Abstract：
:Successful drug delivery to the central nervous system (CNS) is highly dependent on DMPK as well as physicochemical properties and it is therefore important to characterise these properties and take them into account when designing chemical lead series that act at CNS targets. Since the drug discovery/development process is becoming increasingly focused on reducing the time required to enter molecules into the market, industrial DMPK scientists have emerged from their traditional supportive role in drug development to provide valuable support in the drug discovery process, using novel methods to meet the demands of combinatorial chemistry and bioscience groups.
journal_name
Vascul Pharmacoljournal_title
Vascular pharmacologyauthors
Lundquist S,Renftel Mdoi
10.1016/s1537-1891(02)00203-3keywords:
subject
Has Abstractpub_date
2002-06-01 00:00:00pages
355-64issue
6eissn
1537-1891issn
1879-3649pii
S1537189102002033journal_volume
38pub_type
杂志文章abstract：:Evidence from both clinical and experimental studies indicates that Di-peptidyl peptidase-IV (DPP-4) inhibition may mediate favorable effects on the cardiovascular system. The objective of this study was to examine the acute effects of DPP-4 inhibition on vascular responses and to study the underlying mechanisms of al...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2011.03.001
更新日期：2011-07-01 00:00:00
abstract：BACKGROUND:Antitumor activity of paclitaxel is based on promotion of abnormal microtubule (MT) assembly but it is also considered to have significant pro-inflammatory and anti-angiogenic effects in vivo and thus may cause vascular dysfunction. METHODS:We studied 27 women treated with paclitaxel-containing combinations...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2010.05.002
更新日期：2010-09-01 00:00:00
abstract：OBJECTIVE:The major objective of the present study was to examine the cardioprotective effect of resveratrol, an antioxidant presents in red wine, in the rat after ischemia-reperfusion (I/R). DESIGN:The left coronary artery was in occlusion for 30 min followed by a 120 min reperfusion in anesthetized rats. Animals wer...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2006.04.002
更新日期：2006-08-01 00:00:00
abstract：:Bemiparin is a low molecular weight heparin (LMWH) indicated for the acute treatment of deep vein thrombosis with or without pulmonary embolism, for the prophylaxis of venous thromboembolism in surgical and non-surgical patients and for the prevention of clotting in the extracorporeal circuit during hemodialysis. Due ...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2014.03.001
更新日期：2014-07-01 00:00:00
abstract：OBJECTIVE:In patients with familial combined hyperlipidemia (FCHL), without metabolic syndrome (MS), occurrence of non-alcoholic fatty liver disease (NAFLD) is related to a specific pro-inflammatory profile, influenced by genetic traits, involved in oxidative stress and adipokine secretion. Among FCHL or MS patients, h...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2015.04.004
更新日期：2015-09-01 00:00:00
abstract：:In this study, we have investigated the actions of danshensu, an active, water-extractable component of the medicinal herb danshen (Salvia miltiorrhiza), on rat isolated coronary artery rings precontracted with 1 microM 5-hydroxytryptamine (5-HT) and its action compared to the water-extractable fraction of the herb. E...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2006.10.011
更新日期：2007-04-01 00:00:00
abstract：:Angiogenesis has become an attractive target for the treatment of certain diseases such as cancer and rheumatoid arthritis. Our previous studies demonstrated that the saponin fraction from Gleditsia sinensis fruits had anti-angiogenic potential, and Gleditsiosides B (GB) was probably the main active constituent. In th...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2012.09.006
更新日期：2013-01-01 00:00:00
abstract：:The mechanisms of action involved in the vasorelaxant effect of gallic acid (GA) were examined in the isolated rat thoracic aorta. GA exerted a relaxant effect in the highest concentrations (0.4-10mM) in both endothelium-intact and endothelium-denuded aortic rings. Pre-incubation with L-NAME, ODQ, calmidazolium, TEA, ...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2015.10.010
更新日期：2016-06-01 00:00:00
abstract：:We recently demonstrated that lipoic acid suppresses endotoxin-stimulated expression of inducible nitric oxide synthase and nitric oxide production in mouse macrophages. In this study, we tested whether lipoic acid suppresses these inflammatory mediators in the lungs of rats. Rats were assigned to receive either no sp...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2005.08.005
