1,720,976 research outputs found
CCB: A novel anologue of MPCB with high binding affinity and specific kappa opioid receptor agonist
No full textnot availabl
Anti-amnesic and neuroprotective actions of the sigma-1 receptor agonist (-)-MR22 in rats with selective cholinergic lesion and amyloid infusion
No full textanti-amnesic properties of (±)-PPCC, a novel sigma receptor ligand, on cognitive dysfunction induced by selective cholinergic lesion in rats
No full textSynthesis of (+)-(1'R,2'S) and (1'S,2'R)-6,11-Dimethyl-1,2,3,4,5,6- hexahydro-3-[[2'-(alkoxycarbonyl)-2'-phenylcyclopropyl]methyl]-2,6-methano- 3-benzazocin-8-ol. Comparison of the affinities for σ1 and opioid receptors with in the diastereoisomeric MPCB and CCB
No full textThe synthesis and the in vitro receptor affinity for σ and opiod receptors of the two diastereoisomers, of (+)-cis-MPCB namely, (+)-cis- (1'S,2'R)-6,11-Dimethyl-1,2,3,4,5,6-hexahydro-3-[[2'-(methoxycarbonyl)-2'- phenylcyclopropyl]methyl]-2,6-methano-3-benzazocin-8-ol, (1'S,2'R)6a and (+)- cis,(1'R,2'S)-6,11-Dimethyl-1,2,3,5,6-hexahydro-3-[[2'-(methoxycabonyl)-2'- phenylcyclopropyl]methyl]-2,6-methano-3-benzazocin-8-ol, (1'R,2'S)6a are reported. Affinities of (1'S,2'R)6a and (1'R,2'S)6a were compared with those of the (-)-cis-diastereoisomers of MPCB(1), and of its p-Cl phenyl derivative CCB(2). The (+)-cis-N-normetazocine derivatives showed higher affinity for the σ1 sites, labeled with [3H]-(+)-pentazocine than the corresponding (- )-cis- analogs. In particular, compound (1'S,2'R)6a showed a Ki = 66.7 nM for σ1 receptor, associated with a good selectivity for σ1 with respect to κ, μ, δ opioid receptors subtypes (Ki = > 1,000 nM). Analysis of the data seem to support the hypothesis that the (+)-cis-N-normetazocine nucleus posses a specific enantioselectivity for σ1 sites, when supporting bulkier N-substituents functionalized with a carboxy ester group
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe 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
Full text link“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
Synthesis and structure-activity relationships of 1-aralkyl-4- benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent σ ligands
No full textIn the attempt to define more accurately structure-affinity relationships for ó1 and ó2 ligands,we synthesized and tested on ó subtype receptors a series of aralkyl derivatives of 4-benzylpiperidine,in which the effect of modifications on the aralkyl moiety was studied in a systematicway. The affinity of the compounds here described varied to a great extent, with a ó2/ó1selectivity ranging from 0.1 to 9. Thus, to confirm the ability of the piperazine derivative tobind to ó1 receptors in a different way than piperidines, we synthesized and tested a series ofpiperazine compounds; the comparison of their affinity with that of the correspondingpiperidines strongly supports the possibility of a different binding mode. While the compoundshere described are on the whole selective for ó vs serotonin 5-HT1A and dopamine D2 receptors,9aa, 9ba and 9ab possess a remarkable affinity for both ó and 5-HT1A receptors, with Ki inthe nanomolar range, and are selective with respect to D2 receptors. They displayed also apartial agonist profile in a human 5-HT1A [35S]GTPçS binding assay, suggesting their potentialuse as atypical antipsychotic agents
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe 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
Design and synthesis of new bifunctional sigma-1 selective ligands with antioxidant activity
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