GluN2B‐Selective N‐Methyl‐d‐aspartate (NMDA) Receptor Antagonists Derived from 3‐Benzazepines: Synthesis and Pharmacological Evaluation of Benzo[7]annulen‐7‐amines

Given their high neuroprotective potential, ligands that block GluN2B‐containing N‐methyl‐D ‐aspartate (NMDA) receptors by interacting with the ifenprodil binding site located on the GluN2B subunit are of great interest for the treatment of various neuronal disorders. In this study, a novel class of GluN2B‐selective NMDA receptor antagonists with the benzo[7]annulene scaffold was prepared and pharmacologically evaluated. The key intermediate, N‐(2‐methoxy‐5‐oxo‐6,7,8,9‐tetrahydro‐5H‐benzo[7]annulen‐7‐yl)acetamide ( 11 ), was obtained by cyclization of 3‐acetamido‐5‐(3‐methoxyphenyl)pentanoic acid ( 10 b ). The final reaction steps comprise hydrolysis of the amide, reduction of the ketone, and reductive alkylation, leading to cis‐ and trans‐configured 7‐(ω‐phenylalkylamino)benzo[7]annulen‐5‐ols. High GluN2B affinity was observed with cis‐configured γ‐amino alcohols substituted with a 3‐phenylpropyl moiety at the amino group. Removal of the benzylic hydroxy moiety led to the most potent GluN2B antagonists of this series: 2‐methoxy‐N‐(3‐phenylpropyl)‐6,7,8,9‐tetrahydro‐5H‐benzo[7]annulen‐7‐amine ( 20 a , K_i=10 nM ) and 2‐methoxy‐N‐methyl‐N‐(3‐phenylpropyl)‐6,7,8,9‐tetrahydro‐5H‐benzo[7]annulen‐7‐amine ( 23 a , K_i=7.9 nM ). The selectivity over related receptors (phencyclidine binding site of the NMDA receptor, σ₁ and σ₂ receptors) was recorded. In a functional assay measuring the cytoprotective activity of the benzo[7]annulenamines, all tested compounds showed potent NMDA receptor antagonistic activity. Cytotoxicity induced via GluN2A subunit‐containing NMDA receptors was not inhibited by the new ligands.     

A Theoretical and Experimental Study on Solubility of Curatives in Rubbers

The current study provides indications for improving the properties of dissimilar rubber blends. As solubility is a key factor for the distribution and a driving force for the migration of curatives in dissimilar rubber blends, it is of importance to have precise data of their solubilities. The solubilities of (insoluble) sulfur and the accelerators CBS, MBT and DCBS are measured at RT and at 60 °C, in lightly crosslinked SBR, NBR and EPDM. The experimental results correlate well with calculated solubility parameters, as determined using the method of Hoftijzer and van Krevelen.

     

A Phase Blending Study on Rubber Blends Based on the Solubility Preference of Curatives

Using previously obtained data on the solubilities of curatives in SBR, EPDM and in NBR, different mixing procedures were performed on 50/50 SBR/EPDM and NBR/EPDM blends. In contrast to a previous phase‐mixing study, the curatives were added to separate phases before final blending, in an attempt to control the curative distributions in the blends for optimal mechanical properties. Fillers were not applied in the system to exclude their influence on the dispersion of the curatives. The properties of such blends compounded by selective phase mixing are superior to those of blends compounded with normal mixing procedures.

     

Chemical vapor deposition of highly adherent diamond coatings onto co-cemented tungsten carbides irradiated by high power diode laser

The present investigation deals with the definition of a new eco-friendly alternative to pretreat Co-cemented tungsten carbide (WC-Co) substrates before diamond deposition by hot filament chemical vapor deposition (HFCVD). In particular, WC-5.8 wt %Co substrates were submitted to a thermal treatment by a continuous wave-high power diode laser to reduce surface Co concentration and promote the reconstruction of the WC grains. Laser pretreatments were performed both in N(2) and Ar atmosphere to prevent substrate oxidation. Diamond coatings were deposited onto the laser pretreated substrates by HFCVD. For comparative purpose, diamond coatings were also deposited on WC-5.8 wt %Co substrates chemically etched by the well-known two-step pretreatment employing Murakami's reagent and Caro's acid. Surface morphology, microstructure, and chemical composition of the WC-5.8 wt %Co substrates after the different pretreatments and the deposition of diamond coatings were assessed by surface profiler, scanning electron microscopy, energy-dispersive X-ray spectroscopy, and X-ray diffraction analyses. Wear performance of the diamond coatings was checked by dry sliding linear reciprocating tribological tests. The worn volume of the diamond coatings deposited on the laser pretreated substrates was always found lower than the one measured on the chemically etched substrates, with the N(2) atmosphere being particularly promising.     

