Abstract:
:Nebivolol is a new selective beta 1-adrenergic blocking agent, that possesses a peculiar pharmacodynamic profile and an original chemical structure, by which it differs from traditional beta 1-blockers. Nebivolol is a racemic mixture of two enantiomers in equal ratios. It is endowed with a highly selective beta 1-blocking activity, and does not show an intrinsic sympathomimetic activity. Nebivolol is endowed with peripheral vasodilating properties mediated by the modulation of the endogenous production of nitric oxide. It does not significantly decrease airway conductance compared with atenolol and propranolol. Nebivolol does not compromise the left ventricular function, but it may increase stroke volume, and does not reduce heart inotropism during exertion. Nebivolol is quite safe and is well tolerated, also when compared to traditional beta-blockers. The most common adverse effects are dizziness, headache and fatigue. Owing to its combined dual mechanism of action, nebivolol leads to a unique haemodynamic and therapeutic profile by which it may be advantageous in essential hypertension, ischaemic heart disease and congestive heart failure.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Mangrella M,Rossi F,Fici F,Rossi Fdoi
10.1006/phrs.1998.0387subject
Has Abstractpub_date
1998-12-01 00:00:00pages
419-31issue
6eissn
1043-6618issn
1096-1186pii
S1043-6618(98)90387-5journal_volume
38pub_type
杂志文章,评审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 available studies have reported the benefits of statins on all-cause and cardiovascular mortality in chronic kidney disease (CKD) patients. However studies in end-stage renal disease patients on dialysis yielded conflicting results. Therefore, we performed a meta-analysis and provide the most reliable trial data t...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析
doi:10.1016/j.phrs.2013.03.007
更新日期:2013-06-01 00:00:00
abstract::The suppression of the abnormal systemic immune response constitutes a primary strategy for treatment of rheumatoid arthritis (RA); toward this end, the identification of natural compounds with immunosuppressive activity represents a promising strategy for RA drug discovery. Cinnamtannin D1 (CTD-1), a polyphenolic com...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.104513
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:We examined the influence of diabetes mellitus (DM) on the healing of HCl-induced gastric lesions and the healing promoting effect of IGF-1 on these lesions. METHODS:Experiments were performed on rats injected with streptozotocin (STZ, 70 mg kg(-1), i.p.) 5 weeks prior to the experimental session. Diabetic ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0581
更新日期:2000-02-01 00:00:00
abstract::The possible involvement of adenosine 5'-triphosphate (ATP) receptors in the function of the hippocampus is reviewed. The involvement of these receptors in the hippocampus is suggested by data that ATP is released from hippocampal slices [1] and that it also induces fast synaptic currents in cultured hippocampal neuro...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.1998.0382
更新日期:1998-11-01 00:00:00
abstract::Lupeol is a natural triterpenoid that widely exists in edible fruits and vegetables, and medicinal plants. In the last decade, a plethora of studies on the pharmacological activities of lupeol have been conducted and have demonstrated that lupeol possesses an extensive range of pharmacological activities such as antic...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.105373
更新日期:2020-12-11 00:00:00
abstract::There is considerable evidence to support the role of anandamide (AEA), an endogenous ligand of cannabinoid receptors, in neuropathic pain modulation. AEA also produces effects mediated by other biological targets, of which the transient receptor potential vanilloid type 1 (TRPV1) has been the most investigated. Both,...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.06.012
更新日期:2016-09-01 00:00:00
abstract::Tyrosine kinase inhibitors (TKIs) have been widely used for the clinical treatment of patients with non-small cell lung cancer (NSCLC) harboring mutations in the EGFR. Unfortunately, due to the secondary mutation in EGFR, eventual drug-resistance is inevitable. Therefore, to overcome the resistance, new agent is urgen...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.104934
更新日期:2020-09-01 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::We compared the protective abilities of Mangifera indica L. stem bark extract (Vimang) 50-250 mgkg(-1), mangiferin 50 mgkg(-1), vitamin C 100 mgkg(-1), vitamin E 100 mgkg(-1)and beta -carotene 50 mgkg(-1)against the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced oxidative damage in serum, liver, brain as well as i...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0727
更新日期:2000-12-01 00:00:00
abstract::The coronavirus disease 2019 (COVID-19) epidemic has been almost controlled in China under a series of policies, including "early diagnosis and early treatment". This study aimed to explore the association between early treatment with Qingfei Paidu decoction (QFPDD) and favorable clinical outcomes. In this retrospecti...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105290
更新日期:2020-11-01 00:00:00
abstract::Asymmetric (N(G),N(G)) dimethylarginine (ADMA) is present in plasma and cells. It can inhibit nitric oxide synthase (NOS) that generates nitric oxide (NO) and cationic amino acid transporters (CATs) that supply intracellular NOS with its substrate, l-arginine, from the plasma. Therefore, ADMA and its transport mechani...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2009.08.002
更新日期:2009-12-01 00:00:00
abstract::Many data suggest an involvement of toxic oxygen radicals in the termination of endurance to muscle fatigue. Being reduced glutathione (GSH), an efficient intracellular physiological antioxidant, experiments have been performed to discover whether exogenous GSH modifies endurance to exhaustive swimming in mice. GSH wa...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80116-1
更新日期:1991-02-01 00:00:00
