Abstract:
:The insulinotropic action of the meglitinide analogues KAD-1229, A-4166 and repaglinide was examined in rat pancreatic islets deprived of exogenous nutrient or incubated in the presence of nutrient secretagogues such as D-glucose and the methyl esters of pyruvic acid, succinic acid and glutamic acid. The meglitinide analogues exerted little effect on insulin release in the absence of exogenous nutrient or in the presence of methyl pyruvate. They caused obvious stimulation of insulin output in the presence of D-glucose, dimethyl succinate or dimethyl glutamate. It is proposed, therefore, that suitable esters of dicarboxylic nutrients could be used to potentiate the secretory response to meglitinide analogues in non-insulin-dependent diabetes mellitus.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Bakkali Nadi A,Zhang TM,Malaisse WJdoi
10.1006/phrs.1996.0026subject
Has Abstractpub_date
1996-03-01 00:00:00pages
191-4issue
3eissn
1043-6618issn
1096-1186pii
S1043661896900262journal_volume
33pub_type
杂志文章abstract::Given the high and increasing prevalence of obesity, the safe and effective treatment of obesity would be beneficial. Here, we examined whether oral hydroxysafflor yellow A (HSYA), an active compound from the dried florets of Carthamus tinctorius L., can reduce high-fat (HF) diet-induced obesity in C57BL/6 J mice. Our...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.05.012
更新日期:2018-08-01 00:00:00
abstract::Ginseng is one of the most popular herbal remedies. Studies were performed in anaesthetized rats to examine the effect of ginseng on bile secretion. Male Sprague-Dawley rats were anaesthetized with intraperitoneal (i.p.) urethane (1.25 g kg(-1)) and equipped with biliary cannulas inserted into the bile duct through th...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2002.0961
更新日期:2002-04-01 00:00:00
abstract::Myocardial infarction (MI) is a major cause of morbidity and mortality in western countries and the formation of intracoronary thrombi is recognized as a critical determinant of this ischaemic event. Since streptokinase and urokinase cause in vitro lysis of clots, it was though that these drugs were also effective in ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/1043-6618(89)90233-8
更新日期:1989-03-01 00:00:00
abstract::We investigated the anti-platelet effect of a newly synthesized guanidine derivative KR-32560, a sodium/hydrogen exchanger-1 (NHE-1) inhibitor, together with the elucidation of the possible mode of action. KR-32560 concentration dependently inhibited the aggregation of washed rabbit platelets induced by collagen (10 m...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.12.003
更新日期:2006-03-01 00:00:00
abstract::Results presented in this study demonstrate an association between the L-Histidine-mediated enhancement of H2O2-induced cytotoxicity and the formation of DNA double strand breakage (DSB), whereas no relationship exists between the increased cytotoxic response and DNA single strand breakage (SSB). Indeed, the higher le...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(94)80041-3
更新日期:1994-02-01 00:00:00
abstract::The effect of dexamethasone on the ability of activated J774 macrophages to inhibit platelet aggregation was investigated. After 24h incubation with lipopolysaccharide and gamma-interferon, J774 cells generated large amounts of nitric oxide and inhibited platelet aggregation. Incubation of the cells with dexamethasone...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1993.1016
更新日期:1993-02-01 00:00:00
abstract::Flibanserin has been reported to be an agonist at 5-HT1A-receptors and an antagonist at 5-HT2A receptors, with higher affinity for 5-HT1A receptors. Despite the fact that less receptor occupation is required by full agonists than by antagonists to exert their effects, flibanserin was shown to exert 5-HT2A antagonism a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0762
更新日期:2001-02-01 00:00:00
abstract::Quiescent hepatic stellate cell (HSC) activation and subsequent conversion into myofibroblasts is the central event in hepatic fibrosis pathogenesis. Epithelial-mesenchymal transition (EMT), another vital participant in liver fibrosis, has the potential to initiate HSC activation, which promotes abundant myofibroblast...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2017.10.013
更新日期:2018-02-01 00:00:00
abstract::The effect of flumazenil (FLU) on plasma protein binding of diazepam (DZ), nordiazepam (ND) and oxazepam (OX) was determined in plasma from drug-naive dogs to which graded concentrations of tested drugs alone and in combination were added. The results revealed that as the concentration of FLU added to plasma alone was...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80018-0
