Abstract：
:The insulinotropic action of several new esters of succinic acid was assessed in isolated rat islets incubated in the presence of 7 mM D-glucose. An efficient secretory response was observed with the monobenzyl, monoisopropyl, monoallyl, monopropyl, monoethyl, monobutyl, dibutyl, dipropyl and diallyl esters of succinic acid. This indicates that it is possible to design esters of succinic acid which act as insulin secretagogues, while avoiding the undesirable generation of methanol that otherwise results from the use of either the monomethyl or dimethyl ester of this dicarboxylic acid.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Björkling F,Malaisse-Lagae F,Malaisse WJdoi
10.1006/phrs.1996.0038subject
Has Abstractpub_date
1996-04-01 00:00:00pages
273-5issue
4-5eissn
1043-6618issn
1096-1186pii
S1043-6618(96)90038-9journal_volume
33pub_type
杂志文章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：:The protective effect of L-carnitine or coenzyme Q10 (CoQ10) against high magnetic field (20 mT) induced testicular toxicity in mice were evaluated. Animals were injected with L-carnitine (200 mg kg(-1), i.p.) or CoQ10 (200 mg kg(-1), p.o.) 1h before exposure to fractionated doses (30 min per day, three times per week...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043661802001718
更新日期：2002-10-01 00:00:00
abstract：:By the use of combined radioreceptor binding and autoradiographic techniques we attempted to analyse the biochemical characteristics and the anatomical localization of GABA-B receptors in sections of rat circle of Willis and pialarachnoid arteries. 3H-GABA in the presence of 40 microM isoguvacine and 2.5 mM CaCl2 was ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(90)90731-r
更新日期：1990-05-01 00:00:00
abstract：:Macroscale delivery systems that can be locally implanted on the tumor tissue as well as avoid all the complications associated to the systemic delivery of therapeutics have captured researchers' attention, in recent years. Particularly, the microneedle-based devices can be used to efficiently deliver both small and m...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104438
更新日期：2019-10-01 00:00:00
abstract：:We tested the efficacy of novel cyclooxygenase 2 (COX-2) inhibitors in counteracting glia-driven neuroinflammation induced by the amyloidogenic prion protein fragment PrP90-231 or lipopolysaccharide (LPS). In search for molecules with higher efficacy than celecoxib, we focused our study on its 2,3-diaryl-1,3-thiazolid...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.09.010
更新日期：2016-11-01 00:00:00
abstract：:Augmented vasoconstriction is a hallmark of hypertension and is mediated partly by hyper-stimulation of G protein couple receptors (GPCRs) and downstream signaling components. Although GPCR blockade is a key component of current anti-hypertensive strategies, whether hypertension is better managed by directly targeting...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.01.012
更新日期：2019-03-01 00:00:00
abstract：:Exogenously administered fructose-1,6-diphosphate (FDP) has been studied for its ability to protect tissue during hypoxia or ischemia. Recently, a clear effect of FDP on the central nervous system has raised the question whether FDP can get into the brain. FDP levels were measured in blood, brain, liver, kidney, muscl...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2008.01.008
更新日期：2008-03-01 00:00:00
abstract：:Local microcirculatory dysfunction within the pancreatic gland might be an important factor in the conversion of oedematous to necrotizing pancreatitis. Therapeutic agents, improving the pancreatic blood flow, might be valuable in acute pancreatitis treatment. An influence of nitric oxide, heparin and procaine treatme...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0200
更新日期：1997-08-01 00:00:00
abstract：:Rats were treated with furosemide at intraperitoneal doses of 10, 20, and 30 mg kg(-1)day(-1)for 21 days, and some indices of thiamin status (liver, blood and urine thiamin concentrations, erythrocyte transketolase (TK) activity, and thiamin pyrophosphate (TPP) effect, which refers to the increase in TK activity in a ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1999.0632
更新日期：2000-07-01 00:00:00
abstract：:The human gut is populated by an array of bacterial species, which develop important metabolic and immune functions, with a marked effect on the nutritional and health status of the host. Dietary component also play beneficial roles beyond basic nutrition, leading to the development of the functional food concept and ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2009.11.001
更新日期：2010-03-01 00:00:00
abstract：:Efficacy and safety assessments are essential thresholds for drug candidates from preclinical to clinical research. Conventional mammalian in vivo models cannot offer rapid pharmacological and toxicological screening, whereas cell-based or cell-free in vitro systems often lead to inaccurate results because of the lack...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.04.011
更新日期：2018-07-01 00:00:00
abstract：:An important aspect of brain cholinesterase function is related to enzymatic differences. The brain of mammals contains two major forms of cholinesterases: acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The two forms differ genetically, structurally and for their kinetics. Butyrylcholine is not a physi...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2003.11.017
更新日期：2004-10-01 00:00:00
abstract：:Dementia with Lewy bodies (DLB) is a serious age-dependent human neurodegenerative disease, with multiple debilitating symptoms, including dementia, psychosis and significant motor deficits, but with little or no effective treatments. This comparative ligand autoradiographical study has quantified histamine H3 recepto...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.08.034
更新日期：2016-11-01 00:00:00
abstract：:The sphingolipid field has made significant strides over the past 10 years: from identifying metabolites of the sphingomyelin pathway as second messengers to discerning the molecular biology and biophysics of these lipid-derived second messengers. Building upon this vast basic science literature, scientists from multi...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/s1043-6618(03)00048-3
