当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Pharmacological evaluation of the beta-adrenoceptor agonist and thromboxane receptor blocking properties of 1-benzyl substituted trimetoquinol analogues.

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, VI] were studied in guinea pig atria (beta 1) and trachea (beta 2), and in rat thoracic aorta and human platelets, respectively. The rank order of agonist activities in beta 1- and beta 2-adrenoceptor tissues was IV greater than or equal to I greater than II greater than V greater than III greater than VI and I greater than II = IV = V greater than VI greater than III, respectively. An increase of beta 2/beta 1-selectivity (2- to 3-fold) was observed for analogues V and VI as compared to TMQ. The rank order of inhibitory potency against U46619-induced contraction of rat aorta and human platelet aggregation and secretion was the same (I = II = III greater than IV greater than V greater than VI). The results show that varying the substituents at the 3'- and 5'-positions of the trimethoxybenzyl group of TMQ produces compounds which give different profiles of biological activity for beta-adrenoceptor agonism versus TXA2 antagonism. Certain TMQ analogues, notably analogue V, showed a greater selectivity as beta 2-receptor agonists and TXA2 antagonists in vascular smooth muscle than the parent drug (TMQ), and the iodinated analogues (II and III) have promise as potential radioligands or photoaffinity probes for thromboxane A2 receptors.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

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

doi

10.1016/0014-2999(90)90663-q

subject

Has Abstract

pub_date

1990-08-02 00:00:00

pages

21-31

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(90)90663-Q

journal_volume

184

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF PHARMACOLOGY文献大全
  • Selected nucleos(t)ide-based prescribed drugs and their multi-target activity.

    abstract：:Nucleos(t)ide analogues play pivotal roles as antiviral, cytotoxic or immunosuppressive agents. Here, we review recent reports of nucleoside analogues that exhibit broad-spectrum activity towards multiple life-threatening RNA and DNA viruses. We also present a discussion about nucleoside antimetabolites-approved antin...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejphar.2019.172747

    authors： Pastuch-Gawołek G,Gillner D,Król E,Walczak K,Wandzik I

    更新日期：2019-12-15 00:00:00

  • The open field as a paradigm to measure the effects of drugs on anxiety-like behaviors: a review.

    abstract：:The open field is a very popular animal model of anxiety-like behavior. An overview of the literature on the action elicited by effective or putative anxiolytics in animal subjected to this procedure indicates that classical treatments such as benzodiazepine receptor full agonists or 5-HT(1A) receptor full or partial ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/s0014-2999(03)01272-x

    authors： Prut L,Belzung C

    更新日期：2003-02-28 00:00:00

  • Reversal of scopolamine-induced deficits in radial maze performance by (-)-huperzine A: comparison with E2020 and tacrine.

    abstract：:The effects of (-)-huperzine A ((5R,9R,11E)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-5, 9-methanocycloocta[b]pyridin-2(1H)-one), and of the hydrochloride salt of E2020 ((R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl piperidine) and tacrine (9-amino-1,2,3,4-tetrahydroacridine), on the scopolamine-in...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00199-x

    authors： Wang T,Tang XC

    更新日期：1998-05-22 00:00:00

  • Renal actions of the angiotensin AT2 receptor ligands CGP 42112 and PD 123319 after blockade of the renin-angiotensin system.

    abstract：:The purpose of this study was to investigate whether the selective angiotensin AT2 receptor ligands, CGP 42112B (Nic-Tyr-(N alpha-benzoyloxycarbonyl-Arg)Lys-His-Pro-Ile-OH) and PD 123319 ((s)-1-[[4-(dimethylamino)-3-methyl-phenyl]methyl]-5-(diphenylacetyl+ ++)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]-pyridine-6-carboxylic...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(94)90153-8

    authors： Macari D,Whitebread S,Cumin F,De Gasparo M,Levens N

    更新日期：1994-06-23 00:00:00

  • Cocaine discrimination and time-course effects in male and female Wistar rats.

    abstract：:Previously, sex differences have been observed in the behavioral effects of acute and chronic cocaine administration. In the present experiment, male and female rats were trained to discriminate intraperitoneal injections of 10.0 mg/kg cocaine from its vehicle. It was hypothesized that the subjective effects of cocain...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(99)00597-x

    authors： Anderson KG,van Haaren F

    更新日期：1999-10-08 00:00:00

  • Evidence for the interaction of mast cell-degranulating peptide with pertussis toxin-sensitive G proteins in mast cells.

