Organizational and direct support maintenance manual : teleprinter TT-804/MYQ-4A, (NSN 7010-01-153-0775).

Includes index.

Operator's manual : automated data processing system AN/MYQ-4A, (NSN 7010-01-158-5397).

Includes indexes.

Na 1 Nachlass Max Horkheimer, 802 - "Dialektik der Aufklärung" von Max Horkheimer und Theodor W. Adorno (p. XI 6.3 - XI 6.42)

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;

Na 1 Nachlass Max Horkheimer, 805 - Verschiedene Essays, Manuskripte, Entwürfe und Notizen u.a. aus dem Umkreis / bzgl. "Dialektik der Aufklärung" (p. XI 6a - XI 16.1-17)

"Notes. Verschiedene Essays"; Diese Mappe enthielt ursprünglich Fassungen von Aphorismen aus dem Umkreis von "Dialektik der Aufklärung", die den entsprechenden Stücken zugeordnet wurden; außerdem:; 1. Auszüge aus Thomas Hobbes, Leviathan; englisch, Anfang und Schluss fehlen. Typoskript, 5 Blatt; 2. Das Allgemeine nicht tiefer als das Besondere [= "Klassifikation" in der 'Dialektik der Aufklärung']. Typoskript, 1 Blatt; 3. Müßiggang als Merkmal vorbürgerlichen und nachbürgerlichen Zeitalters [GS 12, S. 315]. Typoskript, 1 Blatt; Thesen über Antisemitismus; Zumindest teilweise Vorarbeiten zum Kapitel "Elemente des Antisemitismus" der 'Dialektik der Aufklärung', 1943:; 1. Teilstück aus Abschnitt IV der "Elemente". Typoskript mit eigenen Korrekturen und Manuskript, 4 Blatt; 2. Teilstück aus Abschnitt V der "Elemente". Typoskript, 2 Blatt; 3. Antisemitismus als rationalisierte Ideosynkrasie. Typoskript mit eigenen Korrekturen, 1 Blatt; 4. Mimikry und Selbsterhaltung, Teilstücke:; 4a) Typoskript mit eigenen Korrekturen, 1 Blatt; 4b) Typoskript mit eigenen Korrekturen, 2 Blatt; 4c) Typoskript mit eigenen Korrekturen, 1 Blatt; 5. Technokratie und Faschismus. Teilstück, Typoskript, 1 Blatt; 6. Antisemitismus als verschobener Haß gegen kapitalistische Ausbeutung; Protokoll einer Diskussion zwischen Max Horkheimer und Theodor W. Adorno. Typoskript, 2 Blatt; 7. Über antisemitische Ideosynkrasie; Protokoll einer Diskussion zwischen Max Horkheimer und Theodor W. Adorno zur "Dialektik der Aufklärung", 'Elemte des Antisemitismus', These 4. Fragment, Typoskript, 1 Blatt; 8. Über Mimesis; Protokoll einer Diskussion zwischen Max Horkheimer und Theodor W. Adorno [GS 12, S. 587 ff.]. Typoskript, 3 Blatt; 9. - 10. Über Probleme der Erkenntnis des Antisemitismus in der Tradition der Humanwissenschaften. Typoskript, englisch, mit eigenen Korrekturen, 2 Blatt; 11. Völkischer Antisemitismus; Korrekturblatt. Manuskript, 4 Blatt; 12. Eigene und handschriftliche Notizen, 22 Blatt; 13. Exzerpte aus Werken Friedrich Nietzsches. Typoskript, 3 Blatt; 14. Exzerpt aus Gregorovius: "Wanderjahre in Italien". Typoskript, 1 Blatt; 15. Adorno, Theodor W.: Über antisemitische Propaganda. Typoskript mit eigenen Korrekturen, 6 Blatt; 16. Adorno, Theodor W.: Eigene Notizen, 3 Blatt; 17. 1 Zeitungsausschnitt, 1 Blatt; Manuskripte und Entwürfe als Vorarbeiten oder aus dem Umkreis der "Dialektik der Aufklärung":; 1. Über das Verhältnis von Naturbeherrschung und gesellschaftlicher Herrschaft; [von Theodor W. Adorno ?]. Entwurf, Typoskript, 3 Blatt; 2. Theodor W. Adorno [?]: Über Mythologie und Aufklärung. Typoskript mit eigenen Korrekturen, 13 Blatt; 3. Über das Verhältnis von Ökonomie und Politik in Liberalismus und Spätkapitalismus [GS 12, S. 316 - 318]. Typoskript mit eigenen Korrekturen, 3 Blatt; 4. Über den Begriff des Geistes in der materialistischen Aufklärung: Element der Macht. Teilstück, Typoskript und Manuskript, 1 Blatt; 5. Eigene Notizen u.a. über: Verhältnis von Geist und Natur, Verhältnis der Freudschen Methode zum Positivismus; Entwurf des Romans über Neville Chamberlain; 1942:; 1. "Grober Umriß der Handlung". Typoskript, 12 Blatt; 2. Anfang des