当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Pharmacological profile of YM358, a novel nonpeptide angiotensin AT1 receptor antagonist.

Pharmacological profile of YM358, a novel nonpeptide angiotensin AT1 receptor antagonist.

Abstract：

:The pharmacological profile of YM358, 2,7-diethyl-5-[[2'-(1 H-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]tri azole potassium salt monohydrate, a novel non-peptide angiotensin AT1 receptor antagonist, was studied in vitro and in vivo. YM358 competed with [125I][Sar1, Ile8]angiotensin II for angiotensin AT1 receptors in rat liver membranes. YM358 displayed competitive kinetics and the pKi value was calculated as 8.79. In contrast, YM358 had little effect on the binding of [125I][Sar1, Ile8]angiotensin II to the angiotensin AT2 receptor in bovine cerebellum. In isolated rabbit aorta, YM358 produced a parallel rightward shift in the concentration-response curve for angiotensin II with a pA2 value of 8.82. YM358 had no effect on the contraction induced by KCl, norepinephrine, serotonin, histamine, prostaglandin F2alpha or endothelin-1 even at 10(-5) M. On the basis of pKi values in the binding assay and pA2 values in the isolated tissues, YM358 was approximately 3-10 times more potent than losartan in antagonizing angiotensin AT1 receptors. In pithed rats, intravenous administration of YM358 inhibited an increase in mean blood pressure induced by intravenous infusion of angiotensin II in a dose-dependent manner. In conscious normotensive rats, YM358 at 3-30 mg/kg p.o. inhibited the angiotensin II-induced pressor response in a dose-dependent manner. YM358 at 30 mg/kg caused maximum and complete inhibition 30 min after dosing, and inhibition lasted more than 24 h. These results demonstrate that YM358 is a potent, AT1-selective and competitive nonpeptide angiotensin receptor antagonist. Moreover, YM358 is both orally active and long-lasting. This pharmacological profile suggests that YM358 would be suitable for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Shibasaki M,Fujimori A,Takanashi M,Kusayama T,Tokioka T,Satoh Y,Okazaki T,Uchida W,Inagaki O,Yanagisawa I

doi

10.1016/s0014-2999(97)01189-8

subject

Has Abstract

pub_date

1997-09-24 00:00:00

pages

167-73

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(97)01189-8

journal_volume

335

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • Anti-nociceptive and anti-allodynic effects of a high affinity NOP hexapeptide [Ac-RY(3-Cl)YRWR-NH2] (Syn 1020) in rodents.

    abstract：:There has been a flurry of activity to develop agonists and antagonists for the member of the opioid receptor family, NOP receptor (also known as ORL1), in part to understand its role in pain. Modifications of a hexapeptide originally identified from a combinatorial library have led to the discovery of a high affinity...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2006.12.015

    authors： Khroyan TV,Polgar WE,Orduna J,Zaveri NT,Judd AK,Tuttle DJ,Sanchez A,Toll L

    更新日期：2007-03-29 00:00:00

  • A comparative study of alpha-adrenergic receptor mediated Ca(2+) signals and contraction in intact human and mouse vascular smooth muscle.

    abstract：:In many vascular smooth muscle cells, physiological and pharmacological agonists initiate oscillatory fluctuations in intracellular Ca(2+) to initiate and maintain vasoconstriction. These oscillations are supported by the underlying cellular ultrastructure, particularly the close apposition between the plasma membrane...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2009.11.055

    authors： Dai JM,Syyong H,Navarro-Dorado J,Redondo S,Alonso M,van Breemen C,Tejerina T

    更新日期：2010-03-10 00:00:00

  • Aloe-emodin exerts a potent anticancer and immunomodulatory activity on BRAF-mutated human melanoma cells.

