A novel 5-HT3 receptor agonist, YM-31636, increases gastrointestinal motility without increasing abdominal pain.

Abstract:

:We examined the effects of YM-31636 (2-(1H-imidazol-4-ylmethyl)-8H-indeno[1,2-d]thiazole monofumarate), a novel 5-HT3 receptor agonist, on gastrointestinal functions including visceral pain reflex in rats. Injection of YM-31636 increased the number of fecal pellets. This effect was completely inhibited by ramosetron, a 5-HT3 receptor antagonist. YM-31636 also increased the intracolonic pressure measured in both conscious and anesthetized rats. In isolated distal colon, YM-31636 increased the short-circuit current response. This effect was abolished by ramosetron. Both the maximal response and the potency of YM-31636 were weaker than those of other 5-HT3 receptor agonists. In two visceral pain reflex models, YM-31636 neither changed the magnitude of pressor response to colonic distension in anesthetized rats nor affected the visceromotor threshold to colorectal distension in conscious rats. In conclusion, YM-31636 facilitated defecation without increasing visceral pain. Consequently, 5-HT3 receptor agonists like YM-31636 would be promising in the treatment of chronic constipation.

journal_name

Eur J Pharmacol

authors

Kiso T,Ito H,Miyata K,Kamato T,Naitoh Y,Iwaoka K,Yamaguchi T

doi

10.1016/s0014-2999(01)01425-x

keywords:

subject

Has Abstract

pub_date

2001-11-09 00:00:00

pages

35-41

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(01)01425-X

journal_volume

431

pub_type

杂志文章
  • A role for nitric oxide in the anti-ulcer activity of calcitonin gene-related peptide.

    abstract::The anti-ulcer activity of calcitonin gene-related peptide (CGRP) was inhibited, in a dose-dependent manner, by pretreatment with NG-nitro-L-arginine methyl ester, an inhibitor of nitric oxide synthase. Our results suggest that endogenous nitric oxide is involved in the anti-ulcer activity of CGRP. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90252-6

    authors: Clementi G,Caruso A,Prato A,De Bernardis E,Fiore CE,Amico-Roxas M

    更新日期:1994-04-21 00:00:00

  • MK-801 powerfully protects against N-methyl aspartate neurotoxicity.

    abstract::Using the ex vivo chick embryo retina to study the efficacy of antagonists in blocking the excitotoxic effects of excitatory amino acid agonists, we previously identified phencyclidine as the most powerful known anti-excitotoxin. Here we show that MK-801 is 5 times more powerful than phencyclidine as an anti-excitotox...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90552-8

    authors: Olney J,Price M,Salles KS,Labruyere J,Frierdich G

    更新日期:1987-09-23 00:00:00

  • Comparison of the antiplatelet effect of YM337 and abciximab in rhesus monkeys.

    abstract::We directly compared the effects of YM337, the Fab fragment of the humanized monoclonal antibody C4G1, on platelet aggregation and template bleeding time with those of abciximab, the Fab fragment of the human/murine chimeric monoclonal antibody 7E3, in rhesus monkeys. The duration of inhibition of platelet aggregation...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(97)01241-7

    authors: Suzuki K,Sakai Y,Hisamichi N,Taniuchi Y,Sato K,Terazaki C,Kaku S,Kawasaki T,Yano S,Inagaki O,Masuho Y

    更新日期:1997-10-08 00:00:00

  • Enhanced activity of the brain beta-endorphin system by free-choice ethanol drinking in C57BL/6 but not DBA/2 mice.

    abstract::The objective of the present studies was to investigate the effect of voluntary ethanol consumption for 21 days on the brain beta-endorphin system of C57BL/6 (alcohol-preferring) and DBA/2 (alcohol-avoiding) strains of mice. As expected, C57BL/6 mice consumed a significantly higher quantity of the 10% ethanol solution...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90064-7

    authors: De Waele JP,Gianoulakis C

    更新日期:1994-06-02 00:00:00

  • Role of oxidative stress, inflammation, nitric oxide and transforming growth factor-beta in the protective effect of diosgenin in monocrotaline-induced pulmonary hypertension in rats.