Romans [GS 12, S. 329 - 341]:; 2a) Typoskript mit eigenen Korrekturen, 3 Blatt und eigene Notiz, 1 Blatt; 2b) Typoskript mit eigenen Korrekturen, 2 Blatt; 2c) Typoskript mit eigenen Korrekturen, 1 Blatt; 3. Exzerpte aus Schriften über Chamberlain, gesammelt von Herbert Marcuse. Typoskript, 8 Blatt, mit einer eigenen Notiz von Friedrich Pollock für Max Horkheimer, 1 Blatt; 4. Abschriften aus Zeitungsartikeln über Chamberlain. Typoskript, 22 Blatt; 5. Bibliotheks-Leihscheine und Literaturangaben. Handschriftliche Notizen, 10 Blatt; Über Psychoanalyse; um 1942. Fragment, Typoskript mit eigenen Korrekturen, 4 Blatt; Über Rackets, ihre Bedeutung von der Antike bis zum Kapitalismus; Zu einer Theorie des Proletariats; 1942:; 1. Notizen zum Programm des Buches, 30.8.1942. 2 Blatt; 2. Exzerpte aus Schriften zur Geschichte der Rackets (von Theodor W. Adorno). Typroskript, 30 Blatt; "Betrachtungen zum Curfew" [GS 5, S. 351 - 353]; um 1942:; a) Typoskript mit eigenen Korrekturen, 3 Blatt; b) Typoskript mit eigenen Korrekturen, 3 Blatt; c) Teilstück, Typoskript mit eigenen Korrekturen, 2 Blatt; d) Teilstück, Typoskript mit eigenen Korrekturen, 2 Blatt; e) Typoskript-Manuskript, 2 Blatt; "Sociology of Art" [GS 5, S. 360 - 363], 1942/1943; veröffentlicht in "Encyclopedia of the Arts", New York, 1946:; a) Typoskript, 4 Blatt; b) Photokopie des Drucks, 2 Blatt; Adorno, Theodor W.: Über Paul Tillich, "Man and Society in Religious Socialism"; Entwurf eines Briefs, 16.2.1944. Typoskript mit handschriftlichen Korrekturen von Theodor W. Adorno. 26 Blatt; "The Crisis of the Family", aus Max Horkheimers "Autorität und Familie. Allgemeiner Teil" (Paris 1936) zusammengestellt und übersetzt von Norbert Guterman (S. 63-76 und 49 - 63), 1945 ? Typoskript, 29 Blatt; New Yorker Notizen [II], 1945:; 1. "Dialektik - Mittelwek"; "Notizen zur Dialektik" [GS 12, S. 297 - 302]. Typoskript mit eigenen Korrekturen, 8 Blatt; 2. "Ritterlichkeit" [GS 12, S. 225 - 227]. Typoskript mit eigenen Korrekturen, 4 Blatt; 3. "Soziologische Unterscheidungen" [GS 12, S. 302 - 303]. Typoskript, 2 Blatt; 4. "Vertragstheorie". a) Typoskript, 6 Blatt. b) Typoskript mit eigenen Korrekturen, 7 Blatt; 5. "Bürgerliche Welt" [GS 12, S. 227 - 232]. Typoskript, 8 Blatt; 6. "Enge des Herzens" [GS 12, S. 232 - 234]. Typoskript, 2 Blatt; 7. "Unabänderlichkeit?" [GS 12, S. 234 - 237]. Typoskript mit eigenen Korrekturen, 6 Blatt; 8. "Die Juden und der Eid" [GS 12, S. 303 - 305]:; 8a) Typoskript mit eigenen Korrekturen, 3 Blatt; 8b) Typoskript mit handschriftlichen Korrekturen, 3 Blatt; 8c) Typoskript mit eigenen Korrekturen, 2 Blatt; 9. "Das Rationale und das Irrationale" [GS 12, S. 306]. Typoskript, 1 Blatt; 10. "Zur Dialektik" - "Zur Architektur" - "Zum Commerce" - "Text zu einer Illustration aus 'La Femme 100 tetes'" [GS 12, S. 306 - 308]. Typoskript, 2 Blatt; 11. "On Vivisection" = Brief an Ned R. Healy, New York, 22.3.1945. Typoskript, 2 Blatt; 12. "Der 'Schrecken' in der französischen Revolution" [GS 12, S. 238 - 239]. Typoskript mit eigenen Korrekturen, 3 Blatt; 13. "Autorität und Vernunft" [GS 12, S. 239 - 243]:; 13a) Typoskript mit eigenen Korrekturen, 6 Blatt; 13b) Typoskript mit dem Titel "Faschismus und gesellschaftliche Ordnung", 6 Blatt; 13c) Typoskript mit eigenen Korrekturen, 7 Blatt; 14. "Zum Gottesbegriff":; 14a) Typoskript, 4 Blatt; 14b) Typoskript mit eigenen Korrekturen, 4 Blatt; 15. "Der Mensch verändert sich in der Geschichte" [GS 12, S. 244 - 246]:; 15a) Typoskript, 3 Blatt; 15b) Typoskript, 3 Blatt; 16. "Zur materialistischen Geschichtstheorie" [GS 12, S. 246 - 247]. Typoskript, 2 Blatt; 17. "Die schlechten Elemente des Liberalismus" [GS 12, S. 247 - 249]:; 17a) Typoskript, 3 Blatt; 17b) Typoskript mit eigenen Korrekturen, 3 Blatt;

