946 resultados para 2,3-dicloro-6,7-dinitroquinoxalina


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The 1810 edition published under the title: "An account of expeditions to the sources of the Mississippi ..."

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Trägerband: Inc. qu. 738; Inc. qu. 913; 'Vocabularius Ex quo'; Vorbesitzer: Dominikanerkloster Frankfurt am Main

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3. Aus der "Dialektik der Aufklärung"; Kapitel: "Juliette oder Aufklärung und Moral". Typoskript mit dem Titel "Aufklärung und Rigorismus", mit handschriftlichen Korrekturen, 52 Blatt (2 Exemplare); 4. Aus der "Dialektik der Aufklärung"; Kapitel: "Kulturindustrie". Typoskript mit dem Titel "Das Schema der Massenkultur":; 4a) Typoskript mit handschriftlichen Korrekturen, 67 Blatt; 4b) Typoskript mit eigenen Korrekturen, 106 Blatt; 5. - 110. Gedruckte und ungedruckte Aufzeichnungen und Entwürfe zur "Dialektik der Aufklärung: Sammlungen A, B, C, D, die teilweise identisch sind; 5. - 42. Sammlung A: "Aphorismen"; 5. "Zum Problem der Bedürfnisse". Typoskript, 5 Blatt; 6. "Mensch und Tier". Typoskript mit eigenen Korrekturen, 12 Blatt; 7. "Propaganda". Typoskript, 2 Blatt; 8. "Straftheorie". Typoskript mit eigenen Korrekturen, 3 Blatt; 9. "Dichtung und Moral". Typoskript mit eigenen Korrekturen, 5 Blatt; 10. "Zur Genese der Dummheit". Typoskript, 3 Blatt; 11. "Interesse am Körper". Typoskript mit eigenen Korrekturen, 6 Blatt; 12. "Philosophie und Arbeitsteilung". Typoskript, 3 Blatt; 13. "Widersprüche". Typoskript, 4 Blatt; 14. "Geschichte der amerikanischen Arbeiterschaft". Typoskript, 1 Blatt; 15. "Feind". Typoskript, 2 Blatt; 16. "Gezeichnet". Typoskript mit eigenen Korrekturen, 2 Blatt; 17. "Erkenntnis und Sprache". Typoskript, 1 Blatt; 18. "Unmöglichkeit der Dichtung". Typoskript, 1 Blatt; 19. "Erbsünde und Kopula". Typoskript, 2 Blatt; 20. "Die Einseitigkeit der Negativität". Typoskript, 2 Blatt [= "Für Voltaire" in der "Dialektik der Aufklärung"]; 21. "Klassifikation". Typoskript mit eigenen Ergänzungen, 1 Blatt; 22. "Jüdischer Charakter". Typoskript mit eigenen Korrekturen, 1 Blatt; 23. "Lawine". Typoskript mit eigenen Korrekturen, 2 Blatt; 24. "Solidarität". Typoskript mit eigenen Korrekturen, 2 Blatt; 25. "Bewußtsein". Typoskript, 1 Blatt; 26. "Gegen Bescheidwissen". Typoskript, 1 Blatt; 27. "Der Gedanke". Typoskript, 1 Blatt; 28. "Quand-même". Typoskript, 2 Blatt; 29. "Leeres Erschrecken". Typoskript mit eigenen Korrekturen, 2 Blatt; 30. "Haupt- und Nebensatz". Typoskript, 3 Blatt; 31. "Verwandlung der Idee in Herrschaft". Typoskript mit eigenen Korrekturen, 5 Blatt; 32. "Isolierung durch Verkehr". Typoskript, 1 Blatt; 33. "Kampf und Gewaltlosigkeit". Typoskript, 6 Blatt; 34. "Zwei Welten". Typoskript, 2 Blatt; 35. "Zur Theorie der Gespenster". Typoskript, 1 Blatt; 36. "Notiz" [= "Umschlag der idealistischen Dialektik"]. Typoskript, 1 Blatt; 37. "Massengesellschaft". Typoskript, 1 Blatt; 38. "Tierpsychologie". Typoskript, 1 Blatt; 39. "Denkmale der Humanität". Typoskript mit eigenen Korrekturen, 1 Blatt; 40. "Physiognomik". Typoskript mit eigenen Korrekturen, 1 Blatt; 41. "Die Rackets und der Geist". Typoskript mit eigenen Korrekturen, 7 Blatt; 42. "Altmodisches Problem". Typoskript mit eigenen Korrekturen, 2 Blatt;