    abstract::Pulmonary hypertension is a progressive disease of various origins that is associated with right ventricular dysfunction. In the present study, the protective effect of diosgenin was investigated in monocrotaline-induced pulmonary hypertension in rats. Pulmonary hypertension was induced by a single subcutaneous inject...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.07.026

    authors: Ahmed LA,Obaid AA,Zaki HF,Agha AM

    更新日期:2014-10-05 00:00:00

  • HOE 140, a new highly potent and long-acting bradykinin antagonist in conscious rats.

    abstract::The inhibitory effects of the new bradykinin antagonist HOE 140 (D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg) on depressor responses to exogenous bradykinin were investigated in conscious rats and compared with those of the bradykinin antagonist B4146 (D-Arg-Hyp-Pro-Gly-Thi-Ser-D-Pro-Thi-Arg). HOE 140 showed a 250-700...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90684-i

    authors: Bao G,Qadri F,Stauss B,Stauss H,Gohlke P,Unger T

    更新日期:1991-07-23 00:00:00

  • Coronary response to diadenosine tetraphosphate after ischemia-reperfusion in the isolated rat heart.

    abstract::Diadenosine tetraphosphate (AP4A) is a vasoactive mediator that may be released from platelet granules and that may reach higher plasma concentrations during coronary ischemia-reperfusion. The objective of this study was to analyze its coronary effects in such conditions. To this, rat hearts were perfused in a Langend...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.04.006

    authors: García-Villalón AL,Fernández N,Monge L,Diéguez G

    更新日期:2011-06-25 00:00:00

  • Displacement of RTI-55 from the dopamine transporter by cocaine.

    abstract::The cocaine analog 3 beta-(4-iodophenyl)tropane-2 beta-carboxylic acid methyl ester (RTI-55 or beta CIT) has a higher affinity for the dopamine transporter and may be potentially useful in interfering with cocaine's actions in brain. However, imaging studies have demonstrated displacement of tracer doses of [123I]RTI-...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00698-2

    authors: Gatley SJ,Volkow ND,Chen R,Fowler JS,Carroll FI,Kuhar MJ

    更新日期:1996-01-25 00:00:00

  • Effects of hemicholinium-3 or physostigmine on rat brain noradrenaline depletion induced by foot shocks.

    abstract::Foot shocks applied to the rat on a grid floor caused brain noradrenaline depletion. Hemicholinium-3 injected intracerebroventricularly (i.c.v.) blocked the noradrenaline depletion and this blockade was reversed by choline (i.c.v.). Physostigmine (i.c.v.) had different effects according to the age of the rats: "young"...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90067-x

    authors: Campos HA,Romero E

    更新日期:1977-08-01 00:00:00

  • Ubiquinol rescues simvastatin-suppression of mitochondrial content, function and metabolism: implications for statin-induced rhabdomyolysis.

    abstract::Statin medications diminish cholesterol biosynthesis and are commonly prescribed to reduce cardiovascular disease. Statins also reduce production of ubiquinol, a vital component of mitochondrial energy production; ubiquinol reduction may contribute to rhabdomyolysis. Human rhabdomyosarcoma cells were treated with eith...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.04.009

    authors: Vaughan RA,Garcia-Smith R,Bisoffi M,Conn CA,Trujillo KA

    更新日期:2013-07-05 00:00:00

  • Influence of peptides on reduced response of rats to electric footshock after acute administration of morphine.

    abstract::Acute treatment of rats with morphine (10 mg/kg) resulted in a marked reduction of motor response to inescapable electric footshock (EFS). Nalorphine (2mg/kg) antagonized this action of morphine. Pretreatment with synthetic ACTH 1-24 (10 IU) 60 min prior to testing also inhibited this morphine-induced reduction, where...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(75)90143-0

    authors: Gispen WH,Van Wimersma Greidanus TB,Waters-Ezrin C,Zimmermann E,Krivoy WA,De Wied D