1H-1,3-Diazepines, 5H-1,3-diazepines, 1,3-diazepinones, and 2,4-diazabicyclo[3.2.0]heptenes

Tetrazolo[1,5-a] pyridines/ 2-azidopyridines 1 undergo photochemical nitrogen elimination and ring expansion to 1,3-diazacyclohepta-1,2,4,6-tetraenes 3, which react with alcohols to afford 2-alkoxy-1H-1,3-diazepines 4 (5), with secondary amines to 2-dialkylamino-5H-1,3-diazepines 16, sometimes via isolable 2-dialkylamino-1H-1,3-diazepines 15, and with water to 1,3-diazepin-2-ones 19. The latter are also obtained by elimination of isobutene or propene from 2-tert-butoxy- or 2-isopropoxy-1H-1,3-diazepines 4 or 5. 1,3-Diazepin-2-one 22B and 1,3-diazepin-4-one 24 were obtained from hydrolysis of the corresponding 4-chlorodiazepines. Diazepinones 19 undergo photochemical ring closure to diazabicycloheptenones 25 in high yields. The 2-alkoxy-1H-1,3-diazepines 4 and 5 interconvert by rapid proton exchange between positions N1 and N3. The free energies of activation for the proton exchange were measured by the Forsen - Hoffman method as DeltaGdouble dagger(298) = 16.2 +/- 0.6 kcal mol(-1) as an average for 4a - c in CD2Cl2, acetone-d(6), and methanol-d(4), and 14.1 +/- 0.6 kcal mol(-1) for 4c in acetone/D2O. The structures of 2-methoxy-5,6-bis( trifluoromethyl)-1H-1,3-diazepine 4k, 1,2-dihydro-4-diethylamino-5H-1,3-diazepin-2-one 22bB, and diazabicycloheptanone 26 were determined by X-ray crystallography. The former represents the first reported X-ray crystal structure of any monocyclic N-unsubstituted 1H-azepine.