Manufacturing signature and operating conditions in a variational model for tolerance analysis of rigid assemblies

The need of a univocal language for geometrical product specification considering all steps of the product life cycle such as design, manufacturing, and inspection is inevitable. Most models for Computer-Aided Tolerancing proposed by researchers and used in industry do not fully conform with standards. Moreover, most of them make severe assumptions on observable geometric deviations and can therefore hardly handle all kinds of 3D tolerances. These lacks inspired the idea and the development of a discrete geometry framework that is capable of considering geometric deviations of different stages of the product life cycle and is versatile regarding current and future tolerancing standards. This work uses a point cloud-based geometry representation scheme to implement the pattern left on the surfaces by a manufacturing process; then, this scheme has been inserted in a variational approach for tolerance analysis. Moreover, gravity and friction among the parts to assemble have been simulated too. In this way, a new Computer Aided Tolerancing (CAT) simulation tool has been developed; it approaches reality more than existing software packages do. To verify the effectiveness of the new CAT simulation tool, it has been applied to two case studies. The obtained results have been compared with those due to a geometrical model that has been developed by simulating what happens among the parts in the actual assembly. The obtained results show how the new CAT simulation tool gives results nearer to reality than literature models do.     

Beyond symbolizing: A response to Bornstein’s review.

Responds to the review by R. F. Bornstein (see record 2010-02522-001) on the current author's book, "Psychoanalysis and cognitive science: A multiple code theory" (see record 1997-08863-000). Although there is not much that Bornstein says with which Bucci can disagree, she responds specifically to a few of Bornstein's points and adds a few that he does not include. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Composition of methyl esters from heat-bodied linseed oils

Two heat-bodied linseed oils, with Gardner viscosities of 37 and 55 min, were saponified, converted to their methyl esters, and separated into 2 fractions with urea and methanol. Gas-liquid chromatography showed the adduct fraction, which comprised 38–41% of the total methyl esters, to contain: palmitic, stearic, oleic, “linoleic,” and trace amounts of “linolenic” acid. The nonadducting fraction (59–62%) of the total methyl esters was separated by molecular distillation at 140C/7 μ into a distillate and residue. The distillate amounted to 18–25% of the total methyl esters and had an iodine value (I.V.) of 142–145; its absorption at 232 mμ indicates 2.5–3.0% conjugated diene. Hydrogenation of this distillate gave a liquid product with an iodine number of 4 and a pour point of −50C. Gas chromatograms of the distillate and its hydrogenated derivative indicated at least 5–7 components. Comparison of these peaks with known fatty acid methyl esters indicates that the components of these fractions were either cyclic or branched esters. The nonadducting residue fraction was composed mainly of polymeric acids. Presented before the Division of Organic Coatings and Plastics Chemistry, Am. Chem. Soc. Washington, D.C., 1962. A laboratory of the No. Utiliz. Res. & Dev. Div., ARS, U.S.D.A.     

Polyester amides from linseed oil for protective coatings

The sodium alkoxide-catalyzed reaction of linseed oil or linseed methyl esters with diethanolamine produces almost exclusively linseed diethanolamides. Reaction conditions, e.g., temperature, amount of excess diethanolamine and mode of adding reactants, are reported. The best conditions for producing diethanolamide directly from linseed oil (1 mole) required adding oil to the sodium alkoxide in diethanolamine (6 moles) and heating at 110–115C for 35 min. The linseed diethanolamide isolated in 93–95% yield was an amber oil. Progress of the reaction, followed by thin-layer chromatography, showed only trace amounts of byproducts. Polyester amides were prepared by heating linseed diethanolamide in refluxing xylene with dibasic acids or anhydrides, e.g., azelaic, maleic, fumaric, phthalic, terephthalic, itaconic, brassylic and dimer acids. Molecular weight, viscosity and film properties (air-dried and baked) of the polyester amides were determined. Presented at the AOCS Meeting, Chicago, October 1964. No. Utiliz. Res. Dev. Div., ARS, USDA.     

The need for a "psychoanalytic psychology" in the cognitive science field.

Cognitive science has incorporated seminal concepts of psychoanalysis without acknowledging this influence. This article covers psychoanalytic ideas already incorporated—implicitly or explicitly—in modern cognitive psychology, as well as ideas whose inclusion would benefit the cognitive field. These include the emphasis on mental models, mind–body interaction, unconscious processes, dual processes of thought, and naturalistic research milieus. The article discusses reasons why the psychoanalytic roots of these ideas have not been acknowledged and shows how the theories of multiple coding and the referential process provide a basis for bridging the psychoanalytic and cognitive science fields. Finally, it is argued that scientific psychology requires a subfield of psychoanalytic psychology that covers the integration of information-processing functions, including somatic and emotional processes, in the context of an individual's overall goals. (PsycINFO Database Record (c) 2010 APA, all rights reserved)