1,720,974 research outputs found
New 2- pyridylethylamines with dopaminergic activity: synthesis and radioligand binding evaluation
Going Beyond Counting First Authors in Author Co-citation Analysis
The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
We provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
Benzimidazole, benzoxazole and benzothiazole derivatives as 5HT(2B) receptor ligands. Synthesis and preliminary pharmacological evaluation
2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2-phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2C subtypes. All compounds were characterized by binding affinity determination for 5-HT2A and 5-HT2C subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2C subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations
4-(4-Fluorobenzoyl)-1-[2-(4-iodo-2,5-dimethoxyphenyl)ethyl]piperidine and its derivatives: synthesis and affinity at 5-HT2A, 5-HT2B and 5-HT2c serotonin receptors
A COMPARATIVE BEHAVIOURAL ANALYSIS IN RATS OF THE D2 AGONIST RU 24213 AND TWO NEW STRUCTURALLY SIMILAR COMPOUNDS
The present study reports a comparative analysis of the behavioural effects induced in rats by three structurally similar compounds. One of them is the D2 dopamine agonist RU 24213, the others are newly-synthesized drugs whose selective affinity for D2 receptors has been established in priliminary binding studies. Discussion centers on the possible relationship between their chemical structure and behavioural activity
Synthesis and Evaluation of N-n-Propyl-N-(2-phenylethyl)-2-(3-fluoro-4- hydroxyphenyl)ethylamine Derivatives as Dopamine Receptor Ligands
Polyhydroxylic Prodrugs of Lonidamine
Lonidamine (LND) 1, a drug currently used in the treatment of several neoplasia (i.e. lung, breast, prostate and brain). Its mechanism of action does not affect the protein or nucleic acids synthesis but LND acts reducing the oxygen consumption, and reducing glucose utilization of neoplastic cells by inhibition of mitochondria-bound glycolitic enzyme hexokinase that is usually absent in normal cells. Thus mitochondria represents the intracellular target of LND.
Due to its original mechanism of action, LND is devoid of the usual side effects induced by antiproliferative agents and no serious adverse reactions have been reported even over a long-term treatment period. This gives to LND an added value as anticancer drug candidate.(1) However, pancreatic and hepatic toxicity were observed in dogs receiving LND by intravenous injection whereas oral administration of LND was devoid of such a toxicity in the same studies suggesting that the bioavailability of LND may be limited by its extremely low water solubility (17 mg/L).(2) The present study concerns potential LND prodrugs bearing high hydrophilic molecules such as sugars and polyalcohols conjugated to the carboxyl group of the molecule as an attempt to increase the water solubility of LND itself
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