    abstract：:Aim of this study was to extend the knowledge on the antineoplastic effect of aloe-emodin (AE), a natural hydroxyanthraquinone compound, both in metastatic human melanoma cell lines and in primary stem-like cells (melanospheres). Treatment with AE caused reduction of cell proliferation and induction of SK-MEL-28 and A...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2015.05.057

    authors： Tabolacci C,Cordella M,Turcano L,Rossi S,Lentini A,Mariotti S,Nisini R,Sette G,Eramo A,Piredda L,De Maria R,Facchiano F,Beninati S

    更新日期：2015-09-05 00:00:00

  • Depression by morphine and levorphanol of activity in sympathetic nerve fibres in anaesthetized rats.

    abstract：:In urethane-anesthetized rats, the effects of intravenous injections of morphine, levorphanol, dextrorphan, pentazocine and naloxone were studied studied on the activity in nerve fibres of the cervical sympathetic trunk, and on mean arterial blood pressure and heart rate. Impulse frequency in sympathetic nerve fibres ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(84)90032-3

    authors： Jurna I,Rummel W

    更新日期：1984-05-18 00:00:00

  • Characterization of a binding site for angiotensin IV on bovine aortic endothelial cells.

    abstract：:We have characterized a specific binding site for angiotensin IV on bovine aortic endothelial cell membranes. Pseudo-equilibrium studies at 37 degrees C for 2 h have shown that this binding site recognizes angiotensin IV with a high affinity (Kd = 0.71; average of two experiments that yielded values of 0.71 and 0.72 n...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0922-4106(95)90142-6

    authors： Bernier SG,Servant G,Boudreau M,Fournier A,Guillemette G

    更新日期：1995-10-15 00:00:00

  • Validation of a pharmacological model for mitochondrial dysfunction in healthy subjects using simvastatin: A randomized placebo-controlled proof-of-pharmacology study.

    abstract：:Proof-of-pharmacology models to study compounds in healthy subjects offer multiple advantages. Simvastatin is known to induce mitochondrial dysfunction at least partly by depletion of co-enzyme Q10. The goal of this study was to evaluate a model of simvastatin-induced mitochondrial dysfunction in healthy subjects and ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,随机对照试验

    doi：10.1016/j.ejphar.2017.09.031

    authors： van Diemen MPJ,Berends CL,Akram N,Wezel J,Teeuwisse WM,Mik BG,Kan HE,Webb A,Beenakker JWM,Groeneveld GJ

    更新日期：2017-11-15 00:00:00

  • Cocaine inhibits the release of MPP+ but not dopamine through the rat dopamine transporter.

    abstract：:Transporter-mediated release of dopamine and the parkinsonism-inducing neurotoxin 1-methyl-4-phenylpyridinium (MPP+) was examined in COS cells, a cell line derived from monkey kidney, expressing the rat dopamine transporter. The release of preloaded [3H]MPP+ but not [3H]dopamine was dose-dependently inhibited by cocai...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(96)00406-2

    authors： Kitayama S,Morita K,Dohi T

    更新日期：1996-08-01 00:00:00

  • Ischemic insult induced apoptotic changes in PC12 cells: protection by trans resveratrol.

    abstract：:In this study, we determined the protective potential of trans resveratrol against oxygen-glucose deprivation (OGD) induced reactive oxygen species mediated apoptotic damages in PC12 cells. In vitro model of ischemic cerebral stroke was created by keeping cells in an OGD condition for 6h followed by 24h reoxygenation....

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2011.05.015

    authors： Agrawal M,Kumar V,Kashyap MP,Khanna VK,Randhawa GS,Pant AB

    更新日期：2011-09-01 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

  • The thyrotropin-releasing hormone-like peptides pGlu-Phe-Pro amide and pGlu-Glu-Pro amide increase plasma triiodothyronine levels in the mouse; the activity is sensitive to testosterone.

