当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > In vivo and in vitro characterisation of a nonpeptide vasopressin V(1A) and V(2) receptor antagonist (YM087) in the rat.

In vivo and in vitro characterisation of a nonpeptide vasopressin V(1A) and V(2) receptor antagonist (YM087) in the rat.

Abstract：

:This paper reports the in vitro and in vivo characterisation of a nonpeptide, orally active, vasopressin V(1A) and V(2) receptor antagonist, YM087 (methyl-1,4,5,6-tetrahydroimidazo[4, 5-d][1]benzoazepine-6-carbonyl)-2-phenylbenzanilide monohydrochloride) in the rat. YM087 dose dependently displaced the vasopressin V(1A) receptor antagonist radioligand, 125I-labelled [d(CH(2))(5),sarcosine(7)]vasopressin at vasopressin V(1A) receptors in liver and kidney medulla membranes and caused a concentration dependent displacement of the vasopressin V(2) receptor antagonist radioligand [3H]desGly-NH(2)(9)[d(CH(2))(5), D-Ile(2), Ile(4)]vasopressin at vasopressin V(2) receptors in kidney medulla membranes. In vitro binding kinetic studies showed YM087 acted as a competitive antagonist at liver V(1A) and kidney V(1A) and V(2) vasopressin receptors. Oral administration of YM087 (0.1-3 mg/kg) dose dependently inhibited vasopressin binding to liver V(1A) and kidney V(1A) and V(2) vasopressin receptors over 24 h. Oral YM087 (1-3 mg/kg/day) for 7 days in normotensive rats caused a dose dependent aquaresis with no effect on systolic blood pressure. These results show that YM087 is an orally effective vasopressin V(1A) and V(2) receptor antagonist that may be useful in the treatment of conditions characterised by vasoconstriction and fluid retention such as congestive heart failure.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Risvanis J,Naitoh M,Johnston CI,Burrell LM

doi

10.1016/s0014-2999(99)00530-0

keywords:

subject

Has Abstract

pub_date

1999-09-17 00:00:00

pages

23-30

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(99)00530-0

journal_volume

381

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cells lacking functional GABAB receptors.

    abstract：:The present study shows that the GABAB positive allosteric modulators (PAMs) CGP7930 and GS39783 stimulate extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) signalling in cells that do not express functional GABAB receptors. In human SH-SY5Y neuroblastoma cells, CGP7930 and GS39783 induced a time- and co...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.11.030

    authors： Olianas MC,Dedoni S,Onali P

    更新日期：2017-01-05 00:00:00

  • Involvement of central K(ATP) channels in the gastric antisecretory action of alpha2-adrenoceptor agonists and beta-endorphin in rats.

    abstract：:The intracerebroventricularly (i.c.v.) injected presynaptic alpha2-adrenoceptor agonists, clonidine and oxymetazoline, exerted a dose-dependent inhibition on the gastric acid secretion in pylorus-ligated rats; the ED50 values were 20 and 7.5 nmol/rat, respectively. Moreover, beta-endorphin, given i.c.v., also decrease...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(01)01572-2

    authors： Müllner K,Rónai AZ,Fülöp K,Fürst S,Gyires K

    更新日期：2002-01-25 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

  • New adenosine A2A receptor antagonists: actions on Parkinson's disease models.

    abstract：:The 8-substituted 9-ethyladenine derivatives: 8-bromo-9-ethyladenine (ANR 82), 8-ethoxy- 9-ethyladenine (ANR 94), and 8-furyl-9-ethyladenine (ANR 152) have been characterized in vitro as adenosine receptor antagonists. Adenosine is deeply involved in the control of motor behaviour and substantial evidences indicate th...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2005.01.057

    authors： Pinna A,Volpini R,Cristalli G,Morelli M

    更新日期：2005-04-11 00:00:00

  • Hydralazine-induced vasodilation involves opening of high conductance Ca2+-activated K+ channels.

    abstract：:The purpose of this study was to investigate whether high conductance Ca2+-activated K+ channels (BK(Ca)) are mediating the vasodilator action of hydralazine. In isolated porcine coronary arteries, hydralazine (1-300 microM), like the K+ channel opener levcromakalim, preferentially relaxed contractions induced by K+ (...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00701-8

    authors： Bang L,Nielsen-Kudsk JE,Gruhn N,Trautner S,Theilgaard SA,Olesen SP,Boesgaard S,Aldershvile J

    更新日期：1998-11-13 00:00:00

  • A monoclonal antibody to calcitonin gene-related peptide abolishes capsaicin-induced gastroprotection.