Antidepressant/anxiolytic and anti-nociceptive effects of novel 2-substituted 1,4-benzodiazepine-2-ones

Oxazepam (4a) has been used as overall starting material in the synthesis of novel 2-substituted 1,4-benzodiazepines. By reacting Oxazepam 4a with commercially available hydrazines, hydrazides, semicarbazide, aminoguanidine and N,N-dimethylamino aniline in ethanol under acetic conditions, a series of diazenyl-1,4-benzodiazepines 5a-5i and 2-amino- 1,4-benzodiazepine 5k were obtained in good yields. These novel compounds served as new chemical entities (NCE) for testing in mice. The diazo-benzodiazepine 5d has shown a promising antidepressant effect in initial experiments in vivo at a dose of 5 mg/kg. The highly coloured 2-aminobenzodiazepine derivative 5k showed over a dose range from 5-50 mg/kg an analgesic effect in mice. © Singh et al.

(Table 1) Clay and non-clay mineral composition of dirty ice samples from across the Arctic

Extensive dirty ice patches with up to 7 kg/m**2 sediment concentrations in layers of up to 10 cm thickness were encountered in 2005 and 2007 in numerous areas across the central Arctic. The Fe grain fingerprint determination of sources for these sampled dirty ice floes indicated both Russian and Canadian sources, with the latter dominating. The presence of benthic shells and sea weeds along with thick layers (2-10 cm) of sediment covering 5-10 m2 indicates an anchor ice entrainment origin as opposed to suspension freezing for some of these floes. The anchor ice origin might explain the dominance of Canadian sources where only narrow flaw leads occur that would not favor suspension freezing as an entrainment process. Expandable clays, commonly used as an indicator of a Kara Sea origin for dirty sea ice, are present in moderately high percentages (>20%) in many circum-Arctic source areas, including the Arctic coasts of North America. Some differences between the Russian and the North American coastal areas are found in clay mineral abundance, primarily the much higher abundance of chlorite in North America and the northern Barents Sea as opposed to the rest of the Russian Arctic. However, sea ice clay mineralogy matched many source areas, making it difficult to use as a provenance tool by itself. The bulk mineralogy (clay and non-clay) does not match specific sources possibly due to reworking of the sediment in dirty floes through summer melting or the failure to characterize all possible source areas.

STARTVerso1: A Randomized Trial of Faldaprevir Plus Pegylated Interferon/Ribavirin for Chronic HCV Genotype-1 Infection

BACKGROUND & AIMS: The efficacy and tolerability of faldaprevir, a potent hepatitis C virus (HCV) NS3/4A protease inhibitor, plus peginterferon (PegIFN) and ribavirin (RBV) was assessed in a double-blind, placebo-controlled phase 3 study of treatment-naïve patients with HCV genotype-1 infection. METHODS: Patients were randomly assigned (1:2:2) to PegIFN/RBV plus: placebo (arm 1, n = 132) for 24 weeks; faldaprevir (120 mg, once daily) for 12 or 24 weeks (arm 2, n = 259); or faldaprevir (240 mg, once daily) for 12 weeks (arm 3, n = 261). In arms 2 and 3, patients with early treatment success (HCV-RNA <25 IU/ml at week 4 and undetectable at week 8) stopped all treatment at week 24. Other patients received PegIFN/RBV until week 48 unless they met futility criteria. The primary endpoint was sustained virologic response 12 weeks post-treatment (SVR12). RESULTS: SVR12 was achieved by 52%, 79%, and 80% of patients in arms 1, 2, and 3, respectively (estimated difference for arms 2 and 3 vs. arm 1: 27%, 95% confidence interval 17%-36%; and 29%, 95% confidence interval, 19%-38%, respectively; p < 0.0001 for both). Early treatment success was achieved by 87% (arm 2) and 89% (arm 3) of patients, of whom 86% and 89% achieved SVR12. Adverse event rates were similar among groups; few adverse events led to discontinuation of all regimen components. CONCLUSIONS: Faldaprevir plus PegIFN/RBV significantly increased SVR12, compared with PegIFN/RBV, in treatment-naïve patients with HCV genotype-1 infection. No differences were seen in responses of patients given faldaprevir once daily at 120 or 240 mg.

Up-regulation Of Dnam-1 And Nkp30, Associated With Improvement Of Nk Cells Activation After Long-term Culture Of Mononuclear Cells From Patients With Ovarian Neoplasia.