    更新日期:1975-08-01 00:00:00

  • Protective effects of l-carnitine and piracetam against mitochondrial permeability transition and PC3 cell necrosis induced by simvastatin.

    abstract::Mitochondrial oxidative stress followed by membrane permeability transition (MPT) has been considered as a possible mechanism for statins cytotoxicity. Statins use has been associated with reduced risk of cancer incidence, especially prostate cancer. Here we investigated the pathways leading to simvastatin-induced pro...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.01.001

    authors: Costa RA,Fernandes MP,de Souza-Pinto NC,Vercesi AE

    更新日期:2013-02-15 00:00:00

  • Presynaptic depression of inhibitory postsynaptic potentials by metabotropic glutamate receptors in rat hippocampal CA1 pyramidal cells.

    abstract::The effects of the metabotropic glutamate (mGlu) receptor agonists (+/-)-trans-1-aminocyclopentane-1,3-dicarboxylic acid (trans-ACPD) or 1S,3R-ACPD on gamma-aminobutyric acid (GABA)-mediated inhibitory synaptic responses have been investigated in vitro in CA1 pyramidal cells of rat hippocampal slices. Bath application...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00223-8

    authors: Jouvenceau A,Dutar P,Billard JM

    更新日期:1995-08-04 00:00:00

  • Post-nephrectomy changes in adrenal angiotensin II receptors in the rat; influence of exogenous angiotensin and a competitive inhibitor.

    abstract::3H-angiotensin binding sites have been studied in a particulate fraction prepared from rat adrenal glands. This binding is rapid and reversible, of high affinity (KD29 degrees C = 3-5 X 10(-9) M) and with demonstrable specificity for the angiotensin II octapeptide. The number of binding sites varies with endogenous an...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90042-5

    authors: Pernollet MG,Devynck MA,Matthews PG,Meyer P

    更新日期:1977-06-15 00:00:00

  • Inhibitory actions of ropivacaine on tumor necrosis factor-alpha-induced leukocyte adhesion and tissue accumulation in vivo.

    abstract::We have examined the effect of ropivacaine, a local anesthetic, on leukocyte-endothelium interactions induced by tumor necrosis factor-alpha (TNF-alpha) in vivo by the use of intravital microscopy in the mouse cremaster microcirculation. It was found that ropivacaine markedly reduced venular leukocyte adhesion and tis...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(00)00108-4

    authors: Zhang XW,Thorlacius H

    更新日期:2000-03-24 00:00:00

  • Effect of interleukin-1 receptor antagonist on antigen-induced pulmonary responses in guinea pigs.

    abstract::The ability of the human interleukin-1 receptor antagonist, IL-1ra, to inhibit aerosolized antigen-induced airway hyperreactivity to i.v. substance P and bronchoalveolar lavage inflammatory cell accumulation, under in vivo conditions, was assessed in guinea pigs. Pretreatment with IL-1ra (30 mg/kg i.p., administered 3...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90621-a

    authors: Selig W,Tocker J

    更新日期:1992-03-31 00:00:00

  • Discriminative stimulus effects of BAY 38-7271, a novel cannabinoid receptor agonist.

    abstract::BAY 38-7271 [(-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate] is a novel, highly potent and selective cannabinoid CB(1)/CB(2) receptor agonist with neuroprotective properties. It was the aim of the present study to further confirm its cannabinoid CB(1) receptor agonist properties in a highly...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02697-3

    authors: De Vry J,Rüdiger Jentzsch K

    更新日期:2002-12-20 00:00:00

  • Dopamine D3 receptor modulation of dopamine efflux in the rat nucleus accumbens.

