ah receptor to a dioxin responsive transcriptional enhancer.

    abstract：:The Ah receptor (AhR) mediates many, if not all, of the toxic and biological effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, dioxin) and related halogenated aromatic hydrocarbons. Although wide variations in species sensitivity to these compounds have been observed, numerous biochemical and physiochemical charac...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0926-6917(92)90016-6

    authors： Bank PA,Yao EF,Phelps CL,Harper PA,Denison MS

    更新日期：1992-09-01 00:00:00

  • Ketotifen inhibits paf-acether biosynthesis and beta-hexosaminidase release in mouse mast cells stimulated with antigen.

    abstract：:Acetyl-CoA acetyltransferase (1-O-alkyl-sn-glycero-3-phosphocholine) is a key enzyme in paf-acether biosynthesis. Its immunological activation as related to paf-acether formation was investigated in mast cells derived from mouse bone marrow. The action of ketotifen, a prophylactic anti-asthma drug, on the antigen-indu...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(87)90511-5

    authors： Joly F,Bessou G,Benveniste J,Ninio E

    更新日期：1987-12-01 00:00:00

  • Reserpine-induced locomotor stimulation in mice chronically treated with typical and atypical antidepressants.

    abstract：:Previous studies have shown that chronic treatment with antidepressants (AD) leads to an increased responsiveness of NA systems to noradrenaline (NA) or its agonist. In the present paper the influence is described of a prolonged treatment with AD of different pharmacological profiles on the effect of reserpine in the ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(83)90087-0

    authors： Maj J,Rogóz Z,Skuza G,Sowińska H

    更新日期：1983-03-04 00:00:00

  • Human brain imidazoline receptors: further characterization with [3H]clonidine.

    abstract：:The aim of the present study was to further characterize [3H]clonidine binding in the ventrolateral medulla of the human brainstem, the region involved in the vasodepressor effect of imidazoline drugs of the clonidine type. Under basal conditions, [3H]clonidine can bind both to the imidazoline receptors and to the alp...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0922-4106(94)90205-4

    authors： Bricca G,Greney H,Zhang J,Dontenwill M,Stutzmann J,Belcourt A,Bousquet P

    更新日期：1994-01-01 00:00:00

  • Proanaphylactic action of morphine is mediated through a central cholinergic mechanism.

    abstract：:Intracerebroventricular (i.c.v.) or intravenous (i.v.) administration of morphine (10 micrograms or 25 mg/kg, respectively) increased the mortality rate in experimental anaphylaxis in mice. This effect was blocked by the opiate antagonist naltrexone administered systemically (5 mg/kg) or i.c.v. (10 micrograms). Moreov...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(83)90274-1

    authors： Amir S

    更新日期：1983-11-11 00:00:00

  • Targeting CD52 does not affect murine neuron and microglia function.

    abstract：:The humanized anti-CD52 antibody alemtuzumab is successfully used in the treatment of multiple sclerosis (MS) and is thought to exert most of its therapeutic action by depletion and repopulation of mainly B and T lymphocytes. Although neuroprotective effects of alemtuzumab have been suggested, direct effects of anti-C...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.172923

    authors： Ellwardt E,Vogelaar CF,Maldet C,Schmaul S,Bittner S,Luchtman D

    更新日期：2020-03-15 00:00:00

  • Platycodin D alleviates liver fibrosis and activation of hepatic stellate cells by regulating JNK/c-JUN signal pathway.

    abstract：:Liver fibrosis is involved in the progression of most chronic liver diseases. Even though we have made a huge progress in order to understand the pathogenesis of liver fibrosis, however, there is still a lack of productive treatments. Being a traditional Chinese medicine, Platycodin D (PD), an oleanane kind of triterp...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.172946

    authors： Liu YM,Cong S,Cheng Z,Hu YX,Lei Y,Zhu LL,Zhao XK,Mu M,Zhang BF,Fan LD,Yu L,Cheng ML

    更新日期：2020-06-05 00:00:00

  • Ex vivo studies after oral treatment of the beagle with dihydroergotamine.

    abstract：:Plasma concentrations of unchanged dihydroergotamine (DHE) were measured in beagle dogs on days 1 and 7 of a 1 week treatment with daily oral doses of DHE. Responses to both 5-HT and noradrenaline were monitored isometrically on spiral strips from saphenous arteries and femoral veins removed 24 and 72 h after the last...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(83)90601-5

    authors： Müller-Schweinitzer E,Rosenthaler J

    更新日期：1983-04-22 00:00:00

  • Studies on the H2-receptor antagonism of MK-208 in isolated rabbit gastric glands.

    abstract：:Using isolated rabbit gastric glands, the H2-receptor antagonist MK-208 was investigated with respect to its effects on [14C]aminopyrine uptake as an index of gastric acid secretion. In addition to shifting the histamine concentration-response curve to the right in a parallel fashion, the antagonism produced by MK-208...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(84)90733-7

    authors： Shepherd-Rose AJ,Pendleton RG

    更新日期：1984-11-13 00:00:00

  • Calcium dependence of ouabain-induced contraction in aortas from spontaneously hypertensive rats.

    abstract：:The calcium sensitivity of ouabain-induced contractions of aortic strips from spontaneously hypertensive rat (SHR) was examined using several drugs which affect Na+ and Ca2+ movements across the cell membrane, and the results were compared with those obtained with age-matched Wistar-Kyoto rat (WKY). The Ca2+ concentra...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(90)94121-d

    authors： Shibata R,Morita S,Nagai K,Miyata S,Iwasaki T

    更新日期：1990-11-06 00:00:00

  • Origin of ATP release in the rat vas deferens: concomitant measurement of [3H]noradrenaline and [14C]ATP.

    abstract：:High pressure liquid chromatography (HPLC) combined with radiochemical detection was used to show that [3H]noradrenaline (NA) and [14C]ATP were released concomitantly during field stimulation of the rat vas deferens. The release of radioactivity (3H and 14C) in response to three consecutive field stimulations was cons...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(88)90254-3

    authors： Vizi ES,Burnstock G

    更新日期：1988-12-06 00:00:00

  • The neuronal KCNQ channel opener retigabine inhibits locomotor activity and reduces forebrain excitatory responses to the psychostimulants cocaine, methylphenidate and phencyclidine.

    abstract：:Many central stimulating drugs have a pronounced stimulatory effect on striatal and cortical activity which is associated to enhanced function of mesencephalic dopaminergic neurons. Mesencephalic KCNQ (also termed K(v)7) potassium channels suppress the basal activity of dopaminergic neurons in the substantia nigra and...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2007.05.029

    authors： Hansen HH,Andreasen JT,Weikop P,Mirza N,Scheel-Krüger J,Mikkelsen JD

    更新日期：2007-09-10 00:00:00