This study aimed at evaluating the functional activation and activating receptors expression on resting, short- and long-term NK and NK-like T cells from blood of ovarian neoplasia patients. Blood from patients with adnexal benign alterations (n = 10) and ovarian cancer (grade I-IV n = 14) were collected after signed consent. Effector cells activation was evaluated by the expression of the CD107a molecule. Short-term culture was conducted overnight with IL-2 and long-term culture for 21 days, by a method designed to expand CD56(+) lymphocytes. Short-term culture significantly increased NK cells activation compared to resting NK cells (p<0.05), however, the long-term procedure supported an even higher increase (p<0.001). Resting NK-like T cells showed poor activation, which was not altered by the culture procedures. The long-term culture effectively increased the expression of the activating receptors on NK and NK-like T cells, either by increasing the number of cells expressing a given receptor and/or by up-regulating their expression intensity. As a conclusion, the long-term culture system employed, resulted in a high number of functional NK cells. The culture system was particularly efficient on the up-regulation of NKp30 and DNAM-1 receptors on NK cells.

Hypertrophic Adenoid Is A Major Infection Site Of Human Bocavirus 1.

Human bocavirus 1 (HBoV1) is associated with respiratory infections worldwide, mainly in children. Similar to other parvoviruses, it is believed that HBoV1 can persist for long periods of time in humans, probably through maintaining concatemers of the virus single-stranded DNA genome in the nuclei of infected cells. Recently, HBoV-1 was detected in high rates in adenoid and palatine tonsils samples from patients with chronic adenotonsillar diseases, but nothing is known about the virus replication levels in those tissues. A 3-year prospective hospital-based study was conducted to detect and quantify HBoV1 DNA and mRNAs in samples of the adenoids (AD), palatine tonsils (PT), nasopharyngeal secretions (NPS), and peripheral blood (PB) from patients undergoing tonsillectomy for tonsillar hypertrophy or recurrent tonsillitis. HBoV1 was detected in 25.3% of the AD samples, while the rates of detection in the PT, NPS, and PB samples were 7.2%, 10.5%, and 1.7%, respectively. The viral loads were higher in AD samples, and 27.3% of the patients with HBoV had mRNA detectable in this tissue. High viral loads and detectable mRNA in the AD were associated with HBoV1 detection in the other sample sites. The adenoids are an important site of HBoV1 replication and persistence in children with tonsillar hypertrophy. The adenoids contain high HBoV1 loads and are frequently positive for HBoV mRNA, and this is associated with the detection of HBoV1 in secretions.

A Putative Otu Domain-containing Protein 1 Deubiquitinating Enzyme Is Differentially Expressed In Thyroid Cancer And Identifies Less-aggressive Tumours.

This study aimed to identify novel biomarkers for thyroid carcinoma diagnosis and prognosis. We have constructed a human single-chain variable fragment (scFv) antibody library that was selected against tumour thyroid cells using the BRASIL method (biopanning and rapid analysis of selective interactive ligands) and phage display technology. One highly reactive clone, scFv-C1, with specific binding to papillary thyroid tumour proteins was confirmed by ELISA, which was further tested against a tissue microarray that comprised of 229 thyroid tissues, including: 110 carcinomas (38 papillary thyroid carcinomas (PTCs), 42 follicular carcinomas, 30 follicular variants of PTC), 18 normal thyroid tissues, 49 nodular goitres (NG) and 52 follicular adenomas. The scFv-C1 was able to distinguish carcinomas from benign lesions (P=0.0001) and reacted preferentially against T1 and T2 tumour stages (P=0.0108). We have further identified an OTU domain-containing protein 1, DUBA-7 deubiquitinating enzyme as the scFv-binding antigen using two-dimensional polyacrylamide gel electrophoresis and mass spectrometry. The strategy of screening and identifying a cell-surface-binding antibody against thyroid tissues was highly effective and resulted in a useful biomarker that recognises malignancy among thyroid nodules and may help identify lower-risk cases that can benefit from less-aggressive management.

Treadmill Training Increases Sirt-1 And Pgc-1 α Protein Levels And Ampk Phosphorylation In Quadriceps Of Middle-aged Rats In An Intensity-dependent Manner.

