Abstract：
:As a function of the structural modification of the steroid nucleus, the inhibitory interaction of 11 progesterone derivatives with human Na/K-ATPase (Na+/K(+)-transporting ATPase, EC 3.6.1.37), through C3-O-rhamnosylation, is either much decreased or weakly up to strongly increased, so that the rhamnosyl residue contributes to the complementary Gibbs energy of interaction, at the most, the same Gibbs energy increment as realized in ouabain. After C3 beta-O-rhamnosylation, the activity of some progesterone derivatives considerably surpasses that of 3 beta-O-rhamnosyl-chlormadinolacetate, which has been known to elicit positive inotropy in cats. The progesterone derivatives (aglycons and glycosides), that have been analysed more closely, produce their effects by the same molecular mechanism of interaction with Na/K-ATPase as characteristic for digitalis aglycons and glycosides. The results promise to pave the way for the identification of the chemical nature of endogenous digitalis and for the design of novel inotropic drugs.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Weiland J,Schönfeld W,Menke KH,Repke KRdoi
10.1016/s1043-6618(05)80102-1subject
Has Abstractpub_date
1991-01-01 00:00:00pages
27-32issue
1eissn
1043-6618issn
1096-1186pii
S1043-6618(05)80102-1journal_volume
23pub_type
杂志文章abstract：:Long non-coding RNA (lncRNA) is a class of non-coding RNA with ≥200 nucleotides in length which are involved as critical regulators in various cellular processes. LncRNAs contribute to the development and progression of many human diseases. Autophagy is a key catabolic process which helps to maintain the cellular home...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.02.010
更新日期：2019-04-01 00:00:00
abstract：:Diabetic nephropathy (DN) is a common and serious complication of diabetes and causes kidney failure. Ginsenoside Rg5 (Rg5) is an important monomer in the main protopanaxadiol component of black ginseng. Rg5 has exhibited some beneficial biological effects, such as anti-cancer, neuroprotection, and anti-depression, bu...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.104746
更新日期：2020-05-01 00:00:00
abstract：:In previous studies we observed an enhanced anti-inflammatory activity of MPEG-SOD derivatives in acute inflammation in rat. To assess the activity in chronic inflammation we tested the compound with longer half-life (MPEG-SOD 18) in complete adjuvant arthritis in rat. According to the prophylactic schedule of treatme...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(05)80106-9
更新日期：1991-01-01 00:00:00
abstract：:Parkinson's disease is a progressive age-related neurodegenerative disease with invariant loss of substantia nigra dopamine neurons and striatal projections. This disorder is well known for the associated motoric symptoms including resting tremor and the inability to initiate movement. However, it is now apparent that...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2008.09.006
更新日期：2008-11-01 00:00:00
abstract：:Vascular responses to hypoxia are heterogeneous and involve the release of vasodilators substances such as nitric oxide (NO) and prostacyclin (PGI(2)). In vitro studies have shown that Vitamin K(1) modulates the release of arachidonic acid (AA) in vascular cells, and thus inhibits the capacity of blood vessels to synt...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s104366180200227x
更新日期：2002-12-01 00:00:00
abstract：:Biosimilars started receiving the marketing authorization by European Medicine Agency since 2006. The development of biosimilars follows a well-defined step-wise approach, the so-called comparability exercise, which aims to compare non-clinical (mainly quality features and biological activity) and clinical (efficacy a...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.11.002
更新日期：2017-12-01 00:00:00
abstract：:Osteoporosis caused by aging and menopause had become an emerging threat to human health. The reduction of osteoblast differentiation has been considered to be an essential cause of osteoporosis. Osteoblast differentiation could be regulated by LncRNAs, and increasing evidences have proved that LncRNAs may be adopted ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105230
更新日期：2021-01-01 00:00:00
abstract：:The role of autophagy, a process in which the cell self-digests its own components, was investigated in glioma cell death induced by the hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase-inhibiting drug simvastatin. Induction of autophagy and activation of autophagy-regulating signalling pathways were analyzed by i...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2011.08.003
更新日期：2012-01-01 00:00:00
abstract：:Expression of abnormally long polyglutamine (polyQ) tracks is the source of a range of dominant neurodegenerative diseases, such as Huntington disease. Currently, there is no treatment for this devastating disease, although some chemicals, e.g., metformin, have been proposed as therapeutic solutions. In this work, we ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105105
更新日期：2020-11-01 00:00:00
abstract：:The survey was carried out, between September 1995 and May 1996, in order to describe the prescriptive behaviour among Sicilian general practitioners (GPs) in choosing an empirical antibiotic regimen for LRTIs in adult patients and begin an educational process which involves the same GPs in decisions regarding their p...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1998.0484
更新日期：1999-07-01 00:00:00
abstract：:Inflammation plays a key role in tumor promotion and development. Indeed, cyclooxygenase-2 (COX-2) expression is strongly associated with different types of cancer. An emerging class of compounds with significant anti-inflammatory properties is the hydrogen sulfide-releasing non-steroidal anti-inflammatory drugs (H2S-...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.10.019
更新日期：2016-12-01 00:00:00
abstract：:This article summarizes the discovery and the development of endothelial biology with a special focus on the role of endothelium-dependent vasoconstriction. The physician-scientist Paul Michel Vanhoutte contributed many of the initial observations that helped to understand and form the main concepts of modern vascular...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2011.02.013