    abstract：:K(+)-channel blocker properties have been reported for mast cell-degranulating peptide (MCD) in the central nervous system, but its action mechanism in mast cells remains unknown. We studied the effect of MCD on the membrane potential of rat peritoneal mast cells using the fluorescent probe bis-oxonol. Unexpectedly, M...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0922-4106(91)90037-i

    authors： Mousli M,Bronner C,Bueb JL,Landry Y

    更新日期：1991-07-12 00:00:00

  • Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys.

    abstract：:The aim of the present research was to characterize the pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel quinazolinone-based dipeptidyl peptidase-4 (DPP-4) inhibitor. Alogliptin potently inhibited human DPP-4 in vitro (mean IC(50), ~ 6.9 nM) and exhibited > 10,000-fold selectivity for DPP...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2008.04.047

    authors： Lee B,Shi L,Kassel DB,Asakawa T,Takeuchi K,Christopher RJ

    更新日期：2008-07-28 00:00:00

  • Induction of cytochrome P450 1A1 expression by ginsenoside Rg1 and Rb1 in HepG2 cells.

    abstract：:Transcriptional activation of the human CYP1A1 gene (coding for cytochrome P450 1A1) is mediated by the aryl hydrocarbon receptor. In the present study we have examined interaction of the ginsenoside Rg1 and Rb1 with the carcinogen activation pathway mediated by the aryl hydrocarbon receptor in HepG2 cells. RT-PCR was...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2008.10.057

    authors： Wang Y,Ye X,Ma Z,Liang Q,Lu B,Tan H,Xiao C,Zhang B,Gao Y

    更新日期：2008-12-28 00:00:00

  • Corticotropin-releasing factor receptor type 1 mediates stress-induced relapse to cocaine-conditioned place preference in rats.

    abstract：:Corticotropin-releasing factor (CRF) has been suggested to play an important role in the development of drug dependence and withdrawal. Based on the recent finding that CRF receptor antagonists inhibit the stress-induced relapse to opiate dependence and attenuate anxiety-like responses related to cocaine withdrawal, t...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(01)00840-8

    authors： Lu L,Liu D,Ceng X

    更新日期：2001-03-01 00:00:00

  • Conditioned fear-induced tachycardia in the rat: vagal involvement.

    abstract：:The effects of conditioned fear on gross activity, heart rate, PQ interval, noradrenaline and adrenaline were studied in freely moving rats. Subcutaneous (s.c.) injections of atropine methyl nitrate (0.5 mg/kg) during rest resulted in a significant shortening of the PQ interval, indicating that the PQ interval can be ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(98)00261-1

    authors： Nijsen MJ,Croiset G,Diamant M,Stam R,Delsing D,de Wied D,Wiegant VM

    更新日期：1998-06-05 00:00:00

  • Antiproliferative and apoptotic effects of indole derivative, N-(2-hydroxy-5-nitrophenyl (4'-methylphenyl) methyl) indoline in breast cancer cells.

    abstract：:Indoline derivatives functions as an inhibitors of epidermal growth factor receptor (EGFR) with the anticancer potential against various cancers. We aim to investigate anti-breast cancer effects and mechanism of action of novel indoline derivatives. Molecular docking of seven indoline derivates with EGFR revealed, N-(...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.173195

    authors： Palanivel S,Murugesan A,Subramanian K,Yli-Harja O,Kandhavelu M

    更新日期：2020-08-15 00:00:00

  • Modifications by sumatriptan and acetylcholine of nitric oxide-mediated neurogenic dilatation in dog cerebral arteries.

    abstract：:Canine cerebral arterial strips denuded of endothelium responded to nicotine and transmural electrical stimulation with relaxations, which were abolished by NG-nitro-L-arginine and methylene blue. Magnitudes of relaxation did not differ in the arteries contracted with prostaglandin F2alpha and sumatriptan, an effectiv...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(01)01019-6

    authors： Ayajiki K,Fujioka H,Noda K,Okamura T,Toda N

    更新日期：2001-05-18 00:00:00

  • Effects of tetrandrine on left ventricle hypertrophy in deoxycorticosterone acetate-salt hypertensive rats.

    abstract：:The effect of regression of left ventricular hypertrophy was studied in deoxycorticosterone-acetate-salt hypertensive rats (DOCA-salt hypertensive rats) treated with tetrandrine. Treatment with tetrandrine (by gastric intubation, 50 mg/kg per day for 9 weeks) lowered systolic blood pressure, left ventricular weight, C...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(95)00055-p

    authors： Xu Y,Rao MR

    更新日期：1995-05-04 00:00:00

  • Enhancement by escins Ib and IIb of Mg(2+) absorption from digestive tract in mice: role of nitric oxide.

