Search results for "ISM [Radio continuum]"
showing 10 items of 703 documents
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation
2003
In HEK293 cells stably expressing alpha4beta2 nAChRs, naltrexone, but not naloxone, blocked alpha4beta2 nAChRs via an open-channel blocking mechanism. In primary hippocampal cultures, naltrexone inhibited alpha7 nAChRs up-regulated by nicotine, and in organotypic hippocampal cultures naltrexone caused a time-dependent up-regulation of functional alpha7 nAChRs that was detected after removal of the drug. These results indicate that naltrexone could be used as a smoking cessation aid.
Phosphorylation and activation of endothelial nitric oxide synthase by red fruit (Pandanus conoideus Lam) oil and its fractions
2020
Abstract: Ethnopharmacological relevance Red fruit (Pandanus conoideus Lam) oil (RFO) is utilized by inhabitants of the Papua Island to treat diseases such as infections, cancer, and cardiovascular disease, but the mechanism of action is unknown. Aim of the study We have recently shown that RFO stimulates nitric oxide (NO) production in endothelial cells. The present study was conducted to investigate the molecular mechanism of endothelial NO synthase (eNOS) activation by RFO. Materials and methods NO production by endothelial cells was determined with electron paramagnetic resonance. The vascular function of isolated mouse aorta was examined using a wire myograph system. Phosphorylation of…
Pyrrolo[2,1-d][1,2,3,5]tetrazine-4(3H)-ones, a new class of azolotetrazines with potent antitumor activity.
2003
Pyrrolo[2,1-d][1,2,3,5]tetrazinones 10a-o, compounds that hold the deaza skeleton of the antitumor drug temozolomide, were prepared by reaction of 2-diazopyrroles 9 and isocyanates. Such a synthetic route represents, among those leading to azolotetrazinones reported so far, the only possible one since attempts to cyclize to the title ring system 2-amino-1-carbamoylpyrroles 11 or the mono substituted 2-triazenopyrrole 12 failed. Compounds 10 were screened at the National Cancer Institute (NCI) for their activity against a panel of about 60 human tumor cell lines. Most of them possess remarkable antineoplastic activity having GI(50) values in the low micromolar or sub-micromolar range and rea…
Olympic Games and Their Impacts
2017
The modern Olympic Games is considered by many to be the world’s greatest sport festival. Economic, Sociocultural and Environmental impacts are described along with policy implications, from both an historical and current perspective.
Single nucleotide polymorphism array karyotyping: A diagnostic and prognostic tool in myelodysplastic syndromes with unsuccessful conventional cytoge…
2013
Cytogenetic aberrations identified by metaphase cytogenetics (MC) have diagnostic, prognostic, and therapeutic implications in myelodysplastic syndromes (MDS). However, in some MDS patients MC study is unsuccesful. Single nucleotide polymorphism array (SNP-A) based karyotyping could be helpful in these cases. We performed SNP-A in 62 samples from bone marrow or peripheral blood of primary MDS with an unsuccessful MC study. SNP-A analysis enabled the detection of aberrations in 31 (50%) patients. We used the copy number alteration information to apply the International Prognostic Scoring System (IPSS) and we observed differences in survival between the low/intermediate-1 and intermediate-2/h…
Response to lenalidomide in myelodysplastic syndromes with del(5q): influence of cytogenetics and mutations.
2012
Summary Lenalidomide is an effective drug in low-risk myelodysplastic syndromes (MDS) with isolated del(5q), although not all patients respond. Studies have suggested a role for TP53 mutations and karyotype complexity in disease progression and outcome. In order to assess the impact of complex karyotypes on treatment response and disease progression in 52 lenalidomide-treated patients with del(5q) MDS, conventional G-banding cytogenetics (CC), single nucleotide polymorphism array (SNP-A), and genomic sequencing methods were used. SNP-A analysis (with control sample, lymphocytes CD3+, in 30 cases) revealed 5q losses in all cases. Other recurrent abnormalities were infrequent and were not ass…
Online Hate Speech in the European Union : A Discourse-Analytic Perspective
2017
This book is open access under a CC BY 4.0 license and reports on research carried out as part of the European Union co-funded C.O.N.T.A.C.T. project which targeted hate speech and hate crime across a number of EU member states. It showcases the bearing that discourse analytic research can have on our understanding of this phenomenon that is a growing global cause for concern. Although ‘hate speech’ is often incorporated in legal and policy documents, there is no universally accepted definition, which in itself warrants research into how hatred is both expressed and perceived. The research project synthesises discourse analytic and corpus linguistics techniques, and presents its key finding…
Effects of the intensity of use of social media on brand equity: An empirical study in a tourist destination
2018
PurposeThe purpose of this paper is to provide a comprehensive research of the effects of the intensity of use of social media on destination brand equity. The authors use the schema theory and a multidimensional approach of brand equity to analyse how social media communication affects brand awareness, brand image, customer value, brand quality and loyalty.Design/methodology/approachThe authors carried out a quantitative study through a personal survey with structured questionnaire. The study population were international tourists, over 18 years of age, who were visiting the city of Valencia, Spain. Respondents were asked to take the questionnaire upon arrival in Valencia, that is, before …
Kavapyrone enriched extract fromPiper methysticum as modulator of the GABA binding site in different regions of rat brain
1994
Regional differences in the modulation of [3H] muscimol binding to GABAA receptor complexes by kavapyrones, compounds of the rhizome of the plant Piper methysticum which possess sedative activity, were demonstrated using membrane fractions obtained from target brain centers of kavapyrone action: hippocampus (HIP), amygdala (AMY) and medulla oblongata (MED), and from brain centers outside the main kavapyrone effects as frontal cortex (FC) and cerebellum (CER). The kava extract enhanced the binding of [3H] muscimol in a concentration-dependent manner with maximal potentiation of 358% over control in HIP followed by AMY and MED (main target brain centers). Minimal stimulation was observed in C…
SYNTHESIS OF PYRROLO[3,2-H]QUINOLINONES WITH GOOD PHOTOCHEMOTHERAPEUTIC ACTIVITY AND NO DNA DAMAGE
2010
In the search for new photochemotherapeutic agents, a series of derivatives of the ring system pyrrolo[3,2-h]quinoline--bioisosters of the angular furocoumarin angelicin--were synthesized through a four-step synthetic approach, in reasonable overall yields. Eight of the synthesized derivatives showed a remarkable phototoxicity against a panel of four human tumor cell lines and a great dose UV-A dependence, reaching IC₅₀ values at submicromolar level. The mode of cellular death photoinduced by pyrrolo[3,2-h]quinolines was evaluated through a series of flow cytometric analysis and other tests were performed to clarify their mechanism of action.