    abstract：:Three naturally occurring peptides, pGlu-Glu-Pro amide, pGlu-Phe-Pro amide and pGlu-Gln-Pro amide, with similar structures to thyrotropin releasing hormone (TRH) have recently been identified but no studies of their in vivo activities have been reported previously. We describe here the ability of pGlu-Phe-Pro amide an...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00593-7

    authors： Cremades A,Peñafiel R,Rausell V,Del Rio-Garcia J,Smyth DG

    更新日期：1998-09-25 00:00:00

  • Mechanism of osthole inhibition of vascular Ca(v)1.2 current.

    abstract：:Osthole is a coumarin extracted from Cnidium monnieri (L.) Cusson. The medicinal plant is widely used in Vietnamese as well as Chinese traditional medicine as a vasodilating and antihypertensive agent. Here we have tested the proposition that the block of Ca(v)1.2 channels is mainly responsible for its vascular activi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2012.01.038

    authors： Fusi F,Sgaragli G,Ha le M,Cuong NM,Saponara S

    更新日期：2012-04-05 00:00:00

  • Edematous response caused by [Thi5,8,D-Phe7]bradykinin, a B2 receptor antagonist, is due to mast cell degranulation.

    abstract：:[Thi5,8,D-Phe7]bradykinin caused hind-paw edema and degranulation of isolated peritoneal mast cells in a dose-dependent manner. Pretreatment with diphenhydramine/methysergide or compound 48/80 completely suppressed the edematous response caused by [Thi5,8,D-Phe7]bradykinin, whereas bradykinin-induced hind-paw swelling...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(89)90836-4

    authors： Wang JP,Hsu MF,Ouyang CH,Teng CM

    更新日期：1989-02-28 00:00:00

  • Effect of a decrease in pH on responses mediated by P2 receptors in the rat mesenteric arterial bed.

    abstract：:The present study investigated the effect of acidosis (reduction in pH of the Krebs' solution from 7.4 to 6.9) on responses to vasoconstrictors and vasodilators, with a focus on purines, in the rat isolated perfused mesenteric arterial bed. alpha,beta-Methylene ATP (alpha,beta-meATP) (10 microM), a selective P2X recep...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(00)00631-2

    authors： Ralevic V

    更新日期：2000-10-06 00:00:00

  • Anti-tumor effect of germacrone on human hepatoma cell lines through inducing G2/M cell cycle arrest and promoting apoptosis.

    abstract：:Germacrone is one of the main bioactive components in the traditional Chinese medicine Rhizoma curcuma. In this study, the anti-proliferative effect of germacrone on the human hepatoma cell lines and the molecular mechanism underlying the cytotoxicity of germacrone were investigated. Treatment of human hepatoma cell l...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2012.10.013

    authors： Liu Y,Wang W,Fang B,Ma F,Zheng Q,Deng P,Zhao S,Chen M,Yang G,He G

    更新日期：2013-01-05 00:00:00

  • Differential neurotensin responses to low and high doses of methamphetamine in the terminal regions of striatal efferents.

    abstract：:Neurotensin is a neuropeptide associated with basal ganglia dopaminergic neurons. Because levels of neurotensin in striatal tissue are differentially affected by low or high doses of methamphetamine, we employed microdialysis to assess the dose-dependent effects of methamphetamine on neurotensin release from the termi...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2005.08.036

    authors： Frankel PS,Hoonakker AJ,Hanson GR,Bush L,Keefe KA,Alburges ME

    更新日期：2005-10-17 00:00:00

  • Long-term blockade of the expression of cocaine sensitization by ondansetron, a 5-HT(3) receptor antagonist.

    abstract：:Intermittent cocaine administration induces sensitization (reverse tolerance) to its behavioral effects. The mechanism(s) mediating sensitization is not clear, however, previous research has implicated 5-HT(3) receptors in the expression of sensitization. The present experiment evaluated the ability of the 5-HT(3) rec...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(99)00926-7

    authors： King GR,Xiong Z,Douglass S,Ellinwood EH

    更新日期：2000-04-07 00:00:00

  • Protective effect of WEB 2086, a novel antagonist of platelet activating factor, in endotoxin shock.

