Abstract：
:Respiratory fluoroquinolones are currently considered by several guidelines among the most effective antimicrobial agents for the treatment of acute bacterial rhinosinusitis. The aim of this study was to assess levofloxacin penetration into paranasal sinuses mucosa of 15 patients with chronic rhinosinusitis 1h (n = 4), 2 h (n = 5) and 3 h (n = 6) after a single 500 mg oral dose. Levofloxacin concentrations in plasma and tissue samples were assessed by means of HPLC. Median of mucosal concentrations were 0.96 mg l(-1) at 1 h, 2.50 mg l(-1) at 2 h, 5.84 mg l(-1) at 3 h. Average paranasal sinuses mucosa-to-plasma ratios raised from 1.46 at 1 h, to 1.81 at 2 h and to 2.56 at 3 h. These data are consistent with 500 mg oral levofloxacin ensuring appropriate therapeutic exposure in sinonasal tissue of patients with chronic rhinosinusitis, the concentrations between 1 and 3 h post-dosing being almost always higher than the MIC90 against the major bacterial pathogens responsible for upper respiratory tract infections.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Pea F,Marioni G,Pavan F,Staffieri C,Bottin R,Staffieri A,Furlanut Mdoi
10.1016/j.phrs.2006.10.003subject
Has Abstractpub_date
2007-01-01 00:00:00pages
38-41issue
1eissn
1043-6618issn
1096-1186pii
S1043-6618(06)00185-Xjournal_volume
55pub_type
杂志文章abstract：:Central nervous system (CNS) drug development faces significant difficulties that translate into high rates of failure and lack of innovation. The pathophysiology of neurological and psychiatric disorders often results in the breakdown of blood-CNS barriers, disturbing the CNS microenvironment and worsening disease pr...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105226
更新日期：2020-12-01 00:00:00
abstract：:Breast cancer, the most prevalent cancer in women, remains the second in the list of cancer mortality, the majority of these fatalities resulted from estrogen receptor alpha (ERα) positive disease. ERα is well known for its function on breast cancer initiation and development and has become the most successful biomark...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104294
更新日期：2019-08-01 00:00:00
abstract：:Alzheimer's disease (AD) is regarded as a progressive and devastating neurodegenerative disorder. In aged individuals, it is the most prevalent cause of dementia and is characterized by gradual loss of cognitive functions. In the last decade, numerous research works were undertaken to investigate the pathogenesis of A...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.11.028
更新日期：2018-03-01 00:00:00
abstract：:Exposure to ionizing radiation causes damage to living tissues; however, only a small number of agents have been approved for use in radiation injuries. Radioprotector is the primary countermeasure to radiation injury and none radioprotector has indeed reached the drug development stage. Repurposing the long list of a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.09.024
更新日期：2016-11-01 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：:The antinociceptive effect of the D(2) antagonist prochlorperazine was examined in the mouse hot-plate and abdominal constriction tests. Prochlorperazine (1-2 mg kg(-1) s.c./i.p.) produced an increase of the pain threshold in the mouse hot-plate test. The antinociception produced by prochlorperazine was prevented by t...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2004.02.005
更新日期：2004-09-01 00:00:00
abstract：:New quick-acting blood schizontocides are needed to contain the spread of multiple drug resistant strains of P. falciparum and for the treatment of the cerebral malaria cases. A multiple drug resistant strain of P. yoelii nigeriensis resistant to mefloquine (128 mg/kg x 6 days), quinine (300 mg/kg x 7 days) and chloro...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(89)90159-x
更新日期：1989-07-01 00:00:00
abstract：:We have recently synthesized a new series of 4,5-dihydrobenzo-oxa-cycloheptapyrazole derivatives with the aim to discover novel CB1 antagonist agents characterized by anti-obesity activity comparable to that of SR141716A but with reduced adverse effects such as anxiety and depression. Within the novel class, the CB1 a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2013.06.001
更新日期：2013-08-01 00:00:00
abstract：:Hepatocellular carcinoma (HCC) and intrahepatic cholangiocarcinoma (ICC) are the most prevalent types of primary liver cancer. Compared with HCC, for which several drugs have been approved, ICC is associated with shorter survival, and no drug has been approved for this type. Previously, we reported that Bmi1 drives HC...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105365
更新日期：2020-12-08 00:00:00
abstract：:This study was performed in order to investigate the cholinomimetic response of seminal vesicles isolated from rats treated with hydrocortisone acetate during perinatal life. At the adult phase, the body weight and the wet weight of the seminal vesicle of these animals were unchanged. However, these male rats exhibite...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：
更新日期：2003-07-01 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：INTRODUCTION:Erectile dysfunction (ED) is frequently encountered in patients with arterial hypertension and there is a recent functional correlation between the expression of thermoreceptor channels TRPM8 (melastatin 8) and alterations in blood pressure in hypertension. The aim of this study was to investigate the func...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104329
更新日期：2019-09-01 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：:The cytokine thymic stromal lymphopoietin (TSLP) is involved in the development and the progression of allergic diseases. It is mainly released by epithelial cells at barriers such as skin and gut in response to danger signals. Overexpression of TSLP in keratinocytes (KC) can provoke the development of a type 2 inflam...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.08.001
更新日期：2016-11-01 00:00:00
