当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Effects of methylnaltrexone on morphine-induced inhibition of contraction in isolated guinea-pig ileum and human intestine.

Effects of methylnaltrexone on morphine-induced inhibition of contraction in isolated guinea-pig ileum and human intestine.

Abstract：

:We investigated the effects of methylnaltrexone on morphine-induced inhibition of smooth muscle-strip contraction in isolated guinea-pig ileum and human small intestine. The longitudinal muscle-strip was immersed in a temperature-controlled (37 degrees C) bath containing a physiological solution of 95% O2 and 5% CO2 with pH 7.4. Muscle contraction was elicited by transmural electrical stimulation with a pulse duration of 0.5 ms at frequencies of 1-50 Hz for 5-10 s at 1-3-min intervals. Muscle contraction was blocked by tetrodotoxin or atropine in both preparations. When methylnaltrexone was applied to the bath, the force produced by muscle contraction was enhanced up to approximately 30%. Stimulation-elicited muscle contraction was inhibited by morphine, which decreased the force of contraction 42 +/- 9.5% (S.D.) in the human intestine preparation and 35 +/- 8.6% in guinea-pig ileum at the inhibitory concentration 70% (IC70). Methylnaltrexone effectively antagonized the effects of morphine-induced inhibition of muscle-strip contraction. In the guinea-pig ileum preparation, methylnaltrexone at 30, 100 and 300 nM blocked 25 +/- 10.5%, 74 +/- 7.2% and 89 +/- 9.9% of morphine-induced (300 nM) inhibition, respectively. In the human intestine preparation, methylnaltrexone at the same concentrations blocked 57 +/- 10.9%, 74 +/- 12.9% and 92 +/- 7.2% of morphine-induced (100 nM) inhibition, respectively. The relative ratio of methylnaltrexone to morphine was higher in human intestine (1:1) than in the guinea-pig ileum preparation (1:3). These data provide preliminary information for clinical studies to evaluate the efficacy of methylnaltrexone in preventing or reducing morphine-induced antimotility and antitransit actions.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Yuan CS,Foss JF,Moss J

doi

10.1016/0014-2999(95)00018-g

subject

Has Abstract

pub_date

1995-03-24 00:00:00

pages

107-11

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(95)00018-G

journal_volume

276

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • Down-regulation of miR-204 attenuates endothelial-mesenchymal transition by enhancing autophagy in hypoxia-induced pulmonary hypertension.

    abstract：:Pulmonary arterial remodeling is a crucial cause of increased pulmonary artery pressure during pulmonary hypertension (PH). Recently, growing evidence has upheld the contribution of endothelial-mesenchymal transition (EndMT) to pulmonary arterial remodeling, but the underlying mechanisms remain largely unaddressed. mi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2019.172673

    authors： Liu T,Zou XZ,Huang N,Ge XY,Yao MZ,Liu H,Zhang Z,Hu CP

    更新日期：2019-11-15 00:00:00

  • Intravenously injected CDP-choline increases blood pressure and reverses hypotension in haemorrhagic shock: effect is mediated by central cholinergic activation.

    abstract：:Intravenous (i.v.) administration of cytidine-5'-diphosphate choline (CDP-choline) (100, 250 and 500 mg/kg) increased blood pressure in normal rats and reversed hypotension in haemorrhagic shock. Choline (54 mg/kg; i.v.), at the dose equimolar to 250 mg/kg CDP-choline decreased blood pressure of rats in both condition...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(03)01602-9

    authors： Savci V,Goktalay G,Cansev M,Cavun S,Yilmaz MS,Ulus IH

    更新日期：2003-05-09 00:00:00

  • An asparagine residue regulating conductance through P2X2 receptor/channels.

    abstract：:Single channel currents were recorded from Xenopus oocytes expressing wild-type and mutated P2X2 receptors. When 100 mM Na+ was used as the permeant cation, unitary currents of about 80 pS were recorded from the oocyte expressing the wild-type channels. The single channel conductance was roughly halved when Asn333 was...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00207-6

    authors： Nakazawa K,Inoue K,Ohno Y

    更新日期：1998-04-17 00:00:00

  • Comparative effects of K+ channel blockade on the vasorelaxant activity of cromakalim, pinacidil and nicorandil.