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3-Fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines (14, 16, and 18-22) are highly potent and selective inhibitors of phenylethanolamine N-methyltransferase (PNMT). Molecular modeling studies with 3-fluoromethyl-7-(N-alkyl aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines, such as 16, suggested that the sulfonamide -NH-could form a hydrogen bond with the side chain of Lys57. However, SAR studies and analysis of the crystal structure of human PNMT (hPNMT) in complex with 7 indicated that the sulfonamide oxygens, and not the sulfonamide -NH-, formed favorable interactions with the enzyme. Thus, we hypothesized that replacement of the sulfonamide -NH-with a methylene group could result in compounds that would retain potency at PNMT and that would have increased lipophilicity, thus increasing the likelihood they will cross the blood brain barrier. A series of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines (23-30) were synthesized and evaluated for their PNMT inhibitory potency and affinity for the R2-adrenoceptor. A comparison of these compounds with their isosteric sulfonamides (14, 16, and 18-22) showed that the sulfones were more lipophilic but less potent than their corresponding sulfonamides. Sulfone 24 (hPNMT K-i = 1.3 mu M) is the most potent compound in this series and is quite selective for PNMT versus the R2-adrenoceptor, but 24 is less potent than the corresponding sulfonamide, 16 (hPNMT K-i = 0.13 mu M). We also report the crystal structure of hPNMT in complex with sulfonamide 15, from which a potential hydrogen bond acceptor within the hPNMT active site has been identified, the main chain carbonyl oxygen of Asn39. The interaction of this residue with the sulfonamide -NH-is likely responsible for much of the enhanced inhibitory potency of the sulfonamides versus the sulfones.

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The VPAC(1) receptor belongs to family B of G protein-coupled receptors (GPCR-B) and is activated upon binding of the vasoactive intestinal peptide (VIP). Despite the recent determination of the structure of the N terminus of several members of this receptor family, little is known about the structure of the transmembrane (TM) region and about the molecular mechanisms leading to activation. In the present study, we designed a new structural model of the TM domain and combined it with experimental mutagenesis experiments to investigate the interaction network that governs ligand binding and receptor activation. Our results suggest that this network involves the cluster of residues Arg(188) in TM2, Gln(380) in TM7, and Asn(229) in TM3. This cluster is expected to be altered upon VIP binding, because Arg(188) has been shown previously to interact with Asp(3) of VIP. Several point mutations at positions 188, 229, and 380 were experimentally characterized and were shown to severely affect VIP binding and/or VIP-mediated cAMP production. Double mutants built from reciprocal residue exchanges exhibit strong cooperative or anticooperative effects, thereby indicating the spatial proximity of residues Arg(188), Gln(380), and Asn(229). Because these residues are highly conserved in the GPCR-B family, they can moreover be expected to have a general role in mediating function.

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The reaction of Cs4[Re6Te8(CN)6]·2H2O with Cu(en)2Cl2 in water affords crystals of a cluster complex [{Cu(H2O)(en) 2}{Cu(en)2}Re6Te8(CN)6]·3H2O. The structure of the compound is determined by single crystal X-ray diffraction (a = 10.8082(4) Å, b = 16.5404(6) Å, c = 24.6480(7) Å, β = 92.696(1)°, V = 4401.5(3) Å3, Z = 4, space group P21/n, R 1 = 0.0331, wR 2 (all data) = 0.0652). In the complex, cluster [Re6Te8(CN)6]4- anions are linked by Cu2+ cations into zigzag chains through cyanide bridges. The coordination environment of the copper cations is complemented by ethylenediamine molecules. Each of the cluster anions is additionally coordinated by a terminal fragment {Cu(H2O)(en)2}. © 2014 Pleiades Publishing, Ltd.