    abstract：:The effects of escins Ib and IIb isolated from horse chestnuts on Mg(2+) absorption from the digestive tract and the role of endogenous nitric oxide (NO) were investigated in mice. Test samples were given orally to fasted mice 30, 120, 180, 240 and 300 min before administration of 0.5 M MgSO(4) (10 ml/kg, p.o.). The s...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(99)00772-4

    authors： Li Y,Matsuda H,Wen S,Yamahara J,Yoshikawa M

    更新日期：2000-01-17 00:00:00

  • Gender-related drug effect on several markers of oxidation stress in diabetes patients with and without complications.

    abstract：:We previously reported that circulating lipid (malondialdehyde, MDA) and protein oxidation (carbonyl residues, CO) products can be used as markers of risk for complications in poorly controlled type 2 diabetics. Now, we aimed to evaluate the existence of a gender effect on classical disease markers and oxidative stres...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2015.09.041

    authors： Lodovici M,Bigagli E,Luceri C,Mannucci E,Rotella CM,Raimondi L

    更新日期：2015-11-05 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

  • Morroniside enhances angiogenesis and improves cardiac function following acute myocardial infarction in rats.

    abstract：:Angiogenesis is critical for re-establishing blood supply to the ischemic myocardium after acute myocardial infarction (AMI). This study aimed to investigate the effects of morroniside on angiogenesis after AMI and explored associated proangiogenic mechanisms. A rat model of AMI was established by ligation of the left...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2020.172954

    authors： Liu T,Sun F,Cui J,Zheng S,Li Z,Guo D,Tian X,Zhu Z,Zheng W,Wang Y,Wang W

    更新日期：2020-04-05 00:00:00

  • Mechanisms of phenylalanine-induced pressor effects in conscious rats.

    abstract：:Phenylalanine and tyrosine reportedly decrease blood pressure in conscious restrained rats. However, tyrosine has recently been found to increase blood pressure in anesthetized animals, questioning the generality of findings obtained in restrained animals. The present study therefore evaluated the effects of phenylala...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(89)90494-9

    authors： Yourick DL,Tessel RE

    更新日期：1989-01-31 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

  • Bradykinin and angiotensin II inhibit neurotransmission in rabbit ear artery by releasing prostanoids.

    abstract：:In isolated, perfused rabbit ear artery bradykinin, like [Met5]enkephalin and angiotensin II, inhibited neurogenic constrictions in concentrations lower than 10(-8) M without affecting the responses to exogenous norepinephrine. The IC50 value of bradykinin was 1.95 x 10(-10) M. The inhibitory action of bradykinin and ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(91)90567-a

    authors： Rónai AZ

    更新日期：1991-05-30 00:00:00

  • Famotidine does not induce long QT syndrome: experimental evidence from in vitro and in vivo test systems.

    abstract：:The effects of famotidine on the cardiac repolarization process were assessed using four different levels of test systems described in the draft stage guideline ICH S7B. A supratherapeutic concentration of famotidine (10(-5) M), which is >8 times higher than C(max) obtained after its therapeutic dose, neither inhibite...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0014-2999(03)01559-0

    authors： Sugiyama A,Satoh Y,Takahara A,Nakamura Y,Shimizu-Sasamata M,Sato S,Miyata K,Hashimoto K

    更新日期：2003-04-11 00:00:00

  • In vitro bidirectional permeability studies identify pharmacokinetic limitations of NKCC1 inhibitor bumetanide.

    abstract：:Recently, it has been suggested that bumetanide, an inhibitor of the Na-K-2Cl co-transporter (NKCC1), may be useful in the treatment of central nervous system (CNS) disorders. However, from a physicochemical perspective, bumetanide may not cross the blood-brain barrier to the extent that is necessary for it to be an e...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2015.12.001

    authors： Donovan MD,Schellekens H,Boylan GB,Cryan JF,Griffin BT

    更新日期：2016-01-05 00:00:00

  • RO 16-6028, a benzodiazepine receptor partial agonist, does not exhibit anticonvulsant tolerance in mice.