    abstract：:WEB 2086, a novel specific platelet activating factor (PAF) antagonist derived from triazolodiazepines, inhibited in a dose-related manner the hypotensive and lethal effect of PAF as well as of E. coli endotoxin in the rat. The hypotension induced by endotoxin (15 mg/kg i.v.) or PAF (30 ng/(kg X min) i.v.) in anaesthe...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(87)90602-9

    authors： Casals-Stenzel J

    更新日期：1987-03-17 00:00:00

  • NMDA receptor-dependent long term hyperalgesia after tail amputation in mice.

    abstract：:Amputation of the mouse tail tip (2.5 cm) caused long term thermal and mechanical hyperalgesia in the remaining part of the tail. Hyperalgesia of the hindpaw to noxious heat (55 degrees C) and cold (0 degrees C) stimuli were also observed. Hyperalgesia at both the tail and hindpaw had a rapid onset (< or = 30 min) and...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00197-6

    authors： Zhuo M

    更新日期：1998-05-22 00:00:00

  • Anti-inflammatory and analgesic effects of a novel pyrazole derivative, FR140423.

    abstract：:The pharmacological profile of a novel and newly discovered non-steroidal anti-inflammatory and analgesic compound, 3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4-(methylsulfinyl)phenyl]pyraz ole (FR140423), was investigated. In recombinant human cyclooxygenase enzyme assays, the inhibition of prostaglandin E2 formation ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00868-1

    authors： Ochi T,Jobo-Magari K,Yonezawa A,Matsumori K,Fujii T

    更新日期：1999-01-22 00:00:00

  • Phytochemical compounds targeting on Nrf2 for chemoprevention in colorectal cancer.

    abstract：:Colorectal cancer (CRC) has become one of the major factors of tumor-related morbidity and mortality in the world because of its poor prognosis and consequences of metastatic spread. Currently, chemoprevention has been considered as a way of preventing cancer who takes advantage of plant phytochemicals and synthetic c...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejphar.2020.173588

    authors： Zhu Y,Yang Q,Liu H,Song Z,Chen W

    更新日期：2020-11-15 00:00:00

  • Pinacidil-postconditioning is equivalent to ischemic postconditioning in defeating cardiac ischemia-reperfusion injury in rat.

    abstract：:Ischemic postconditioning (IPO) had been reported as a promising method against myocardial ischemia-reperfusion (I/R) injury, but IPO was later proved with poor clinical benefit. In this study, we compared the protective effects of pinacidil-postconditioning (PPO) and IPO against myocardial I/R injury. Langendorff rat...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2016.03.027

    authors： Yang YH,Zhang Y,Chen W,Wang Y,Cao S,Yu T,Wang H

    更新日期：2016-06-05 00:00:00

  • Orally delivered all-trans-retinoic acid- and transforming growth factor-β-loaded microparticles ameliorate type 1 diabetes in mice.

    abstract：:Type 1 diabetes (T1D) is a multifactorial autoimmune disease that develops as a consequence of macrophage- and T cell-dependent pancreatic β-cell death. Multiple approaches for induction of anti-inflammatory/regulatory mechanisms that would attenuate T1D have been utilized, with little or no beneficial effects. To ach...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2019.172721

    authors： Koprivica I,Gajic D,Saksida T,Cavalli E,Auci D,Despotovic S,Pejnovic N,Stosic-Grujicic S,Nicoletti F,Stojanovic I

    更新日期：2019-12-01 00:00:00

  • Effects of EXP3174, a non-peptide angiotensin II receptor antagonist, on renal hemodynamics and renal function in dogs.

    abstract：:We examined the effects of intrarenal infusion of EXP3174, a non-peptide angiotensin II receptor antagonist, in order to evaluate the physiological role of endogenous angiotensin II in regulating renal hemodynamics and urine formation and to assess the possibility of a tubular site(s) of action of endogenous angiotens...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90221-3

    authors： Tamaki T,Nishiyama A,Yoshida H,He H,Fukui T,Yamamoto A,Aki Y,Kimura S,Iwao H,Miyatake A