更新日期：2003-05-01 00:00:00
abstract：:Plasma lipid and lipoprotein levels were evaluated in 27 adults with essential hypertension at four different periods during a 12-month treatment with doxazosin. Mean plasma total cholesterol (TC), low-density lipoprotein-cholesterol (LDLC), triglyceride (TG), very low density lipoprotein-cholesterol (VLDLC) and the L...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1016/1043-6618(94)80108-8
更新日期：1994-10-01 00:00:00
abstract：:Cysteamine, a potent somatostatin depletor, was used in the present study to investigate the role of endogenous somatostatin in acute peripheral inflammation. The acute inflammation was induced by intraplantar injection of carrageenan (1%), histamine (5 micromol), or formalin (2.5%) in the rat hind paw. The induced in...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2002.0955
更新日期：2002-04-01 00:00:00
abstract：:The influence of intracerebroventricular (i.c.v.) injections of (S)-3,5-dihydroxyphenyl-glycine (S)-3,5-DHPG, a selective agonist of group I metabotropic glutamate receptors (mGluRs), on the activity of the central nervous system was examined in male rats. (S)-3,5-DHPG at doses of 25, 50 and 100 nmol significantly att...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2000.0683
更新日期：2000-09-01 00:00:00
abstract：:In this study, we have investigated the vasodilator response to acetylcholine under diabetic conditions in isolated renal arteries of Wistar rats. The effect of nitric oxide synthase (NOS) inhibition on acetylcholine-induced vasodilator response was investigated. We have also examined the effects of two endothelium-de...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(03)00109-9
更新日期：2003-09-01 00:00:00
abstract：:Paradoxical sleep deprivation in rats is considered as an experimental animal model of mania endowed with face, construct, and pharmacological validity. We induced paradoxical sleep deprivation by placing rats onto a small platform surrounded by water. This procedure caused the animal to fall in the water at the onset...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.11.029
更新日期：2017-03-01 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：:Asthma and COPD make up the majority of obstructive airways diseases (OADs), which affects ∼11 % of the population. The main drugs used to treat OADs have not changed in the past five decades, with advancements mainly comprising variations on existing treatments. The recent biologics are beneficial to only specific su...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105029
更新日期：2020-09-01 00:00:00
abstract：:A bovine dopamine transporter (bDAT) cDNA was transfected into CV-1 cells, a cell line that lacks vesicular storage and release mechanisms. Using this cell line, the effects of neuroleptic drugs on DAT-mediated uptake and release of dopamine (DA) were examined. All of the neuroleptic drugs tested, inhibited DA uptakes...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：
更新日期：1997-05-01 00:00:00
abstract：:The interaction of mianserin with ethanol in central nervous system (CNS) was investigated. Mianserin was administered at a single dose of 5 or 20 mgkg(-1) i.p. or as daily injections in a dose of 2.5 mgkg(-1) given for 14 days. The influence of mianserin on acute ethanol toxicity (LD(50)), on ED(50) of ethanol in rot...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(02)00031-2
更新日期：2002-07-01 00:00:00
abstract：:Most solid tumor cells adapt to their heterogeneous microenvironment by depending largely on aerobic glycolysis for energy production, a phenomenon called the Warburg effect, which is a hallmark of cancer. The altered energy metabolism not only provides cancer cell with ATP for cellular energy, but also generate essen...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104511
更新日期：2019-12-01 00:00:00
abstract：:The gut microbiota and its short chain fatty acid (SCFA) metabolites have been established to play an important protective role against neurodegenerative diseases. Our previous study demonstrated that cerebral ischemic stroke triggers dysfunctional gut microbiota and increased intestinal permeability. In this study, w...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104403
更新日期：2019-10-01 00:00:00
abstract：:Bleomycin (BLM) is a drug used to treat different types of neoplasms. BLM's most severe adverse effect is lung toxicity, which induces remodeling of lung architecture and loss of pulmonary function, rapidly leading to death. While its clinical role as an anticancer agent is limited, its use in experimental settings is...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2015.04.012
更新日期：2015-07-01 00:00:00
abstract：:ABT-737, ABT-263 (Navitoclax) and ABT-199 (Venetoclax) are under intensive preclinical and clinical investigation as treatments for hematologic and other malignancies. These small molecules mimic pro-death B-cell lymphoma-2 (Bcl-2) Homology 3 (BH3) domain-only proteins. They also bear a structural resemblance to certa...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.01.040
更新日期：2019-04-01 00:00:00
abstract：:CHF5074 is a non-steroidal anti-inflammatory derivative holding disease-modifying potential for the treatment of Alzheimer's disease. The aim of the present study was to characterize the electrophysiological and metabolic profile of CHF5074 in the hippocampus. Electrophysiological recordings show that CHF5074 inhibits...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2014.02.010
更新日期：2014-03-01 00:00:00
abstract：:The aqueous extract from aerial parts of Artemisia copa Phil. (Compositae), was evaluated for antinociceptive activity using writhing, formalin, and hot-plate tests in mice. A dose-related antinociceptive response was obtained in the writhing test at doses of 500 and 1000 mg/kg p.o. (percentage of inhibition 23.3 and ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2003.12.016
更新日期：2004-07-01 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