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It has been reported that fetal exposure to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) causes defects in the male reproductive system of the rat. We set out to replicate and extend these effects using a robust experimental design. Groups of 75 (control vehicle) or 55 (50, 200 or 1000 ng of TCDD kg-1 bodyweight) female Wistar(Han) rats were exposed to TCDD on Gestational Day (GD) 15, then allowed to litter. The high dose group dams showed no sustained weight loss compared to control, but four animals had total litter loss. Pups in the high dose group showed reduced body weight up till day 21, and pups in the medium dose group showed reduced body weight in the first week post partum. Balano-preputial separation (BPS) was significantly delayed in the high dose group male offspring. There were no significant effects of treatment when the offspring were subjected to a functional observational battery, or mated with females to assess reproductive capability. 25 males per group were killed on post natal day (PND) 70, and ~60 animals per group (~30 for the high dose group) on PND120 to assess seminology and other endpoints. At PND120, the two highest dose groups showed a statistically significant elevation of sperm counts, compared to control; however, this effect was small (~30%), within the normal range of sperm counts for this strain of rat, was not reflected in testicular spermatid counts nor PND70 data, and is therefore postulated to have no biological significance. Although there was an increase in the proportion of abnormal sperm at PND70, seminology parameters were otherwise unremarkable. Testis weights in the high dose group were slightly decreased at PND 70 and 120, and at PND120, brain weights were decreased in the high dose group, liver to body weight ratios were increased for all three dose groups, with an increase in inflammatory cell foci in the epididymis in the high dose group. These data show that TCDD is a potent developmental toxin after exposure of the developing fetus, but that acute developmental exposure to TCDD on GD15 caused no decrease in sperm counts.

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We compared the effects of a single acute dose, or chronic fetal exposure, to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) on the male reproductive system of the Wistar(Han) rat. Tissue samples were taken from dams on GD16 and GD21, and from offspring on PND70 and 120. Steady state concentration of TCDD was demonstrated in the chronic study: body burdens were comparable in both studies. Fetal TCDD concentrations were comparable after acute and chronic exposure, and demonstrate more potent toxicity after chronic versus acute dosing. In maternal liver, cytochrome P450 (CYP)1A1 and CYP1A2 RNA were induced. In fetus, there was induction of both CYP1A1 and CYP1A2 RNA at medium and high doses, but inadequate evidence for induction at low dose in either study. The low level induction of CYP1A1 RNA at low dose in fetus argues against AhR activation in fetus as a mechanism of toxicity of TCDD in causing delay in balanopreputial separation, and the greater induction of CYP1A1 RNA in PND70 offspring liver suggests that lactational transfer of TCDD is crucial to this toxicity. These data characterise the maternal and fetal disposition of TCDD, induction of CYP1A1 RNA as a measure of AhR activation, and suggest that lactational transfer of TCDD determines the difference in delay in balanopreputial separation between the two studies.

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The mixed anion mineral dixenite has been studied by Raman spectroscopy, complimented with infrared spectroscopy. The Raman spectrum of dixenite shows bands at 839 and 813 cm-1 assigned to the (AsO3)3- symmetric and antisymmetric stretching modes. The most intense Raman band of dixenite is the band at 526 cm-1 and is assigned to the ν2 AsO33- bending mode. DFT calculations enabled the position of AsO22- symmetric stretching mode at 839 cm-1, the antisymmetric stretching mode at 813 cm-1, and the deformation mode at 449 cm-1 to be calculated. Raman bands at 1026 and 1057 cm-1 are assigned to the SiO42- symmetric stretching vibrations and at 1349 and 1386 cm-1 to the SiO42- antisymmetric stretching vibrations. Both Raman and infrared spectra indicate the presence of water in the structure of dixenite. This brings into question the commonly accepted formula of dixenite as CuMn2+14Fe3+(AsO3)5(SiO4)2(AsO4)(OH)6. The formula may be better written as CuMn2+14Fe3+(AsO3)5(SiO4)2(AsO4)(OH)6•xH2O.

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The structure of the 1:1 brucinium salt of cis-cyclohexane-1,2-dicarboxylic acid, 2,3-dimethoxy-10-oxostrychnidinium (1R,2S)-2-carboxycyclohexane-1-carboxylate dihydrate, has revealed the resolved (1R,2S) enantiomer of the acid. Crystals of the compound are orthorhombic, space group P212121, with unit cell dimensions a = 8.1955(3), b = 12.4034(3), c = 29.9073(9)Å, and Z = 4. The asymmetric unit comprises the brucinium cation, the hydrogen cis-cyclohexane-1,2-dicarboxylate cation, in which the carboxylate group is disordered over two sites (58, 42%), and two water molecules of solvation, one of which is occupies two 50% occupancy sites. The classic undulating brucinium cation substructures are present with the anion and the water molecules occupying the interstitial cavities and are hydrogen-bonded to them in a two-dimensional network structure.