Abstract:
:Gastric mucosa is frequently exposed to various gastric irritants, and there is a continuing requirement to develop new gastro-protective agents. This study compares the effects of three such agents, sucralfate, rebamipide, and cimetidine in both in vivo and in vitro indomethacin-induced gastric damage models. For the in vivo approach, rats were orally administered sucralfate, rebamipide, and cimetidine at 300 mg/kg before an acute dose of indomethacin (30 mg/kg). Gastric lesions were then macroscopically examined. For the in vitro approach, gastric mucosal cells were incubated with sucralfate (3 and 5 mg/mL), rebamipide (0.3 and 1 mm), and cimetidine (10 and 50 μg/mL) before exposure to indomethacin (3.8 mm). The release of lactate dehydrogenase (LDH) and mitochondrial function were then measured. Sucralfate, rebamipide, and cimetidine displayed gastro-protective effects in vivo (decreased number of gastric ulcers: -50% P < 0.05, -22% NS, and -69% P < 0.05, respectively, and reduced length of gastric lesions: -62% P < 0.05, -29% NS, and -70% P < 0.001, respectively). Cell damage induced by indomethacin in vitro was inhibited by sucralfate (LDH release) and by rebamipide and cimetidine (mitochondrial function and LDH release). In contrast, sucralfate accentuated the indomethacin-induced decrease in mitochondrial function. Although cultured gastric cells offer a promising tool for evaluating the cytotoxic or protective effects of test compounds, data from in vivo models are still needed to confirm in vitro data. Using both approaches provides more comprehensive insight into the effects of test compounds on the gastric mucosa.
journal_name
Fundam Clin Pharmacoljournal_title
Fundamental & clinical pharmacologyauthors
Goineau S,Castagné Vdoi
10.1111/fcp.12248subject
Has Abstractpub_date
2017-04-01 00:00:00pages
155-164issue
2eissn
0767-3981issn
1472-8206journal_volume
31pub_type
杂志文章abstract::The aim of this study was to investigate biochemical and antioxidant parameters in alloxan-resistant (ALR) and alloxan-susceptible (ALS) rats. Diabetes was induced in 60-day-old male Wistar rats by a single intraperitonial injection of alloxan (AL, 150 mg/kg). Ten days after induction, a group of rats showed a signifi...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2008.00628.x
更新日期:2008-12-01 00:00:00
abstract::Ivermectin, a parasiticide that long ago proved its worth in veterinary medicine, became one of the most effective tools for control programs against human filarial diseases in the 1980s. It is provided at no cost, is effective against microfilariae (blocking their transmission) and can be administered annually as a s...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1046/j.1472-8206.2003.00170.x
更新日期:2003-04-01 00:00:00
abstract::In addition to their direct effects on cardiac contractility, a number of positive inotropic agents also induce, through direct peripheral vasodilation, a reduction in afterload which is of major importance in their beneficial effects in the treatment of congestive heart failure. However, the induced increase in cardi...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1991.tb00759.x
更新日期:1991-01-01 00:00:00
abstract::It has been suggested that salicylate hydroxylation can be used to detect hydroxyl radical formation in vivo. In the present study we investigated the effects of verapamil and or ryanodine on salicylate (SA) and its hydroxylated adduct; 2,3-dihydroxybenzoic acid (2,3-DHBA) levels in glutamate induced neurotoxicity of ...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2000.tb00389.x
更新日期:2000-01-01 00:00:00
abstract::The hypotensive and negative chronotropic effects of 5 calcium entry blockers (verapamil 200 micrograms/kg IV; diltiazem 300 micrograms/kg IV; nifedipine 5 micrograms/kg IV; nicardipine 50 micrograms/kg IV; and bepridil 5 mg/kg IV) were compared in control normotensive and acute neurogenic hypertensive anaesthetized d...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1987.tb00548.x
更新日期:1987-01-01 00:00:00
abstract::Abstract The relationship between depression and dopamine deficiency in the mesolimbic pathway has been hypothesized for many years. The experimental studies with animal models of depression and the human studies implicate the role of the dopamine system in depression. Not only do dopaminergic receptor agonists, but a...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2004.00287.x
更新日期:2004-12-01 00:00:00
abstract::A number of antiplatelet drugs, principally aspirin alone or in combination, have been evaluated in randomized trials of survivors of prior occlusive vascular disease events or of individuals at high risk because of multiple cardiovascular risk factors. In this meta-analysis we compare single and dual antiplatelet reg...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,meta分析
doi:10.1111/j.1472-8206.2008.00582.x
更新日期:2008-06-01 00:00:00
abstract::The new oral anticoagulants are announced as an important therapeutic revolution, particularly after their approval by authorities for stroke prevention in atrial fibrillation. However, the pharmacology of these new drugs is not homogeneous. In this review, we summarize the main pharmacological characteristics of the ...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/fcp.12091
更新日期:2015-02-01 00:00:00
abstract::By use of a simple anticonflict procedure (Vogel test), it was demonstrated that L-pyroglutamic acid (L-pyrrolidone carboxylic acid [L-PCA]), an amino acid naturally occurring in mammalian tissues and fluids, possesses anxiolytic activity. This tissues and fluids, possesses anxiolytic activity. This effect was stereos...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1988.tb00623.x
更新日期:1988-01-01 00:00:00
abstract::In addition to their effects on blood pressure, antihypertensive agents may produce additional effects on blood rheology and arterial compliance abnormalities which may play a role in target-organ damage. However, these effects may depend only on the specific pharmacological properties of certain antihypertensive agen...