    abstract::The effect of antipsychotics on electrically evoked dopamine efflux in the rat nucleus accumbens core and shell was investigated, using in vitro fast cyclic voltammetry. In the nucleus accumbens core, the dopamine D2/D3 receptor agonist, (+/-)7-OH-DPAT ((+/-)-2-dipropylamino-7-hydroxy-1,2,3,4-tetrahydronaphthalene), i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.01.014

    authors: Roberts C,Cummins R,Gnoffo Z,Kew JN

    更新日期:2006-03-18 00:00:00

  • Effects of histamine H(1) receptor antagonists on hippocampal theta rhythm during spatial memory performance in rats.

    abstract::The effects of histamine H(1) receptor antagonists (promethazine, diphenhydramine, chlorphenilamine and triprolidine) on hippocampal theta rhythm during eight-arm radial maze performance were investigated using rats. Promethazine showed a significant increase in the number of total errors and working memory errors at ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.08.020

    authors: Masuoka T,Mikami A,Yasuda M,Shinomiya K,Kamei C

    更新日期:2007-12-08 00:00:00

  • The analgesic efficacy of partial opioid agonists is increased in mice with targeted inactivation of the alpha2A-adrenoceptor gene.

    abstract::Alpha(2A)-Adrenoceptors mediate the antinociceptive effects of alpha(2)-adrenoceptor agonists in mice, and analgesic synergism between noradrenergic and opioidergic mechanisms has been reported to be lacking in mice devoid of functional alpha(2A)-adrenoceptors. We investigated whether the antinociceptive actions of op...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.10.029

    authors: Ozdoğan UK,Lähdesmäki J,Scheinin M

    更新日期:2006-01-04 00:00:00

  • Alpha 1-adrenoceptor stimulation increases intracellular pH and Ca2+ in cardiomyocytes through Na+/H+ and Na+/Ca2+ exchange.

    abstract::The effects of alpha 1-adrenergic stimulation on intracellular pH (pHi) and Ca2+ concentration ([Ca2+]i) were investigated in isolated rat cardiomyocytes with fluorescence dyes, BCECF and fura-2, respectively. In the presence of 5 or 25 mM HCO3- norepinephrine (NE) increased pHi in a dose-dependent manner. Intracellul...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)94057-5

    authors: Iwakura K,Hori M,Watanabe Y,Kitabatake A,Cragoe EJ Jr,Yoshida H,Kamada T

    更新日期:1990-09-04 00:00:00

  • Behavioural topography in the striatum: differential effects of quinpirole and D-amphetamine microinjections.

    abstract::Behavioural evidence has accumulated that supports the hypothesis that specific territories of the striatum contribute differentially to the control of motor behaviours. The present experiments compare the behavioural effects of microinjections of amphetamine (20 microg/0.5 microl) with those elicited by the D2-class ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00752-3

    authors: Canales JJ,Iversen SD

    更新日期:1998-12-04 00:00:00

  • Assessment of the oestrogenic activity of the contraceptive progestin levonorgestrel and its non-phenolic metabolites.

    abstract::Levonorgestrel (13beta-ethyl-17alpha-ethynyl-17beta-hydroxy-4-gonen-3-one), a potent contraceptive progestin stimulates growth and proliferation of cultured breast cancer cells through a receptor-mediated mechanism, even though levonorgestrel does not bind to the oestrogen receptor (ER). To assess whether the oestroge...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)01263-8

    authors: Santillán R,Pérez-Palacios G,Reyes M,Damián-Matsumura P,García GA,Grillasca I,Lemus AE

    更新日期:2001-09-14 00:00:00

  • Activation of spinal α2 adrenergic receptors induces hyperglycemia in mouse though activating sympathetic outflow.

    abstract::The roles of α2-adrenergic receptors located in the spinal cord in the regulation of blood glucose levels were studied in imprinting control region (ICR) mice. Mice were treated intrathecally (i.t.) with clonidine or yohimbine, and the blood glucose levels were measured at 0, 30, 60 and 120min after i.t. administratio...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.08.022

    authors: Sim YB,Park SH,Kim SS,Lim SM,Jung JS,Suh HW

    更新日期:2014-10-15 00:00:00

  • Effects of a dual L/N-type Ca(2+) channel blocker cilnidipine on neurally mediated chronotropic response in anesthetized dogs.