    abstract：:The development of anticonvulsant tolerance with RO 16-6028, a benzodiazepine receptor partial agonist, was assessed in mice using an i.v. infusion of pentylenetetrazol as the convulsive stimulus. In contrast to other benzodiazepines tested previously in this seizure model the anticonvulsant protection afforded by RO ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(88)90788-1

    authors： Haigh JR,Feely M

    更新日期：1988-03-01 00:00:00

  • Effect of a smooth muscle relaxant from the stonefish, Synanceia trachynis, on KCl-induced responses in the guinea-pig vas deferens.

    abstract：:Stonefish skin secretion contains a smooth muscle relaxant, synancein II, that selectively inhibits tonic responses of KCl-induced contractions of the guinea-pig vas deferens. Synancein II (5-50 micrograms/ml) and nifedipine (10(-8)-10(-7) M) reduced tonic responses equally. Over these concentrations, synancein II inh...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(86)90341-9

    authors： Hoy AW,Cameron AM

    更新日期：1986-09-23 00:00:00

  • In vivo measurement of extracellular dopamine and DOPAC in rat striatum after various dopamine-releasing drugs; implications for the origin of extracellular DOPAC.

    abstract：:In order to further examine the likely origin of the dopamine (DA) metabolite, 3,4-dihydroxyphenylacetic acid (DOPAC), certain drugs known to release DA from different intraneuronal pools were tested for their effects on extracellular striatal DA and DOPAC levels by means of brain microdialysis in the halothane-anaest...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(88)90110-0

    authors： Zetterström T,Sharp T,Collin AK,Ungerstedt U

    更新日期：1988-04-13 00:00:00

  • Involvement of a NO-cyclic GMP-PKG signaling pathway in nitrous oxide-induced antinociception in mice.

    abstract：:The antinociceptive effect of nitrous oxide (N(2)O) is dependent on nitric oxide (NO); however, the next step in the pathway activated by NO is undetermined. The present study was conducted to test the hypothesis that a N(2)O action involves sequential activation of NO synthase, soluble guanylyl cyclase and protein ki...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2011.01.006

    authors： Zhang Y,Quock LP,Chung E,Ohgami Y,Quock RM

    更新日期：2011-03-11 00:00:00

  • N1phenethyl-norcymserine, a selective butyrylcholinesterase inhibitor, increases acetylcholine release in rat cerebral cortex: a comparison with donepezil and rivastigmine.

    abstract：:The effects of (-)-N(1)phenethyl-norcymserine (PEC, 5 mk/kg, i.p.) on acetylcholine release and cholinesterase activity in the rat cerebral cortex were compared with those of donepezil (1 mg/kg, i.p.), a selective acetylcholinesterase inhibitor, and rivastigmine (0.6 mg/kg, i.p.), an inhibitor of acetylcholinesterase ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.ejphar.2007.06.053

    authors： Cerbai F,Giovannini MG,Melani C,Enz A,Pepeu G

    更新日期：2007-10-31 00:00:00

  • The effect of sodium nitroprusside on the uptake and efflux of 45Ca from rabbit and rat vessels.

    abstract：:In this study we investigated if sodium nitroprusside (NaNP), a vasodilator with direct action on smooth muscle, would have any effect on calcium kinetics in blood vessels. The effect of NaNP, in 0.1-10 micrometer concentration, was studied in vitro on the uptake of 45Ca with the lanthanum method and on the efflux of ...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(77)90052-8

    authors： Zsotér TT,Henein NF,Wolchinsky C

    更新日期：1977-09-01 00:00:00

  • Identification of subtypes of [3H]prazosin-labelled alpha 1 receptor binding sites in rat brain.

    abstract：:Detailed antagonist competition curves for [3H]prazosin-labelled binding sites in rat cerebral cortex membranes reveal anomalous binding characteristics. Dihydroergocryptine and indoramine compete in a steep, monophasic manner while WB4101 and phentolamine exhibit shallow competition curves. Computer-assisted analysis...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章

    doi：10.1016/0014-2999(85)90432-7

    authors： Morrow AL,Battaglia G,Norman AB,Creese I

    更新日期：1985-02-26 00:00:00

  • Gastrointestinal afferents as targets of novel drugs for the treatment of functional bowel disorders and visceral pain.

    abstract：:An intricate surveillance network consisting of enteroendocrine cells, immune cells and sensory nerve fibres monitors the luminal and interstitial environment in the alimentary canal. Functional bowel disorders are characterized by persistent alterations in digestive regulation and gastrointestinal discomfort and pain...

    journal_title：European journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/s0014-2999(01)01319-x

    authors： Holzer P

    更新日期：2001-10-19 00:00:00