更新日期：2011-06-01 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：:The renal and metabolic effects of chronic carnitine administration were evaluated in the early stages of experimentally-induced renal failure. Laevo-carnitine (n = 5), Propionyl-carnitine (n = 5) both at 200 mg kg-1 of body weight, or vehicle (physiological saline solution, 0.4 ml kg-1 body weight, n = 5) were admini...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0083
更新日期：1996-09-01 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：:Atropine (5 mg/kg, s.c., twice daily) had no significant effect on 24-h water consumption on day 1 of treatment; on subsequent days the rats showed a significant increase. Procyclidine (5 mg/kg, s.c., twice daily) had a similar effect, except that the increase in daily water consumption began on the third day of treat...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(90)90745-y
更新日期：1990-01-01 00:00:00
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)...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2006.10.003
更新日期：2007-01-01 00:00:00
abstract：:Mild cognitive impairment (MCI), regarded as the prodromal stage before the clinical phase of Alzheimer's disease (AD), has been considered for early intervention. Unfortunately, many trials in this stage with drugs with single-target turned out to be little or no effect. Multi-targeting in nature based on the theory ...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1016/j.phrs.2019.104319
更新日期：2019-08-01 00:00:00
abstract：:Pepducins are cell-penetrating, membrane-tethered lipopeptides designed to target the intracellular region of a G protein-coupled receptor (GPCR) in order to allosterically modulate the receptor's signaling output. In this proof-of-concept study, we explored the pain-relief potential of a pepducin series derived from ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.104750
更新日期：2020-05-01 00:00:00
abstract：:Excess fructose consumption causes high prevalence of metabolic syndrome and inflammatory liver diseases. The aim of the current study was to investigate the therapeutic effects and underlying molecular mechanisms of curcumin and allopurinol in high fructose-induced hepatic inflammation. Male Sprague-Dawley rats were ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.09.021
更新日期：2018-11-01 00:00:00
abstract：:Disruption of the circadian clock is associated with a variety of human pathologies, including cancer. Rather than being a mere consequence of a global changes associated with the cancer cell transcriptome, the aberrant clock gene expression observed in many tumors may serve for cancer cell survival. This scenario sug...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2015.08.008
更新日期：2015-10-01 00:00:00
abstract：:This study investigated the impact of benzodiazepine receptor agonist, midazolam and antagonist, flumazenil, on the rat frontal cortex slices oxygen consumption (QO(2)), in presence and absence of gamma-aminobutyric acid (GABA). QO(2) was polarographically determined, using the biological oxygen monitor. As it was pre...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(02)00289-x
更新日期：2003-02-01 00:00:00
abstract：:Though the AMPA receptor has been implicated in several neurodegenerative processes (epilepsy, ischemia, spasticity), its role in cognition is yet to be clarified. The aim of this study was to assess in the rat the effects of the AMPA receptor antagonist NBQX (3.5, 7, 10, 20 and 30 mgkg(-1), i.p.) on learning and memo...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0898
更新日期：2002-01-01 00:00:00
abstract：:In the last decade, the prevalence of autism spectrum disorders (ASD) has dramatically escalated worldwide. Currently available drugs mainly target some co-occurring symptoms of ASD, but are not effective on the core symptoms, namely impairments in communication and social interaction, and the presence of restricted a...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104579
更新日期：2020-02-01 00:00:00
abstract：:Treatment of MC3T3E-1 osteoblast cultures with combined interferon- gamma(IFN- gamma), lipopolysaccharide (LPS) and tumor necrosis factor- alpha(TNF- alpha) induces expressions of inducible nitric oxide synthase (iNOS) and interleukin-6 (IL-6), resulting in sustained releases of large amounts of nitric oxide and IL-6....
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2000.0778
更新日期：2001-03-01 00:00:00
abstract：:Extensive studies have reported the significant roles of numerous cellular features and processes in properly maintaining neuronal morphology and function throughout the lifespan of an animal. Any alterations in their homeostasis appear to be strongly associated with neuronal aging and the pathogenesis of various neur...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.003
更新日期：2017-05-01 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：:The antioxidant properties of a novel water-soluble antioxidant of the benzofuran family (5-hydroxy-4,6,7-trimethyl-2,3-dihydrobenzofuran-2-acetic acid, BFA) were studied. In rat liver mitochondria BFA increases the lag-time and decreases the extent of lipid peroxidation induced by ascorbate/Fe2+; an IC50 value of abo...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(91)90041-u
更新日期：1991-12-01 00:00:00
abstract：:Several studies have demonstrated that any beneficial effects of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (statins), of which simvastatin (Merck Sharp & Dohme) is an example, on coronary events are linked to their hypocholesterolemic properties. The in vivo effects of simvastatin treatment ...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1006/phrs.2000.0787
更新日期：2001-04-01 00:00:00
abstract：:Kindling represents an accepted model of human epileptogenesis. Furthermore, it has been demonstrated that kindled rats show a diminished learning performance in an active avoidance task. In our study we administered different nootropic drugs to kindled rats to test their effects on learning a two-way active avoidance...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(05)80003-9
更新日期：1995-09-01 00:00:00