The present study investigated the effects of running at 0.8 or 1.2 km/h on inflammatory proteins (i.e., protein levels of TNF- α , IL-1 β , and NF- κ B) and metabolic proteins (i.e., protein levels of SIRT-1 and PGC-1 α , and AMPK phosphorylation) in quadriceps of rats. Male Wistar rats at 3 (young) and 18 months (middle-aged rats) of age were divided into nonexercised (NE) and exercised at 0.8 or 1.2 km/h. The rats were trained on treadmill, 50 min per day, 5 days per week, during 8 weeks. Forty-eight hours after the last training session, muscles were removed, homogenized, and analyzed using biochemical and western blot techniques. Our results showed that: (a) running at 0.8 km/h decreased the inflammatory proteins and increased the metabolic proteins compared with NE rats; (b) these responses were lower for the inflammatory proteins and higher for the metabolic proteins in young rats compared with middle-aged rats; (c) running at 1.2 km/h decreased the inflammatory proteins and increased the metabolic proteins compared with 0.8 km/h; (d) these responses were similar between young and middle-aged rats when trained at 1.2 km. In summary, the age-related increases in inflammatory proteins, and the age-related declines in metabolic proteins can be reversed and largely improved by treadmill training.

The Analgesic Effect Of Dipyrone In Peripheral Tissue Involves Two Different Mechanisms: Neuronal K(atp) Channel Opening And Cb(1) Receptor Activation.

Dipyrone (metamizole) is an analgesic pro-drug used to control moderate pain. It is metabolized in two major bioactive metabolites: 4-methylaminoantipyrine (4-MAA) and 4-aminoantipyrine (4-AA). The aim of this study was to investigate the participation of peripheral CB1 and CB2 cannabinoid receptors activation in the anti-hyperalgesic effect of dipyrone, 4-MAA or 4-AA. PGE2 (100ng/50µL/paw) was locally administered in the hindpaw of male Wistar rats, and the mechanical nociceptive threshold was quantified by electronic von Frey test, before and 3h after its injection. Dipyrone, 4-MAA or 4-AA was administered 30min before the von Frey test. The selective CB1 receptor antagonist AM251, CB2 receptor antagonist AM630, cGMP inhibitor ODQ or KATP channel blocker glibenclamide were administered 30min before dipyrone, 4-MAA or 4-AA. The antisense-ODN against CB1 receptor expression was intrathecally administered once a day during four consecutive days. PGE2-induced mechanical hyperalgesia was inhibited by dipyrone, 4-MAA, and 4-AA in a dose-response manner. AM251 or ODN anti-sense against neuronal CB1 receptor, but not AM630, reversed the anti-hyperalgesic effect mediated by 4-AA, but not by dipyrone or 4-MAA. On the other hand, the anti-hyperalgesic effect of dipyrone or 4-MAA was reversed by glibenclamide or ODQ. These results suggest that the activation of neuronal CB1, but not CB2 receptor, in peripheral tissue is involved in the anti-hyperalgesic effect of 4-aminoantipyrine. In addition, 4-methylaminoantipyrine mediates the anti-hyperalgesic effect by cGMP activation and KATP opening.

Synthesis And Antiproliferative Activity Of 8-hydroxyquinoline Derivatives Containing A 1,2,3-triazole Moiety.

Twelve novel 8-hydroxyquinoline derivatives were synthesized with good yields by performing copper-catalyzed Huisgen 1,3-dipolar cycloaddition (click reaction) between an 8-O-alkylated-quinoline containing a terminal alkyne and various aromatic or protected sugar azides. These compounds were evaluated in vitro for their antiproliferative activity on various cancer cell types. Protected sugar derivative 16 was the most active compound in the series, exhibiting potent antiproliferative activity and high selectivity toward ovarian cancer cells (OVCAR-03, GI50 < 0.25 μg mL(-1)); this derivative was more active than the reference drug doxorubicin (OVCAR-03, GI50 = 0.43 μg mL(-1)). In structure-activity relationship (SAR) studies, the physico-chemical parameters of the compounds were evaluated and docking calculations were performed for the α-glucosidase active site to predict the possible mechanism of action of this series of compounds.