Abstract:
:The monoethyl, monopropyl and monoisopropyl esters of succinic acid, administered intravenously at the dose of 2 micromol/g body weight, were found to increase the insulinotropic action of gliquidone (0.2 nmol/g body weight) in anaesthetized rats. The monoisopropyl ester of succinic acid also doubled the hypoglycemic action of gliquidone. These findings indicate that it is possible to design esters of succinic acid that are devoid of the risk of generating methanol by intracellular hydrolysis, and yet susceptible to increase both the insulinotropic and hypoglycemic responses to antidiabetic agents.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
García-Martínez JA,Villanueva-Peñacarrillo ML,Valverde I,Björkling F,Malaisse WJdoi
10.1016/s0014-2999(97)00099-xsubject
Has Abstractpub_date
1997-04-23 00:00:00pages
65-8issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(97)00099-Xjournal_volume
325pub_type
杂志文章abstract::Obesity-associated non-alcoholic fatty liver disease (NAFLD) increases coagulation and inflammation. We hypothesized that (S)YS-51, an agent found to be beneficial in animal models of sepsis, may reduce NAFLD in high-fat diet (HFD) mice by reducing coagulation and inflammation. C57BL/6 mice were fed either a chow diet...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2016.06.040
更新日期:2016-10-05 00:00:00
abstract::The use of antipsychotic medication has consistently been associated with serious side effects including weight gain and metabolic abnormalities. Strategies for mitigating these side effects have been tested, yet effective interventions have not been identified. The current study tested whether two recently identified...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2011.01.019
更新日期:2011-03-25 00:00:00
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
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doi:10.1016/s0014-2999(98)00207-6
更新日期:1998-04-17 00:00:00
abstract::Pulmonary and systemic hemodynamic effects of delta 9-tetrahydrocannabinol (delta 9-THC) in conscious dogs and in those anesthetized with morphine (3 mg/kg, i.m.) plus alpha-chloralose (100 mg/kg i.v.) were evaluated in this study. A decrease in the heart rate, cardiac output (PBF) and a concomitant increase in the pu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(78)90268-6
更新日期:1978-12-15 00:00:00
abstract::Imatinib (IMA) is the standard treatment for CML; however, stopping IMA sometimes results in disease relapse, which suggests that leukemic stem cells (LSCs) remain in such patients, even after complete molecular remission has been achieved. Therefore, new strategies will be required to eradicate LSCs. The Janus kinase...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2018.02.022
更新日期:2018-04-15 00:00:00
abstract::The neuroprotective effects of erythropoietin on 1-methyl-4-phenylpyridinium (MPP(+))-induced oxidative stress and apoptosis in cultured PC12 cells as well as the underlying mechanism were investigated. Treatment of PC12 cells with MPP(+) caused the loss of cell viability, which was associated with the elevation in ap...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.02.020
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abstract::The localization of natriuretic peptide receptors was studied in LLC-PK1 cell monolayers grown on a micro-porous membrane filter. The addition of alpha-human atrial natriuretic peptide (alpha-hANP) to the apical side of the cells produced a concentration-dependent increase in cyclic GMP (cGMP) formation, the extent of...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90071-x
更新日期:1994-08-16 00:00:00
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
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abstract::We investigated whether or not insulin and cAMP-elevating agents induce the proliferation of adult rat hepatocytes during the early and late phases of primary culture. Adult rat hepatocytes synthesized a significant amount of DNA when cultured in the presence of 10(-7) M insulin for 3 h. Under these conditions, the nu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)89682-3
更新日期:1997-05-26 00:00:00
abstract::The relationship between two known actions of prednisolone-3, 20-bisguanylhydrazone (PBGH); Na+, K+-ATPase inhibition and positive inotropic effects, was investigated. In electrically driven left atrial preparations of guinea pig heart, the positive inotropic action of PBGH was not affected by beta-adrenergic or hista...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(78)90068-7
更新日期:1978-05-15 00:00:00
abstract::The effects of phenoxybenzamine on alpha 1- and alpha 2-adrenergic receptor binding sites were examined directly using radioligand binding assays of the antagonist drugs [125I]BE 2254 and [3H]rauwolscine, respectively, in homogenates of rat cerebral cortex. Treatment with phenoxybenzamine caused an irreversible, dose-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(83)90458-2
更新日期:1983-10-14 00:00:00
abstract::The long-term survival of rats with healed myocardial infarction and congestive heart failure treated with milrinone, enalapril and the combination of milrinone plus enalapril, was documented. Seven days after sham or coronary ligation, 200 rats (99 sham and 101 myocardial infarcted) were randomized based on electroca...