abstract：:Curcumin, a bioactive polyphenol, is a yellow pigment of the Curcuma longa (turmeric) plant. Curcumin has many pharmacologic effects including antioxidant, anti-carcinogenic, anti-obesity, anti-angiogenic and anti-inflammatory properties. Recently, it has been found that curcumin affects lipid metabolism, and subseque...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.008
更新日期：2017-05-01 00:00:00
abstract：:The review emphasizes the role of NGF, the most representative member of the neurotrophins family, in cardiac physiopathology with a particular focus on healing and sprouting processes occurring after tissue damage. Cardiac and circulating NGF levels dramatically increase following myocardial injury (MI). A very early...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2010.12.017
更新日期：2011-04-01 00:00:00
abstract：:DB-67 and its lactone homolog DB-91 are derivatives of topoisomerase I inhibitor camptothecin (CPT) with silyl moiety, which may exhibit a slower inactivation process by changed kinetics of protein binding and/or hydrolysis of its lactone ring and result in increased antitumor activity and decreased toxicity. Pharmaco...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2009.07.005
更新日期：2010-02-01 00:00:00
abstract：:The first studies of histamine and diabetes date back to the 1950s. Since that time the involvement of histamine in diabetes was related to its well known vasoactive properties and permeability leakage effects. In particular, the first evidence for a correlation between histamine and diabetes arose in 1989 when an inc...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.06.021
更新日期：2016-09-01 00:00:00
abstract：:Indole-based compounds, such as the alkyl-indole (AI) compound WIN55212-2, activate the cannabinoid receptors, CB1 and CB2, two well-characterized G protein-coupled receptors (GPCR). Reports indicate that several indole-based cannabinoid agonists, including WIN55212-2, lack selectivity and interact with at least two a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.10.025
更新日期：2017-01-01 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 metabolism of arachidonic acid by cytochrome P450 (CYP) epoxygenases generates epoxyeicosatrienoic acids (EETs) which affect numerous cellular process including Ca(2+) signaling and the activity of Ca(2+)-dependent K(+) channels. The expression of the CYP epoxygenase(s) that generate EETs in endothelial cells is n...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2003.11.016
更新日期：2004-06-01 00:00:00
abstract：:The Renin Angiotensin System (RAS) is a pivotal physiological regulator of heart and kidney homeostasis, but also plays an important role in the pathophysiology of heart and kidney diseases. Recently, new components of the RAS have been discovered, including angiotensin converting enzyme 2 (ACE2), Angiotensin(Ang)-(1-...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.03.018
更新日期：2016-05-01 00:00:00
abstract：:Diabetes mellitus is an important risk factor for the development of cardiovascular disease. The impact of diabetes on the heart in part resides in the changes in metabolic fuel availability evoked by lack of insulin or resistance to its action. This review addresses how the metabolic abnormalities associated with poo...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2009.04.006
更新日期：2009-09-01 00:00:00
abstract：:Etifoxine (EFX) is a non-benzodiazepine psychoactive drug which exhibits anxiolytic effects through a dual mechanism, by directly binding to GABAA receptors (GABAARs) and to the mitochondrial 18-kDa translocator protein, resulting in the potentiation of the GABAergic function. The β subunit subtype plays a key role in...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.04.034
更新日期：2019-07-01 00:00:00
abstract：:It has been reported that patients with Hodgkin's disease (HD) show altered porphyrin metabolism, and suggested that the cause is the neoplastic process itself. If this is true, disease progression should be associated with higher levels of porphyrin excretion. The aim of this study was to evaluate urinary coproporphy...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2004.09.005
更新日期：2005-03-01 00:00:00
abstract：:The altered vascular responses to various vasopressors and relaxants have been well reported in various animal models of hypertension, insulin resistance and diabetes. Though the role of oxidative stress (increased superoxide levels) associated with these altered vascular responses in hyperglycemic/diabetic state is w...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2005.11.002
更新日期：2006-03-01 00:00:00
abstract：:TMEM16A plays critical roles in physiological process and may serve as drug targets for diverse diseases. Recently, TMEM16A has started to be regarded as potential primary lung adenocarcinoma targets. Here, we identified that arctigenin, a natural compound, is a novel TMEM16A inhibitor, and it can suppress lung adenoc...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.104721
更新日期：2020-05-01 00:00:00
abstract：:Since the regenerative capacity of the adult mammalian heart is limited, cardiac injury leads to the formation of scar tissue and thereby increases the risk of developing compensatory heart failure. Stem cell therapy is a promising therapeutic approach but is facing problems with engraftment and clinical feasibility. ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.07.020
更新日期：2018-01-01 00:00:00
abstract：:The objective of the study was to investigate possible changes in vancomycin serum levels induced by cardio-pulmonary bypass (CPB). Ten cardiac patients (seven males, three females, aged between 56 and 81), who underwent cardiac surgery requiring CPB, took part in the study. Vancomycin (15 mg kg-1) was intravenously i...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1006/phrs.1998.0370
更新日期：1998-10-01 00:00:00
abstract：:Advanced glycation end-products (AGE) and the receptor for AGE (RAGE) have been linked to numerous diabetic vascular complications. RAGE activation promotes a self-sustaining state of chronic inflammation and has been shown to induce apoptosis in various cell types. Although previous studies in vascular smooth muscle ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2015.12.015
更新日期：2016-02-01 00:00:00