    abstract：:Three agents with K+ channel blocking activity, procaine, 4-aminopyridine (4-AP) and tetraethylammonium (TEA), were tested for inhibition of vasorelaxation and 86Rb+ efflux induced by cromakalim (BRL 34915), pinacidil and nicorandil in rabbit isolated mesenteric artery. The potency order for inhibition of vasorelaxati...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(88)90728-5

    authors： Wilson C,Coldwell MC,Howlett DR,Cooper SM,Hamilton TC

    更新日期：1988-08-02 00:00:00

  • Comparison of short-term administration of sertindole, clozapine and haloperidol on the inactivation of midbrain dopamine neurons in the rat.

    abstract：:The present study describes the effect of sertindole, clozapine and haloperidol on the number of spontaneously active dopamine neurons in ventral tegmental area and substantia nigra pars compacta after daily oral treatment for 1, 2 or 3 weeks. In general, daily administration of high dosages (sertindole: 2.8 mumol/kg/...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(94)90468-5

    authors： Skarsfeldt T

    更新日期：1994-03-21 00:00:00

  • Anti-thrombin action of low-dose acetylsalicylic acid.

    abstract：:It is known that low-dose aspirin is effective in coronary artery therapy, although it has not yet been clarified how it exerts its action. Here, we report that treatment of coronary artery patients with 100 mg/day of aspirin does not attenuate thrombin generation, but reduces free thrombin by favouring the formation ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(02)02925-4

    authors： Di Micco B,Colonna G,Di Micco P,Di Micco G,Russo BM,Macalello MA,Ragone R

    更新日期：2003-01-26 00:00:00

  • Antinociceptive effects induced through the stimulation of spinal cannabinoid type 2 receptors in chronically inflamed mice.

    abstract：:The stimulation of spinal cannabinoid type 2 (CB(2)) receptors is a suitable strategy for the alleviation of experimental pain symptoms. Several reports have described the up-regulation of spinal cannabinoid CB(2) receptors in neuropathic settings together with the analgesic effects derived from their activation. Besi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2011.06.057

    authors： Curto-Reyes V,Boto T,Hidalgo A,Menéndez L,Baamonde A

    更新日期：2011-10-01 00:00:00

  • Role of Cl(-) channels in alpha-adrenoceptor-mediated vasoconstriction in the anesthetized rat.

    abstract：:In vitro studies have provided evidence that Cl(-) ion currents are important for activation of vascular smooth muscle contraction. The stilbene, 4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS), disrupts Cl(-) metabolism by blocking Cl(-) channels and by inhibiting Cl(-) bicarbonate exchange. The aims of thi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(00)00471-4

    authors： Lamb FS,Kooy NW,Lewis SJ

    更新日期：2000-08-11 00:00:00

  • Terfenadine induces thymocyte apoptosis via mitochondrial pathway.

    abstract：:The treatment of rat thymocytes with 10 microM terfenadine resulted in a significant increase in DNA fragmentation. The DNA fragmentation induced by terfenadine was dependent on its concentration and incubation time. In terfenadine-treated cells, the translocation of phosphatidylserine from the inside of plasma membra...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2004.05.048

    authors： Enomoto R,Komai T,Yoshida Y,Sugahara C,Kawaguchi E,Okazaki K,Kinoshita H,Komatsu H,Konishi Y,Lee E

    更新日期：2004-08-02 00:00:00

  • Combined oral contraceptives modify the effect of smoking on inflammatory cellular indexes and endothelial function in healthy subjects.