更新日期：2005-12-01 00:00:00
abstract：:MicroRNAs (miRNAs) have emerged as crucial players regulating the magnitude of gene expression in a variety of organisms. This class of short (22 nucleotides) noncoding RNA molecules have been shown to participate in almost every cellular process investigated so far, and their deregulation is observed in different hum...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2011.07.004
更新日期：2011-10-01 00:00:00
abstract：:β-Adrenoceptors (β-ARs) modulate ERK1/2 and p38 in different cells, but little is known about the contribution of these signaling pathways to the function of β-ARs in vascular tissue. Immunoblotting analysis of rat aortic rings, primary endothelial (ECs) and smooth muscle cells (SMCs) isolated from aorta showed that β...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2014.04.003
更新日期：2014-05-01 00:00:00
abstract：:Tyrosine kinase pathway has been shown to be involved in the effects of hypoxia in pulmonary arteries, but its role in pulmonary vein is not known. The aims of this study were to determine the effect of hypoxia in sheep isolated pulmonary veins and to identify the role of tyrosine kinase pathway in hypoxic response. G...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/s1537-1891(03)00051-x
更新日期：2003-10-01 00:00:00
abstract：:The objective of this study was to determine the mechanism by which Na(+)/H(+) exchanger (NHE) inhibitors induce vasodilatation. The NHE inhibitors, 5-(N,N-dimethyl)-amiloride (DMA), cariporide, and amiloride, evoked endothelium-dependent relaxation in rat aortas with ED50 values of 16, 89, and 148μM, respectively, an...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2012.11.004
更新日期：2013-04-01 00:00:00
abstract：:To investigate the vasorelaxant effect of fasudil mesylate (FM) in vivo and in vitro. The relaxation effect of FM was studied using cerebral vasospasm (CVS) model in vivo and isolated aortic rings in vitro. FM (0.35, 1.2, 3.5 mg·kg⁻¹) increased cerebrovascular flow (CVF) and femoral blood flow (FBF) dose-dependently i...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2011.06.005
更新日期：2011-11-01 00:00:00
abstract：:Next generation sequencing has uncovered a trove of short noncoding RNAs (e.g., microRNAs) and long noncoding RNAs (lncRNAs) that act as molecular rheostats in the control of diverse homeostatic processes. Meanwhile, the tsunamic emergence of clustered regularly interspaced short palindromic repeats (CRISPR) editing h...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2019.02.004
更新日期：2019-03-01 00:00:00
abstract：:Propranolol is a non-selective beta-adrenergic receptor blocker used in the treatment of cardiovascular diseases and migraine prophylaxis. Although it has been shown that propranolol dilates the peripheral arteries of rat, its action in the central nervous system vasculature has not been investigated. In this study, t...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2012.12.004
更新日期：2013-04-01 00:00:00
abstract：:Systemic inflammatory response syndrome (SIRS), initially reported after cardiovascular surgery, has been described after various interventional cardiology procedures, including endovascular/thoracic aortic repair (EVAR/TEVAR), implantation of heart rhythm devices, percutaneous coronary intervention (PCI), electrophys...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2018.04.003
更新日期：2018-04-12 00:00:00
abstract：:MicroRNAs (e.g., miRNAs), endogenously expressed small non-coding RNAs, control gene expression by regulating target messenger RNA at post-transcriptional level. Recent studies have identified a specific role for microRNAs as key regulators of vascular function and dysfunction. The zebrafish (Danio rerio) system is a ...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2011.08.224
更新日期：2011-10-01 00:00:00
abstract：:In systemic sclerosis, microvascular injury often precedes the development of fibrosis. Whereas the development of digital ulcers and skin fibrosis causes high morbidity, the affection of internal organs, in particular complications such as interstitial lung disease and pulmonary (arterial) hypertension, account for t...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2012.12.001
更新日期：2013-03-01 00:00:00