    更新日期：1993-05-12 00:00:00

  • Expression of purinergic P2Y receptor subtypes by INS-1 insulinoma beta-cells: a molecular and binding characterization.

    abstract：:Purinergic P2Y-receptor agonists amplify glucose-induced insulin secretion from pancreatic beta-cells, thus offering new opportunities for the treatment of type 2 diabetes. However, little is known about which subtypes of purinergic P2Y receptors are expressed in these cells. The INS-1 beta-cell line is used as a mode...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2007.04.012

    authors： Lugo-Garcia L,Filhol R,Lajoix AD,Gross R,Petit P,Vignon J

    更新日期：2007-07-30 00:00:00

  • Protein kinase A-dependent coupling of mouse prostacyclin receptors to Gi is cell-type dependent.

    abstract：:The ability of the prostacyclin (IP) receptor agonist cicaprost to activate Gs-, Gq/11- and Gi-mediated cell signalling pathways has been examined in Chinese hamster ovary (CHO) cells and human embryonic kidney 293 (HEK 293) cells expressing the cloned human (hIP) or mouse (mIP) prostacyclin receptor, and compared wit...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(03)02006-5

    authors： Chow KB,Jones RL,Wise H

    更新日期：2003-08-01 00:00:00

  • Relaxation by calcitonin gene-related peptide may involve activation of K+ channels in the human uterine artery.

    abstract：:The vasodilatory role of calcitonin gene-related peptide in activating K+ channels was examined in isolated, suffused human uterine arteries. Calcitonin gene-related peptide produced a concentration-dependent relaxation of norepinephrine (1 microM)-induced contractions. Calcitonin gene-related peptide was antagonized ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90249-h

    authors： Nelson SH,Suresh MS,Dehring DJ,Johnson RL

    更新日期：1993-10-05 00:00:00

  • Ethanol differentially modulates the expression and activity of cell cycle regulatory proteins in rat aortic smooth muscle cells.

    abstract：:The aim of this study was to determine the effect of ethanol on cell cycle events during the G(1) and S phases in cultured vascular smooth muscle cells (VSMC). Flow cytometric analysis for the DNA content in rat aortic VSMC indicated that following ethanol treatment, the cell population in the G(0)/G(1) phase increase...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(02)01761-2

    authors： Sayeed S,Cullen JP,Coppage M,Sitzmann JV,Redmond EM

    更新日期：2002-06-12 00:00:00

  • Protective effect of verbascoside on 1-methyl-4-phenylpyridinium ion-induced neurotoxicity in PC12 cells.

    abstract：:The neuroprotective effects of verbascoside, one of phenylpropanoid glucoside isolated from the Chinese herbal medicine Buddleja officinalis Maxim, on 1-methyl-4-phenylpyridinium ion (MPP(+)) induced apoptosis and oxidative stress in PC12 neuronal cells were investigated. Treatment of PC12 cells with MPP(+) for 48 h i...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(02)02240-9

    authors： Sheng GQ,Zhang JR,Pu XP,Ma J,Li CL

    更新日期：2002-09-13 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

  • 20-hydroxyeicosatetraenoic acid is an endothelium-dependent vasoconstrictor in rabbit arteries.

    abstract：:Recently we have demonstrated that 20-hydroxy-5,8,11,14-eicosatetraenoic acid (20-HETE) constricts rat aortic rings and that this effect is cyclooxygenase- and endothelium-dependent. Incubation of 20-HETE with ram seminal vesicles, a rich source of cyclooxygenase, led to the identification of vasoconstrictor metabolit...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(93)90812-v

    authors： Escalante B,Omata K,Sessa W,Lee SG,Falck JR,Schwartzman ML

    更新日期：1993-04-22 00:00:00