    abstract：:Little information is available on the influence of sex in combination with smoking habits and combined oral contraceptives (COC) use on cellular inflammatory indexes such as neutrophil/lymphocyte ratio (NLR), derived NRL (dNLR), platelet/lymphocyte ratio (PLR), monocyte/lymphocyte ratio (MLR), mean platelet volume/pl...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.173762

    authors： Campesi I,Montella A,Sotgiu G,Dore S,Carru C,Zinellu A,Palermo M,Franconi F

    更新日期：2021-01-15 00:00:00

  • Galantamine (Reminyl) delays cardiac ventricular repolarization and prolongs the QT interval by blocking the HERG current.

    abstract：:Galantamine is a reversible inhibitor of acetylcholinesterase and an allosteric-potentiating ligand of the nicotinic acetylcholine receptors. It is used for treating mild-to-moderate Alzheimer's disease. Interestingly, QT interval prolongation on the electrocardiogram (ECG), malignant ventricular arrhythmias and synco...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2012.02.002

    authors： Vigneault P,Bourgault S,Kaddar N,Caillier B,Pilote S,Patoine D,Simard C,Drolet B

    更新日期：2012-04-15 00:00:00

  • The influence of gastric pentadecapeptide BPC 157 on acute and chronic ethanol administration in mice.

    abstract：:The stable gastric pentadecapeptide BPC 157 (GEPPPGKPADDAGLV, M.W.1419), which was promising in inflammatory bowel disease (PL-10, PLD-116, PL-14736, Pliva) trials, protects against both acute and chronic alcohol-induced lesions in stomach and liver, but also, given peripherally, affects various centrally mediated dis...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2004.07.112

    authors： Blagaic AB,Blagaic V,Romic Z,Sikiric P

    更新日期：2004-09-24 00:00:00

  • Some effects of disopyramide and its N-dealkylated metabolite on isolated nerve and cardiac muscle.

    abstract：:In animals and man the antidysrhythmic agent disopyramide in primarily metabolised by mono-N-dealkylation. The effects of disopyramide and its N-dealkylated metabolite (MIP) have been investigated using isolated cardiac and nervous tissue, and their effects have been compared with the effects of other antidysrhythmic ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(78)90313-8

    authors： Grant AM,Marshall RJ,Ankier SI

    更新日期：1978-06-15 00:00:00

  • Transfection of PDCD5 sensitizes colorectal cancer cells to cisplatin-induced apoptosis in vitro and in vivo.

    abstract：:This study was purposed to explore the mechanism of augmenting apoptosis-inducing effects of cisplatin on colorectal cancer SW480 cells by stable transfection of Programmed Cell Death 5 (PDCD5) gene, both in vitro and in vivo. The expression level of PDCD5 of SW480 cells stably transfected with PDCD5 (SW480/PDCD5) and...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2010.09.040

    authors： Yin A,Jiang Y,Zhang X,Zhao J,Luo H

    更新日期：2010-12-15 00:00:00

  • Quantitative autoradiography of [3H]piquindone binding sites (dopamine D2 receptors) in rat brain.

    abstract：:(-)Piquindone is a new antipsychotic pyrroloisoquinoline derivative that binds to dopamine D2 receptors. We used in vitro quantitative autoradiography to determine the distribution of [3H](-)piquindone binding sites in rat forebrain. [3H](-)Piquindone binding to brain slices was sodium dependent, saturable and of high...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(86)90259-1

    authors： Nock B,Sedvall G,Mcewen BS

    更新日期：1986-03-04 00:00:00

  • Enhancement of bone morphogenetic protein-2 expression and bone formation by coumarin derivatives via p38 and ERK-dependent pathway in osteoblasts.

    abstract：:Osteoporosis is a reduction in skeletal mass due to an imbalance between bone resorption and bone formation. Bone morphogenetic protein (BMP) plays important roles in osteoblastic differentiation and bone formation. Therefore, components involved in BMP activation are good targets for the development of anti-osteoporo...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2007.10.013

    authors： Tang CH,Yang RS,Chien MY,Chen CC,Fu WM

    更新日期：2008-01-28 00:00:00

  • Upscaling of a living membrane for bioartificial kidney device.