    abstract：:Calcitonin gene-related peptide (CGRP) released from vasodilator nerves is implicated in the gastroprotective action of capsaicin. This experimental paradigm was used to prove the effectiveness of a monoclonal anti-CGRP antibody. The experiments were performed in anaesthetized rats in which intragastric capsaicin (0.5...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90645-x

    authors： Peskar BM,Wong HC,Walsh JH,Holzer P

    更新日期：1993-11-30 00:00:00

  • Receptor binding and vasoconstrictor activity of big endothelin.

    abstract：:We studied the effects of synthetic porcine big endothelin (ET), a putative 39-residue intermediate deduced from cDNA sequence analysis, on receptor binding activity in cultured rat vascular smooth muscle cells as well as its vasoconstrictive activity in rat pulmonary artery. Big ET was about two orders of magnitude l...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(90)90532-b

    authors： Hirata Y,Kanno K,Watanabe TX,Kumagaye S,Nakajima K,Kimura T,Sakakibara S,Marumo F

    更新日期：1990-02-06 00:00:00

  • Effects of 4-aminopyridine on cat blood pressure in relation to the sympathetic nervous system.

    abstract：:The pressor effect of 4-aminopyridine (4-AP) was studied in anesthetized cats and in isolated cat aortic ring preparations. A significant increase in blood pressure (38.9 +/- 11.4 mmHg) was observed following intravenous administration of 4-AP (0.3 mg/kg). The elevated blood pressure lasted for 1.3 h and returned to t...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(85)90343-7

    authors： Yen MH,Lee SH,Ho ST

    更新日期：1985-07-11 00:00:00

  • Effects of granisetron, a 5-HT3 receptor antagonist, on morphine-induced potentiation of brain stimulation reward.

    abstract：:Using the curve-shift method, we studied the effects of four doses (0.003, 0.03, 0.3 and 3 mg/kg, s.c.) of granisetron (endo-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1-methyl-1H-indazole-3- carboxamide hydrochloride), a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist, on the potentiation of brain stimulatio...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00497-1

    authors： Rompré PP,Injoyan R,Hagan JJ

    更新日期：1995-12-20 00:00:00

  • Phenylpyrrolidine structural mimics of pirfenidone lacking antifibrotic activity: A new tool for mechanism of action studies.

    abstract：:Pirfenidone recently received FDA approval as one of the first two drugs designed to treat idiopathic pulmonary fibrosis. While the clinical data continues to support the efficacy of pirfenidone, the specific molecular mechanism of action of this drug has not been fully defined. From a chemical perspective the compara...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2017.05.050

    authors： Haak AJ,Girtman MA,Ali MF,Carmona EM,Limper AH,Tschumperlin DJ

    更新日期：2017-09-15 00:00:00

  • Comparison of clenbuterol enantiomers using four psychopharmacological tests sensitive to beta-agonists.

    abstract：:The effects of the enantiomers of clenbuterol were compared in four psychopharmacological tests in which beta-adrenergic agonists are known to be active. In mice (+/-)-clenbuterol 0.06 mg/kg decreased motor activity and antagonized the hypothermia induced by 16 mg/kg of apomorphine; at 0.5 mg/kg it increased head-twit...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(85)90481-9

    authors： Martin P,Puech AJ,Brochet D,Soubrié P,Simon P

    更新日期：1985-10-29 00:00:00

  • Meta-chlorophenylpiperazine induced changes in locomotor activity are mediated by 5-HT1 as well as 5-HT2C receptors in mice.

    abstract：:1-(Meta-chloro)phenylpiperazine (m-CPP) is a 5-HT receptor agonist which has been purported to be relatively selective for the 5-HT2C receptor. In particular, the hypolocomotion produced by m-CPP has been suggested to be mediated by 5-HT2C receptors. m-CPP binds with high affinity to 5-HT1 as well as 5-HT2 receptors, ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(97)01474-x

    authors： Gleason SD,Shannon HE

    更新日期：1998-01-12 00:00:00

  • Chronic gastric ulcer healing in rats subjected to selective and non-selective cyclooxygenase-2 inhibitors.

    abstract：UNLABELLED:The influence of different nonsteroidal anti-inflammatory drugs (NSAIDs) and of a proton pump inhibitor on the healing parameters of a chronic gastric ulcer was evaluated. Wistar rats were used after the induction of a chronic acetic acid ulcer. The animals were treated orally for 8 and 15 days, twice daily,...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(02)01494-2

    authors： Berenguer B,Alarcón de la Lastra C,Moreno FJ,Martín MJ

    更新日期：2002-05-03 00:00:00

  • Role of 5-hydroxytryptamine and mast cells in the tachykinin-induced contraction of rat trachea in vitro.