journal_title:Fundamental & clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1111/j.1472-8206.1998.tb00972.x
更新日期:1998-01-01 00:00:00
abstract::Advances in paediatric clinical pharmacology are interdependent with a better understanding of the influence of growth on drug disposition and action. In this field, there is an increasing need for non-invasive drug monitoring approaches. This paper aims to discuss the role of positron emission tomography in such prac...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2008.00650.x
更新日期:2008-12-01 00:00:00
abstract::France is experiencing an increase in the number of opioid prescriptions and related fatalities. We carried out a retrospective observational study using data from the Paris PCC over a 10-year period. The main objective was to obtain an epidemiological description of the severe reported cases. The secondary objectives...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12534
更新日期:2020-08-01 00:00:00
abstract::The maturation of the N-acetyltransferase-dependent AFMU production from caffeine was studied during infancy. The group of children (N = 14) consisted of 4 premature newborn infants and ten 1-19 month-old infants who received caffeine citrate solution for the treatment and prevention of apnea. Caffeine, AFMU, 1X and 9...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1989.tb00461.x
更新日期:1989-01-01 00:00:00
abstract::The present study examined 15 patients previously resistant to conventional antihistamines, in which doxepin at doses in the range of 50-75 mg/day was shown to be effective in treatment of chronic urticaria and without significant adverse side effects. However, some controversy remains about its mechanism of action in...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1990.tb00482.x
更新日期:1990-01-01 00:00:00
abstract::HMG CoA reductase inhibitors (statins) have an established place in the treatment of coronary artery disease. However, their role in the treatment of heart failure (HF), including HF due to coronary artery disease, has been controversial since beneficial as well as possible harmful effects may occur. Several recent st...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2007.00538.x
更新日期:2007-11-01 00:00:00
abstract::Free radical species have been implicated as important agents involved in myocardial ischemic and reperfusion injuries. Superoxide is capable of mobilizing iron from ferritin and the released iron can cause hydroxyl formation from H2O2. The aim of this study was to evaluate the time-dependent increase in lipid peroxid...
journal_title:Fundamental & clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1111/j.1472-8206.1998.tb00947.x
更新日期:1998-01-01 00:00:00
abstract::The aim of this study was to characterize the model of oxidative stress consisting in the infection of malonate (3 mumol), an inhibitor of mitochondrial complex II, in the rat striatum. The striatal concentrations of both the reduced and oxidized forms of glutathione (the major endogenous antioxidant) were determined ...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2004.00297.x
更新日期:2005-02-01 00:00:00
abstract::Using an isolated non-working rat heart model, this study investigated the mechanisms of pharmacological pre-conditioning (PC) induced by P2Y receptor stimulation with pyridoxal-5'-phosphate (PLP). After 6-hydroxydopamine pretreatment and a 15-min stabilization period, isolated rat hearts were perfused for 25 min then...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2009.00677.x
更新日期:2009-06-01 00:00:00
abstract::ATP-Binding Cassette transporters such as ABCG2 confer resistance to various anticancer drugs including irinotecan and its active metabolite, SN38. Early quantitative evaluation of efflux transporter inhibitors-cytotoxic combination requires quantitative drug-disease models. A proof-of-concept study has been carried o...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12005
更新日期:2014-04-01 00:00:00
abstract::The contractile activity of (-)-Bay k 8644 was assessed in rat isolated aortic ring preparations bathed in a potassium-free medium. (-)-Bay k 8644 (0.01-3 microM) caused extracellular calcium-dependent contractile responses, which were significantly greater in tissues with, than deprived of a functional endothelium. I...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1989.tb00469.x
更新日期:1989-01-01 00:00:00
abstract::A meta-analysis was performed on the results of clinical trials of buflomedil in intermittent claudication. The analysis used results from 744 patients enrolled in ten studies, conducted at 42 centers in seven countries. All studies were randomized, double-blind, placebo-controlled trials which measured improvement in...