    abstract：:The limited removal of metabolic waste products in dialyzed kidney patients leads to high morbidity and mortality. One powerful solution for a more complete removal of those metabolites might be offered by a bioartificial kidney device (BAK), which contains a hybrid "living membrane" with functional proximal tubule ep...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.07.009

    authors： Chevtchik NV,Fedecostante M,Jansen J,Mihajlovic M,Wilmer M,Rüth M,Masereeuw R,Stamatialis D

    更新日期：2016-11-05 00:00:00

  • Expression of multidrug resistance protein 4 and 5 in the porcine coronary and pulmonary arteries.

    abstract：:Guanosine 3',5'-cyclic monophosphate (cGMP) has an important role in regulating vascular smooth muscle tone. We examined whether mRNA for multidrug resistance protein (MRP) 4 and MRP5, which were recently identified as ATP-dependent export pumps for cyclic nucleotides, is expressed in the porcine coronary and pulmonar...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(03)01552-8

    authors： Mitani A,Nakahara T,Sakamoto K,Ishii K

    更新日期：2003-04-11 00:00:00

  • Amygdalar neuropeptide Y Y1 receptors mediate the anxiolytic-like actions of neuropeptide Y in the social interaction test.

    abstract：:The effects of intra-amygdalar neuropeptide Y infusions were assessed in rats using the social interaction test. Neuropeptide Y administered into the central nucleus of the amygdala did not alter behavior, while injections into the basolateral nucleus of the amygdala produced an increased social interaction time. Furt...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(99)00018-7

    authors： Sajdyk TJ,Vandergriff MG,Gehlert DR

    更新日期：1999-03-05 00:00:00

  • Comparison of the effects of several calcium antagonistic drugs on the electrical activity of guinea pig Purkinje fibers.

    abstract：:The effects of several slow channel blockers were compared on the normal fast action potentials (APs) and the slow APs of guinea pig Purkinje fibers. In spontaneously-firing Purkinje fibers perfused with normal Tyrode solution, mesudipine (analog of nifedipine) at 10(-7) and 10(-6) M, had no significant effect on the ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(83)90007-9

    authors： Molyvdas PA,Sperelakis N

    更新日期：1983-03-25 00:00:00

  • The ligand binding ability of dopamine D1 receptors synthesized using a wheat germ cell-free protein synthesis system with liposomes.

    abstract：:G-protein coupled receptors (GPCRs) share a common seven-transmembrane topology and mediate cellular responses to a variety of extracellular signals. However, structural and functional approaches to GPCRs have often been limited by the difficulty of producing a sufficient amount of receptor protein using conventional ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2014.10.011

    authors： Arimitsu E,Ogasawara T,Takeda H,Sawasaki T,Ikeda Y,Hiasa Y,Maeyama K

    更新日期：2014-12-15 00:00:00

  • Studies on the mechanism of the vasodilator effects of prazosin in dogs and rabbits.

    abstract：:In pentobarbital (35.0 mg/kg) anaesthetised dogs, bolus injections of prazosin into the femoral artery (3.0--300.0 microgram) provoked a dose-related fall in the vascular resistance of the innervated hind limb. In contrast to papaverine, prazosin failed to produce the same effect in dogs under spinal anaesthesia even ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(78)90101-2

    authors： Cavero I,Fenard S,Gomeni R,Lefevre F,Roach AG

    更新日期：1978-06-01 00:00:00

  • Naloxone causes apparent antinociception and pronociception simultaneously in the rat paw formalin test.

    abstract：:Naloxone is known to decrease, increase or have no effect on nociceptive thresholds. Here, using two commonly accepted pain-related behaviors (licking and flinching) associated with injection of noxious formalin into a hind paw in rats, naloxone (0.1-1 mg/kg s.c.) simultaneously decreases and increases nociceptive res...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90589-a

    authors： Wheeler-Aceto H,Cowan A

    更新日期：1993-05-19 00:00:00

  • Effect of azelastine on airway hyperresponsiveness mediated by stimulated macrophages.