    abstract：:The in vivo bronchoconstrictor effect of tachykinins in Fisher 344 rats is accompanied by release into the airways of 5-hydroxytryptamine (5-HT). 5-HT is possibly derived from mast cells. In the present study the presumed mast cell-tachykinin interaction was studied in isolated trachea from Fisher 344 rats. Contractio...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(97)81929-2

    authors： Joos GF,Lefebvre RA,Bullock GR,Pauwels RA

    更新日期：1997-11-12 00:00:00

  • Functional and druggability analysis of the SARS-CoV-2 proteome.

    abstract：:The infectious coronavirus disease (COVID-19) pandemic, caused by the coronavirus SARS-CoV-2, appeared in December 2019 in Wuhan, China, and has spread worldwide. As of today, more than 46 million people have been infected and over 1.2 million fatalities. With the purpose of contributing to the development of effectiv...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.173705

    authors： Cavasotto CN,Lamas MS,Maggini J

    更新日期：2021-01-05 00:00:00

  • Alterations of beta-receptor-adenylyl cyclase coupling by long-term ATP depletion in cultured rat cardiomyocytes.

    abstract：:In cultured rat heart muscle cells, reversible long-term ATP depletion induces a decrease in beta-adrenoceptor density and a fall in isoproterenol- as well as forskolin-stimulated cAMP formation. However, isoproterenol-stimulated adenylyl cyclase activity in membrane preparations is not reduced after ATP depletion. Th...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0922-4106(91)90104-p

    authors： Wagenknecht B,Beuttler C

    更新日期：1991-11-13 00:00:00

  • 2-Ethoxy-4,5-diphenyl-1,3-oxazine-6-one activates the Nrf2/HO-1 axis and protects against oxidative stress-induced neuronal death.

    abstract：:Apoptosis or programmed cell death has been suggested as an important mode of neurodegeneration in Alzheimer's disease pathogenesis. The present study explored the neuroprotective effect of 2-ethoxy-4,5-diphenyl-1,3-oxazine-6-one (EDPOO) against H(2)O(2)-induced cell death in rat pheochromocytoma (PC12) cells. We foun...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2011.02.028

    authors： Ansari N,Khodagholi F,Amini M

    更新日期：2011-05-11 00:00:00

  • Tryptase-induced airway microvascular leakage in guinea pigs: involvement of tachykinins and leukotrienes.

    abstract：:Tryptase, a serine protease synthesized by and stored in mast cells, is implicated as an important mediator in the pathogenesis of airway inflammation. In this study, tryptase was evaluated for its ability to induce microvascular leakage into the airways of guinea pigs. Dose- and time-dependent increases in airway mic...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(01)00960-8

    authors： Greenfeder S,Sehring S,McHugh N,Corboz M,Rivelli M,Anthes JC,Billah M,Egan RW,Chapman RW

    更新日期：2001-05-11 00:00:00

  • Membrane activity of class III antiarrhythmic compounds; a comparison between ibutilide, d-sotalol, E-4031, sematilide and dofetilide.

    abstract：:This study compares the membrane activity of ibutilide, d-sotalol, sematilide, E-4031 and dofetilide on single ventricular cells under identical experimental conditions. We found that ibutilide and dofetilide produced a 'bell-shaped' concentration-dependent effect on action potential duration. Ionic current measuremen...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90704-l

    authors： Lee KS,Tsai TD,Lee EW

    更新日期：1993-03-30 00:00:00

  • The impact of GABAB receptors and their pharmacological stimulation on cocaine reinforcement and drug-seeking behaviors in a rat model of depression.

    abstract：:Depression and cocaine use disorder represent frequent co-current diagnoses and the GABAB receptors are involved in both conditions. This research involved the application of the animal model of depression (bulbectomy, OBX) and cocaine use disorder (self-administration) to assess the efficiency of GABAB receptor agoni...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.173324

    authors： Gawlińska K,Jastrzębska J,Gamberini S,Gawliński D,Pieniążek R,Suder A,Wydra K,Frankowska M

    更新日期：2020-09-15 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

  • An outline for the pharmacological effect of icariin in the nervous system.

    abstract：:Icariin is a major active component of the traditional herb Epimedium, also known as Horny Goat Weed. It has been extensively studied throughout the past several years and is known to exert anti-oxidative, anti-neuroinflammatory, and anti-apoptotic effects. It is now being considered as a potential therapeutic agent f...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejphar.2018.10.006

    authors： Jin J,Wang H,Hua X,Chen D,Huang C,Chen Z

    更新日期：2019-01-05 00:00:00

  • Role of protein kinase C in the endothelin-induced contraction in the rabbit saphenous vein.