更新日期:1995-11-01 00:00:00
abstract::The modification in the composition of bile acids in hamster by the administration of high dose of ursodeoxycholic acid (UDCA) was investigated. Male Golden Syrian hamsters were divided into five groups: a control group, two groups that received 0.5 g of UDCA per 100 g of standard diet during 30 and 60 days and anothe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(90)90727-u
更新日期:1990-05-01 00:00:00
abstract::Mast cells take part of armamentarium immunologic for host defense against parasitic and bacterial infections. They are derived from bone marrow progenitors and can be activated by immunological and chemical stimuli in order to get its degranulation. The activation of mast cells generates a signalling cascade leaded t...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2009.11.014
更新日期:2010-09-01 00:00:00
abstract::In hypothermic rats with acute hypertension induced by intravenous injection of adrenalin, regional changes in blood-brain barrier permeability to macromolecules were investigated using Evans blue as indication. Evans blue albumin extravasation was determined as a macroscopic finding and a quantitative estimation with...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:
更新日期:1992-07-01 00:00:00
abstract::Kidney disease is a frequent complication in diabetes, and significant differences have been reported between male and female patients. Our working hypothesis was that diabetes might modify the vascular actions of testosterone in isolated rabbit renal arteries and the mechanisms involved in these actions. Testosterone...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2009.09.002
更新日期:2010-02-01 00:00:00
abstract::The epidemic of pneumonia (COVID-19) caused by novel coronavirus (SARS-CoV-2) infection has been listed as a public health emergency of international concern by the World Health Organization (WHO), and its harm degree is defined as a global "pandemic". At present, the efforts of various countries focus on the rapid di...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104929
更新日期:2020-08-01 00:00:00
abstract::Cells continuously turn over proteins through cycles of synthesis and degradation in order to maintain a functional proteome and to exert a tight control in the levels of regulatory proteins. Selective degradation of proteins was initially thought to be an exclusive function of the ubiquitin-proteasome system, however...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2012.10.002
更新日期:2012-12-01 00:00:00
abstract::Metastatic cancers account for more than 90% of cancer mortality. The metastasis of all cancers is critically mediated by enzymes that degrade extracellular matrix. Aggressive tumors are characterized by an imbalance between enzymes that degrade ECM and endogenous inhibitors of the enzymes. Matrix metalloproteinases (...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2010.11.003
更新日期:2011-02-01 00:00:00
abstract::The present study examines the effect of benzyl isothiocyanate (BITC) on uterine contraction in vitro. BITC (10-320 microM) caused irreversible, concentration-dependent inhibition of the spontaneous, prostaglandin F(2alpha) (PGF(2alpha)) and oxytocin-induced force of gravid and non-gravid rat uterine contractions in c...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2003.10.011
更新日期:2004-05-01 00:00:00
abstract::CYT387 is an orally bioavailable, small molecule inhibitor of Janus family of tyrosine kinases (JAK) 1 and 2. It is currently undergoing Phase I/II clinical trials for the treatment of myelofibrosis and myeloproliferative neoplasms. We aimed to establish whether the multidrug efflux transporters P-glycoprotein (P-gp; ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2013.06.009
更新日期:2013-10-01 00:00:00
abstract::Protein tyrosine phosphatases (PTPs), which are ubiquitously expressed in hematopoietic and non-hematopoietic cells, are critical for regulating cell proliferation as well as differentiation in the physiology of multicellular organisms. PTPs regulate the intracellular signaling mechanism of immune cells via dephosphor...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.04.011
更新日期:2019-06-01 00:00:00
abstract::This paper describes a new sensitive gas chromatographic method with electron capture detector to assay estazolam in human plasma, which has been developed and validated for pharmacokinetic purposes. The drug and the internal standard (triazolam) were extracted from plasma buffered at pH 9.0 into toluene and analysed ...