    abstract：:The effect of the anti-allergic drug azelastine, 4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepine-4-yl)-1-(2H)-phth alazione), on airway hyperresponsiveness induced by immunologically stimulated pulmonary alveolar macrophages was investigated in canine bronchial segments under isometric conditions in vitro. Macroph...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00114-z

    authors： Tamaoki J,Takemura H,Tagaya E,Sakai A,Yamawaki I,Konno K

    更新日期：1995-05-15 00:00:00

  • Psychological co-morbidities in COPD: Targeting systemic inflammation, a benefit for both?

    abstract：:COPD is a chronic lung disease characterized by persistent respiratory symptoms and airflow limitation due to airway and/or alveolar abnormalities. Furthermore, COPD is often characterized by extrapulmonary manifestations and comorbidities worsening COPD progression and quality of life. A neglected comorbidity in COPD...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejphar.2018.10.001

    authors： Pelgrim CE,Peterson JD,Gosker HR,Schols AMWJ,van Helvoort A,Garssen J,Folkerts G,Kraneveld AD

    更新日期：2019-01-05 00:00:00

  • Regulation of ion transport by histamine in mouse cecum.

    abstract：:Histamine levels are elevated in inflammatory bowel disease. We investigated the mechanism by which histamine affects electrolyte transport in the mouse cecum. Using the Ussing-chamber voltage clamp technique, histamine was found to cause a transient concentration-dependent increase in short-circuit current, a measure...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(97)00184-2

    authors： Homaidan FR,Tripodi J,Zhao L,Burakoff R

    更新日期：1997-07-23 00:00:00

  • Differences in the mechanisms for relaxation of aorta induced by 17beta-estradiol or progesterone between normotensive and hypertensive rats.

    abstract：:The tension in isolated ring preparations of the thoracic aorta from Wistar-Kyoto rats (WKY) and spontaneously hypertensive rats (SHR) was measured isometrically to study if there are any differences in the mechanisms of 17beta-estradiol- or progesterone-induced relaxation between WKY and SHR aortic rings. 17beta-Estr...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(03)01858-2

    authors： Unemoto T,Honda H,Kogo H

    更新日期：2003-07-04 00:00:00

  • Effects of selective adenosine A1 and A2 receptor agonists and antagonists on local rates of energy metabolism in the rat brain.

    abstract：:The quantitative [14C]2-deoxyglucose autoradiographic technique was applied to the measurement of the cerebral metabolic effects of adenosine A1 and A2 receptor agonists and antagonists in adult rats. The adenosine A1 receptor agonist and antagonist, 2-chloro-N6-cyclopentyladenosine (CCPA) and 8-cyclopentyl-1,3-diprop...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(94)90057-4

    authors： Nehlig A,Daval JL,Boyet S

    更新日期：1994-06-02 00:00:00

  • Relaxant effects of vasoactive intestinal peptide and bethanechol in cat intrapulmonary artery.

    abstract：:The relaxant actions of vasoactive intestinal peptide (VIP) and bethanechol were examined on ring segments of intrapulmonary artery (IPA) isolated from cat lung. On a molar basis, VIP was 75 times more potent than bethanechol; however, VIP was less efficacious than bethanechol in reversing phenylephrine induced tone. ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(83)90039-0

    authors： Altiere RJ,Diamond L

    更新日期：1983-09-16 00:00:00

  • A possible mechanism of choleretic action of 3-(2,4,5-triethoxybenzoyl)-propionic acid (AA-149) in dogs.

    abstract：:The choleretic action of 3-(2,4,5-triethoxybenzoyl)propionic acid (AA-149) was studied in anesthetized dogs. AA-149 produced a dose-dependent increase of the bile flow with both i.v. and intrajejunal administration of doses 1 mg/kg and higher. Biliary clearance of 14C-erythritol showed that AA-149 stimulated canalicul...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(78)90050-x

    authors： Satoh H,Kanno M,Maki Y

    更新日期：1978-03-01 00:00:00