abstract：:The antiplatelet and antithrombotic activities of a newly synthesized CP201, 2-(3,5-di-tert-butyl-4-hydroxyl)-3-chloro-1,4-naphthoquinone on human platelet aggregation in vitro and murine pulmonary thrombosis in vivo were examined. In addition, the antiplatelet activity of CP201 involved in calcium-signaling cascade w...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2004.04.001
更新日期：2004-02-01 00:00:00
abstract：:Hyperhomocysteinemia (HHcy) is a metabolic disorder marked by an excess amount of the amino acid homocysteine (Hcy) in the blood stream. Hcy is a H(2)S precursor-formed from the metabolism of methionine. Elevated Hcy levels have been associated with higher blood pressure. However, the precise contribution of H(2)S to ...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2010.05.004
更新日期：2010-09-01 00:00:00
abstract：:Phosphorylation of proteins on tyrosine acts as a reversible and specific trigger mechanism, forming or disrupting regulatory connections between proteins. Tyrosine kinases and phosphatases participate in multiple cellular processes, and considerable evidence now supports a role for tyrosine phosphorylation in vascula...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1537-1891(03)00009-0
更新日期：2002-11-01 00:00:00
abstract：AIM:Selenium, a trace element involved in important enzymatic activities inside the body, has protective effects against cardiovascular diseases including atherosclerosis. The safe dose of selenium in the organism is very narrow, limiting the supplementation of selenium in diet. The aim of this study is to explore whet...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2019.01.005
更新日期：2019-04-01 00:00:00
abstract：:Endothelial cell dysfunction may play an important role in the development of various vascular diseases, including atherosclerosis. Here we investigated whether lithium chloride (LiCl), an inhibitor of glycogen synthase kinase-3β (GSK-3β), could counteract atherosclerosis induced by a high-fat diet in ApoE⁻/⁻ mice. Te...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2010.09.004
更新日期：2010-11-01 00:00:00
abstract：:Ion channels control electrical excitability in living cells. In mammalian heart, the opposing actions of Na(+) and Ca(2+) ion influx, and K(+) ion efflux, through cardiac ion channels determine the morphology and duration of action potentials in cardiac myocytes, thus controlling the heartbeat. The last decade has se...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2005.07.013
更新日期：2006-02-01 00:00:00
abstract：:Propionyl-l-carnitine (PLC) is a natural short-chain derivative of l-carnitine (LC), a natural amino acid that plays an important role in fatty acid metabolism. Recent studies suggest that PLC has vascular protective effects. Because of the importance of endothelial nitric oxide synthase (eNOS) and its product, antiat...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2013.07.001
更新日期：2013-09-01 00:00:00
abstract：:AMP-activated protein kinase (AMPK) is present in the arterial wall and is activated in response to cellular stressors that raise AMP relative to ADP/ATP. Activation of AMPK in vivo lowers blood pressure but the influence of hyperlipidemia on this response has not been studied. ApoE(-/-) mice on high fat diet for 6wee...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2015.07.010
更新日期：2015-11-01 00:00:00
abstract：:Chemerin is an adipokine associated with increased blood pressure, and may link obesity with hypertension. We tested the hypothesis that chemerin-induced contraction of the vasculature occurs via calcium flux in smooth muscle cells. Isometric contraction of rat aortic rings was performed in parallel with calcium kinet...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2016.11.009
更新日期：2017-01-01 00:00:00
abstract：:Small GTPase Rap1 has been extensively studied in vitro and shown to regulate multiple basic cellular processes. Until recently, the best studied aspect of Rap1 function in endothelial cells involved its role in regulation of cell-cell junction formation and remodeling. These in vitro studies have increased understand...
journal_title：Vascular pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.vph.2010.03.003
更新日期：2010-07-01 00:00:00
abstract：:To investigate mechanisms of protective effects of fenofibrate on the diabetic kidney, male Wistar rats were divided into control, untreated diabetes, and fenofibrate-treated (32 mg kg(-1) d(-1), 8 weeks) diabetes groups. Diabetes induced by streptozotocin (25 mg/kg) and a high-fat diet was characterized by the disord...
journal_title：Vascular pharmacology
pub_type： 杂志文章
doi：10.1016/j.vph.2006.01.004
更新日期：2006-05-01 00:00:00