journal_title:Fundamental & clinical pharmacology
pub_type: 临床试验,杂志文章,meta分析
doi:10.1111/j.1472-8206.1995.tb00515.x
更新日期:1995-01-01 00:00:00
abstract::Anticonvulsant action of CGP 40116, a competitive antagonist of N-methyl-D-aspartate type of excitatory amino acid receptors, was studied in rats during development (7, 12, 18, 25 and 90 days old). Two types of motor seizures were elicited by a subcutaneous injection of pentylenetetrazol. Pretreatment with CGP 40116 d...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1998.tb00981.x
更新日期:1998-01-01 00:00:00
abstract::In this review, the major enzyme systems involved in vivo in the oxidative metabolism of xenobiotic amines in humans are discussed, i.e. the monooxygenases [cytochrome P450 system (CYPs) and flavin-containing monooxygenases (FMOs)] and the amine oxidases (AOs). Concerning the metabolism of xenobiotic amines (drugs in ...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.2007.00498.x
更新日期:2007-10-01 00:00:00
abstract::Restenosis after coronary angioplasty, the main limitation of interventional cardiology, remains an unsolved issue. The failure to-date of all pharmacological attempts at prevention has prompted the development of alternative strategies. A mechanistic approach to the problem of restenosis is based on the assumption th...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.1995.tb00259.x
更新日期:1995-01-01 00:00:00
abstract::Quercetin is a flavonol polyphenol widely found in many vegetables, grains, and fruits. Quercetin has been shown to inhibit proliferation and invasion of various glioma cells and is regarded as a potential anticancer agent against glioma. However, whether and how this drug could affect brain blood vessels and endothel...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12514
更新日期:2020-04-01 00:00:00
abstract::The action of ouabain, a cell membrane Na+, K+-ATPase blocker, on contractions induced by manganese ions (Mn2+) in Ca2+-free, isotonic solutions with varying concentrations of K+ in the external medium were investigated in order to evaluate the underlying role of external Na+ in Mn2+-induced contractions in isolated t...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2005.00334.x
更新日期:2005-06-01 00:00:00
abstract::In the present study, contractile responses and [3H]-noradrenaline overflow evoked by electrical field stimulation were assessed, respectively, in the small mesenteric artery and in tail artery removed from rats pre-treated with either saline or lipopolysaccharide (LPS). In small mesenteric arteries, LPS treatment did...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.2000.tb00445.x
更新日期:2000-11-01 00:00:00
abstract::The aim of this review is to comment the results described in the literature concerning the possible pharmacodynamic mechanisms involved in the improvement of quality of life of angiotensin converting enzyme inhibitors that is just a working hypothesis. These drugs, widely used in the treatment of hypertension, preven...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1111/j.1472-8206.1996.tb00592.x
更新日期:1996-01-01 00:00:00
abstract::Abuse of alcohol triggers neurodegeneration in human brain. Minocycline has characteristics conferring neuroprotection. Current study evaluates the role of the CREB-BDNF signaling pathway in mediating minocycline's neuroprotective effects against alcohol-induced neurodegeneration. Seventy adult male rats were randomly...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/fcp.12584
更新日期:2020-06-24 00:00:00
abstract::The involvement of radical reactions in the ageing process, physiological as well as pathological, is well demonstrated. It is accepted that alloxan cyto-toxicity is linked to a production of hydroxylated free radicals and that a substance preventing the development of alloxanic diabetes possesses scavenger properties...
journal_title:Fundamental & clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1472-8206.1989.tb00673.x
更新日期:1989-01-01 00:00:00