    abstract::We investigated the effects of an L-type and N-type Ca(2+) channel blocker, cilnidipine, on neurally mediated chronotropic responses to clarify the anti-autonomic profile of cilnidipine in anesthetized dogs. Pretreatment with cilnidipine (0.3, 1.0 and 3.0 microg/kg, i.v.), which decreased mean blood pressure by 5 to 3...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00738-5

    authors: Konda T,Takahara A,Maeda K,Dohmoto H,Yoshimoto R

    更新日期:2001-02-09 00:00:00

  • Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex.

    abstract::Histamine stimulated the accumulation of [3H]inositol 1-phosphate in the presence of lithium in [3H]inositol-prelabelled slices from rat brain cortex in a concentration-dependent manner, with an EC50 value of 94.7 microM. High concentrations of antagonists of histamine H2 receptors, muscarinic receptors, alpha 1-adren...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90659-x

    authors: Claro E,Arbonés L,García A,Picatoste F

    更新日期:1986-04-16 00:00:00

  • Pharmacological evaluation of the beta-adrenoceptor agonist and thromboxane receptor blocking properties of 1-benzyl substituted trimetoquinol analogues.

    abstract::The beta 1- and beta 2-adrenoceptor agonist and thromboxane A2 (TXA2) antagonist properties of trimetoquinol (TMQ, I) and 1-benzyl substituted TMQ analogues [3'-iodo-4',5'-dimethoxy TMQ, II; 3',5'-diiodo-4'-dimethoxy TMQ, III; 3',4'-dimethoxy-5'-nitro TMQ, IV; 3',4'-dimethoxy-5'-amino TMQ; V; and 3',4'-dimethoxy TMQ, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90663-q

    authors: Shams G,Romstedt KJ,Gerhardt MA,Harrold MW,Miller DD,Feller DR

    更新日期:1990-08-02 00:00:00

  • Azaphenylalanine-based serine protease inhibitors induce caspase-mediated apoptosis.

    abstract::Molecules regulating cell death constitute prominent therapeutic targets. The pro-apoptotic role of serine protease inhibitors prompted us to search for novel modulators of this process. We have tested some recently synthesized antithrombotic compounds for their potential to induce apoptotic cell death. Cell based ana...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.11.008

    authors: Celhar T,Batista Napotnik T,Obreza A,Zega A,Anderluh PS,Kikelj D,Mlinaric-Rascan I

    更新日期:2009-01-05 00:00:00

  • PLGA nanoparticles loaded with beta-lactoglobulin-derived peptides modulate mucosal immunity and may facilitate cow's milk allergy prevention.

    abstract::Beta-lactoglobulin (BLG)-derived peptides may facilitate oral tolerance to whey and prevent cow's milk allergy (CMA). Loading of BLG-peptides in poly(lactic-co-glycolic acid) (PLGA) nanoparticles (Pep-NP) may improve this. Here we studied the uptake of NP and the capacity of NP and Pep-NP to activate bone marrow dendr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.10.051

    authors: Kostadinova AI,Middelburg J,Ciulla M,Garssen J,Hennink WE,Knippels LMJ,van Nostrum CF,Willemsen LEM

    更新日期:2018-01-05 00:00:00

  • Synergistic anti-tumor effects of Liraglutide, a glucagon-like peptide-1 receptor agonist, along with Docetaxel on LNCaP prostate cancer cell line.

    abstract::Docetaxel is a first line chemotherapy agent, which stabilizes microtubules in metastatic prostate cancer (PCa). Resistance to Docetaxel and its side effects remain as obstacle for its efficacy in monotherapy. Recently, combination with novel adjuvants have been emerged as a beneficial alternative strategy, which targ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2020.173102

    authors: Eftekhari S,Montazeri H,Tarighi P

    更新日期:2020-07-05 00:00:00