journal_title:European journal of pharmacology
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abstract::The binding of [3H]LSD to serotonergic sites in human brain was studied. The pharmacological profile of [3H]LSD binding in frontal cortex differed to that in hippocampus. Analysis of the inhibition of [3H]LSD binding by serotonin and spiperone was consistent with the presence of two binding sites, which differed in ph...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90555-6
更新日期:1982-08-13 00:00:00
abstract::Insulin resistance is a condition in which the glycemic response to insulin is less than normal. The change in insulin sensitivity leads to several sets of responses. One set effects the beta cell and leads to its accelerated destruction and the development of diabetes mellitus. The other set generates a series of non...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2004.02.051
更新日期:2004-04-19 00:00:00
abstract::Metabotropic glutamate mGlu(1) receptors play a modulatory role in the nervous system. They enhance cell excitability, modulate synaptic neurotransmission and are involved in synaptic plasticity. During the last 10 years, several selective metabotropic glutamate mGlu(1) receptor competitive antagonists and potentiator...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2009.12.043
更新日期:2010-08-10 00:00:00
abstract::Organ culture is an in vitro method for investigating cellular mechanisms involved in upregulation of vasocontractile G-protein coupled receptors. We hypothesize that mitogen-activated-protein kinase (MEK) and/or extracellular-signal-regulated kinase (ERK) specific inhibitors will attenuate the G-protein coupled recep...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2010.06.053
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abstract::Many studies have demonstrated that cyclophosphamide (CPA) can affect hepatic cytochrome p450 (CYP) isoenzyme activity in animals. We have investigated the effect of CPA on gene expression of various CYP enzymes as well as beta-actin in the human acute promyelocytic leukemia cell line (HL-60S) and its multidrug-resist...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01995-7
更新日期:2002-08-09 00:00:00
abstract::Methadone used for opioid dependence therapy is associated with increased pain sensitivity. This study aimed to investigate whether methadone administration lowers nociceptive threshold in adult male Sprague-Dawley (SD) rats, and if this threshold could be altered by the NMDA receptor antagonist memantine. Rats were i...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2009.09.056
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abstract::In this study we have investigated the functional activity of GR127935 (2-methyl-1,2,4 oxadiazol-3-yl)-biphenyl-[4-carboxylic acid 4-methoxy-3-(4-methyl-piperazine-1-yl]-amide) at human 5-HT1D alpha and 5-HT1D beta receptors which have been expressed in a Chinese Hamster Ovary (CHO) cell line. Using [35S] GTP gamma S ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00579-1
更新日期:1996-10-31 00:00:00
abstract::Current clinical options for the treatment of neovascular disorders of the posterior segment of the eye have several drawbacks. Photocoagulation lasers can impair peripheral and night vision. Photodynamic therapies as well as intravitreal macromolecule injections (Macugen and Lucentis) require frequent, invasive admin...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2007.04.044
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abstract::The effects of loxapine and its hydroxylated metabolites 7-hydroxyloxapine and 8-hydroxyloxapine on 3H-spiroperidol binding to rat striatal membranes were investigated. Whereas 7-hydroxyloxapine and loxapine displayed strong affinities for 3H-spiroperidol binding sites, 8-hydroxyloxapine was essentially inactive. The ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90396-0
更新日期:1979-04-15 00:00:00
abstract::Levtiracetam (Lev), an inhibitor of SV2A (synaptic vesicle protein A2), affected the ATP-dependent priming of Ca(2+)-regulated exocytosis in antral mucous cells of guinea pig. In antral mucous cells, the Ca(2+)-regulated exocytosis, which is activated by acetylcholine (ACh), consists of an initial peak that declines r...
journal_title:European journal of pharmacology
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doi:10.1016/j.ejphar.2013.09.037
更新日期:2013-12-05 00:00:00
abstract::We studied the relationships between arachidonic acid (AA) metabolism and contractile responses to Na arachidonate (NaA) and the prostaglandins (PGs) in mesenteric arteries isolated from sham-operated and totally pancreatectomized dogs. PGE2 and PGF2 alpha produced a similar dose-dependent relaxation of mesenteric art...
journal_title:European journal of pharmacology
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abstract::The present study examines whether a correlation exists between cyclic nucleotides and the mechanism of action of arginine vasopressin (AVP) on adrenocorticotropin hormone (ACTH) secretion from pituitary corticotrophs. Incubation of cultured anterior pituitary cells with 3-isobutyl-1-methylxanthine (IBMX) or Rolipram ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90043-5
更新日期:1989-01-02 00:00:00
abstract::In this study the effect of purified rat anti-mouse IL-5 monoclonal antibody on aeroallergen-induced infiltration of eosinophils in the bronchoalveolar lavage fluid of guinea pigs was studied. The i.p. injection of anti-IL-5 antibody 4 h after aeroallergen challenge inhibited eosinophil infiltration in a dose-dependen...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90273-7
更新日期:1992-01-28 00:00:00
abstract::In this work, the involvement of ionotropic glutamatergic receptors and nitric oxide on striatal dopamine release induced by anatoxin-a was investigated in conscious and freely-moving rats. To study the participation of glutamatergic receptors, the effects of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (A...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.07.044
更新日期:2006-10-24 00:00:00
abstract::The effect of prolonged administration of high doses of buspirone on its 5-hydroxytryptamine (5-HT) release-inhibitory and anxiolytic-like properties was investigated. The 5-HT release-inhibitory effect of a challenge dose of buspirone (0.5 mg/kg, s.c.) was identical in rats chronically treated with vehicle or buspiro...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90977-p
更新日期:1993-08-03 00:00:00
abstract::This paper presents the effect of 14-day intraperitoneal (i.p.) neuroleptic treatment on the behavioural response of Wistar rats to (-)-quinpirole hydrochloride (3 mg/kg, i.p.) administered 24 h after the last neuroleptic dose. Chlorpromazine hydrochloride (10 mg/kg), haloperidol (2 mg/kg) or (+/-)-sulpiride (100 mg/k...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00666-4
更新日期:1999-11-19 00:00:00
abstract::The pathophysiology of chronic neurodegenerative diseases, as Alzheimer's diseases, has remained inaccessible till recently. But this situation is changing quickly. In the past decades, genes causing familiar forms of the disease have been identified and provided the genetic framework for the emerging amyloid hypothes...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2009.10.020
更新日期:2010-01-10 00:00:00
abstract::In the present study, the emetic effect of the anticancer drug cisplatin, and the protective effects of 5-HT3 receptor antagonists against cisplatin emesis were investigated in the pigeon. The experimental set-up involved the i.v. administration of drugs and subsequent observation of the percentage of vomiting animals...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90721-f
更新日期:1992-10-20 00:00:00