journal_title:Pharmacological research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1006/phrs.1997.0144
更新日期:1997-04-01 00:00:00
abstract::Pharmacokinetics is a relatively young branch of the life sciences, which has developed rapidly in the last 15-20 years, thanks to a series of analytical achievements that have allowed drug concentrations to be measured in biological matrices with highly selective and sensitive methods. Most old drugs and all new drug...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.1997.0254
更新日期:1997-12-01 00:00:00
abstract::Apoptosis of tissues may contribute to ischaemia-reperfusion injury. The aim of the present study was to determine whether administration of a colloid solution would prevent apoptosis after liver ischaemia-reperfusion. New Zealand rabbits, weighing 1.5-2 kg, were randomized to receive either 4% SG (20 ml kg (-1)h(-1) ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2002.0984
更新日期:2002-06-01 00:00:00
abstract::Extrasynaptically located γ-aminobutyric acid (GABA) receptors type A are often characterized by the presence of a δ subunit in the receptor complex. δ-Containing receptors respond to low ambient concentrations of GABA, or respond to spillover of GABA from the synapse, and give rise to tonic inhibitory currents. In ce...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.05.014
更新日期:2016-09-01 00:00:00
abstract::The polyphenol resveratrol is considered to exert many beneficial actions, such as antioxidant, anti-inflammatory, insulin-sensitizer and anticancer effects. Its benefits in patients with type 2 diabetes mellitus (T2DM) are controversial. Our aims were to determine whether resveratrol supplementation at two different ...
journal_title:Pharmacological research
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.phrs.2016.08.010
更新日期:2016-09-01 00:00:00
abstract::Based on the role of ATG7 in the initiation of autophagy, autophagy can be divided into ATG7-dependent selective autophagy and ATG7-independent alternative autophagy. However, the detailed roles of two different types of autophagy in antitumor therapy have not been fully elucidated so far. Here, we for the first time ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105324
更新日期:2021-01-01 00:00:00
abstract:BACKGROUND AND PURPOSE:The enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) hydrolyze endogenous cannabinoids (eCBs), N-arachidonoyl ethanolamine (AEA) and 2-arachidonoyl glycerol (2-AG), respectively. These enzymes also metabolize eCB analogs such as lipoamines and 2-acyl glycerols, most of...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.04.020
更新日期:2016-08-01 00:00:00
abstract::Endocannabinoids are part of a bioactive lipid signaling system, not only in the central nervous system but also in various peripheral organs. Accumulating evidence implicates dysregulation of the endocannabinoid system (ECS) in the pathogenesis of various cardiovascular diseases, including hypertension, atheroscleros...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2009.04.003
更新日期:2009-08-01 00:00:00
abstract::Cardiovascular baroreflex mechanisms and sympathetic tone could be involved in the arterial hypertension by coarctation of abdominal aorta artery (CoA). The present work analyzes the effect on the arterial pressure and heart rate (HR) of the clonidine, an alpha(2)-adrenergic central acting antihypertensive agent, afte...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:
更新日期:2003-07-01 00:00:00
abstract::Previous studies have suggested additional beneficial effects of sodium-glucose co-transporter-2 (SGLT2) inhibitors including the lipid-lowering effect; however, results on lipid profile are controversial. Thus, this meta-analysis aimed to determine the effect of SGLT2 inhibitors treatment on lipid levels in patients ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.105068
更新日期:2020-10-01 00:00:00
abstract::Anti-hypertensive agents may differently stimulate compensatory neuro-hormonal mechanisms and induce different effects on the cardiovascular remodeling and function. The combination of low doses of the two synergistic drugs may lead to a lesser activation of counter regulatory mechanisms and could provide optimal ther...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.10.010
更新日期:2005-04-01 00:00:00