abstract::"Funny" (f) channels underlie the cardiac "pacemaker"I(f) current, originally described as an inward current activated on hyperpolarization to the diastolic range of voltages in sino-atrial node myocytes [Brown, HF, DiFrancesco, D, Noble, SJ. How does adrenaline accelerate the heart? Nature 1979;280:235-236]. The invo...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2006.03.006
更新日期:2006-05-01 00:00:00
abstract::Echinomycin, in typical DNA minor groove binder, had comparable efficacy compared to 5-FU in the phase II trail of colon cancer treatment. To improve echinomycin's drawback (hydrophobicity, toxicity), we synthesized the YK-2000 series (echinomycin analogues). Among these, YK-2000 had the best in vitro cytotoxicity on ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.01.005
更新日期:2004-08-01 00:00:00
abstract::Although calcimimetics were developed to block parathyroid hormone synthesis, some reports suggest that they may also reduce blood pressure by unknown mechanisms. Calcimimetic-induced changes in the synthesis of endothelial vasoactive factors could be involved. Wistar rats were treated with the calcimimetic R-568, and...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2013.07.006
更新日期:2013-10-01 00:00:00
abstract::Erectile function is a widely accepted indicator of systemic endothelial activity since from a clinical standpoint erectile dysfunction (ED) often precedes cardiovascular events. Recently it has been described a potential role for β3 adrenoceptor in cardiovascular diseases emphasizing a possible development of new dru...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2017.07.025
更新日期:2017-10-01 00:00:00
abstract::In this study, we have addressed the pharmacogenomic basis of the response of gastrointestinal tumors to six anticancer drugs using a panel of fifteen cell lines derived from pancreatic, stomach and biliary tract cancers. We determined the constitutive expression levels of 96 genes, whose encoded proteins contribute t...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.09.007
更新日期:2016-11-01 00:00:00
abstract::Contrasting results have been reported on the role of rs628031 and rs683369 polymorphisms of SLC22A1 and rs776746 of CYP3A5 on imatinib treatment response in patients with chronic myeloid leukemia (CML). In the present study, we conducted a systematic review and meta-analysis of published studies to estimate the impac...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析
doi:10.1016/j.phrs.2018.02.005
更新日期:2018-05-01 00:00:00
abstract::The anti-inflammatory effect of glucocorticoids depends, at least in part, on the induction of two regulatory proteins, lipocortin and vasocortin, both preventing the release of inflammatory mediators. Lipocortin inhibits phospholipase A2 (PLA2) and therefore reduces arachidonic acid metabolites formation. Vasocortin ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/s1043-6618(05)80058-1
更新日期:1992-01-01 00:00:00
abstract::The smoothened (SMO) receptor, an essential signal transducer in the Hedgehog pathway, was targeted with antagonists to suppress the tumor. It is interesting that SMO D473H mutation confers resistance on inhibitor LDE-225 rather than LEQ-506. In this paper, the binding modes of them against the wild type and mutant SM...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2017.11.025
更新日期:2018-03-01 00:00:00
abstract::Evodiae fructus is a widely used herbal drug in traditional Chinese medicine. Evodia extract was found to inhibit hERG channels. The aim of the current study was to identify hERG inhibitors in Evodia extract and to investigate their potential proarrhythmic effects. Dehydroevodiamine (DHE) and hortiamine were identifie...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.02.024
更新日期:2018-05-01 00:00:00
abstract::The effects of trans-resveratrol (RSV) combined with ethanol (EtOH) were evaluated by (31)P NMR on total ATP and sn-glycerol-3-phosphate (sn-G3P) contents measured in real time in isolated and perfused whole liver of the rat. Mitochondrial ATP turnover was assessed by using specific inhibitors of glycolytic and mitoch...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2011.12.003
更新日期:2012-03-01 00:00:00
abstract::The rationale underlying therapeutic strategies designed to inhibit the action of endogenous sex hormones in malignant breast cells is provided by the demonstration of their involvement in supporting the development and growth of breast carcinoma. The surgical removal of steroid-secreting glands, in order to reduce th...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.1998.0437
更新日期:1999-05-01 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::Corticosteroids are shown to have deleterious effects on wound healing for various tissues. Arginine metabolism and nitric oxide (NO) synthesis play an important role in many aspects of inflammation and wound healing. The study was designed to evaluate the relationship of dexamethasone impaired healing of tracheal ana...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00130-5
更新日期:2002-09-01 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 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 succini...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0038
更新日期:1996-04-01 00:00:00
abstract::Exogenous hydrogen sulfide (H2S) protects against myocardial ischemia/reperfusion injury but the mechanism of action is unclear. The present study investigated the effect of GYY4137, a slow-releasing H2S donor, on myocardial infarction given specifically at reperfusion and the signalling pathway involved. Thiobutabarb...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.06.028
更新日期:2016-09-01 00:00:00
abstract::It has been suggested that hypertension results from a loss of immunological tolerance and the resulting autoimmunity may be an important underlying factor of its pathogenesis. This stems from the observations that many of the features involved in autoimmunity are also implicated in hypertension. Furthermore, the unde...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.09.008
更新日期:2016-11-01 00:00:00