    abstract：:The role of protein kinase C in the endothelin-induced contraction was examined in the isolated rabbit saphenous vein in which endothelin-1, endothelin-3, sarafotoxin S6c and IRL 1620 (succinyl-[Glu9,Ala11,15]endothelin-1-(8-21))-induced contraction at the threshold concentrations of 0.1-1 pM. A selective inhibitor of...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00542-0

    authors： Sudjarwo SA,Karaki H

    更新日期：1995-12-27 00:00:00

  • Source of the elevation Ca2+ evoked by 15-HETE in pulmonary arterial myocytes.

    abstract：:We have previously reported that 15-hydroxyeicosatetraenoic acid (15-HETE), a metabolite of arachidonic acid by 15-lipoxygenase, causes pulmonary vasoconstriction via increasing the intracellular Ca(2+) concentration ([Ca(2+)]i). However, the multiple sources of Ca(2+) that contribute to Ca(2+) elevation during and af...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2008.10.028

    authors： Zheng X,Li Q,Tang X,Liang S,Chen L,Zhang S,Wang Z,Guo L,Zhang R,Zhu D

    更新日期：2008-12-28 00:00:00

  • Influence of the 21-aminosteroid U74389F on ischemia-reperfusion injury in the rat.

    abstract：:We examined the effects of the administration of 21-[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]-pregna-1,4,9( 11)-triene-3,20-dione, monomethansulfonate (U74389F), a 21-aminosteroid and so-called lazaroid, that is characterized by an inhibitory activity against iron-dependent lipid peroxidation, on ischemi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00638-9

    authors： Paroni R,De Vecchi E,Lubatti L,Conti E,Beretta C,Rinaldi P,Kienle MG,Trazzi R

    更新日期：1995-12-29 00:00:00

  • DOI is a mixed agonist-antagonist at postjunctional 5-HT2 receptors in the pithed rat.

    abstract：:The maximal pressor effect induced by DOI in the pithed rat was smaller than that induced by 5-HT, suggesting partial agonistic properties of DOI. DOI shifted the dose-pressor response curve of 5-HT to the right. It is concluded that, in addition to its 5-HT2 agonistic properties, DOI also possesses 5-HT2 antagonistic...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(89)90143-x

    authors： Dabiré H,Chaouche-Teyara K,Cherqui C,Fournier B,Schmitt H

    更新日期：1989-10-24 00:00:00

  • Behavioral studies with the beta-carboline FG 7142 combined with related drugs in monkeys.

    abstract：:The beta-carboline FG 7142 was studied alone and in combination with Ro 15-1788, CGS 8216 and lorazepam in squirrel monkeys trained to respond under a fixed-interval (FI) schedule of food presentation. FG 7142 (0.3-5.6 mg/kg i.v.) produced dose-related decreases in the rate of FI responding, effects opposite to those ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(89)90190-8

    authors： Wettstein JG

    更新日期：1989-04-25 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

  • Functional characterization of α7 nicotinic acetylcholine and NMDA receptor signaling in SH-SY5Y neuroblastoma cells in an ERK phosphorylation assay.

    abstract：:In the present study, the functional properties of α7 nicotinic acetylcholine receptors (α7 nAChRs) and N-methyl-D-aspartate receptors (NMDARs) endogenously expressed in SH-SY5Y human neuroblastoma cells were characterized in an extracellular-signal regulated kinase (ERK) phosphorylation assay. Both choline and N-meth...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2018.02.047

    authors： Elnagar MR,Walls AB,Helal GK,Hamada FM,Thomsen MS,Jensen AA

    更新日期：2018-05-05 00:00:00

  • Two mechanistically distinct effects of dihydropyridine nifedipine on CaV1.2 L-type Ca²⁺ channels revealed by Timothy syndrome mutation.

    abstract：:Dihydropyridine Ca(2+) channel antagonists (DHPs) block Ca(V)1.2 L-type Ca(2+) channels (LTCCs) by stabilizing their voltage-dependent inactivation (VDI); however, it is still not clear how DHPs allosterically interact with the kinetically distinct (fast and slow) VDI. Thus, we analyzed the effect of a prototypical DH...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2012.04.029

    authors： Sheng X,Nakada T,Kobayashi M,Kashihara T,Shibazaki T,Horiuchi-Hirose M,Gomi S,Hirose M,Aoyama T,Yamada M

    更新日期：2012-06-15 00:00:00