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Riesz Lattices and Daniell Spaces. Measure Spaces, Associated Daniell Spaces, and Stieltjes Functionals. The Closure of a Daniell Space. The Integral for a Daniell Space. Integrals Derived from Measures and Measurability. Historical Remarks on the Definition of the Integral. List of Symbols and Notation. Index.

Rezension zu: 1) Deutsches Institut für Erwachsenenbildung: Trends der Weiterbildung. DIE-Trendanalyse 2010. Reihe DIE spezial. Bielefeld: W. Bertelsmann 2010. ISBN 978-3-7639-4242-8. 2) Dollhausen, Karin; Feld, Timm C.; Seitter, Wolfgang (Hrsg.): Erwachsenenpädagogische Organisationsforschung: Theorie und Empirie lebenslangen Lernens. Wiesbaden: VS Verl. f. Sozialwiss. ISBN 978-3-531-17634-5. 3) Ganguin, Sonja: Computerspiele und lebenslanges Lernen: eine Synthese von Gegensätzen. Wiesbaden: VS Verl. f. Sozialwiss. 2010. ISBN 978-3-531-17487-7. 4) Grotlüschen, Anke: Erneuerung der Interessetheorie: die Genese von Interesse an Erwachsenen- und Weiterbildung. Wiesbaden: VS Verl. f. Sozialwiss. 2010. ISBN 978-3-531-17491-4. 5) Hippel, Aiga von; Tippelt, Rudolf (Hrsg.). Fortbildung der Weiterbildner/innen: eine Analyse der Interessen und Bedarfe aus verschiedenen Perspektiven. Weinheim u.a.: Beltz 2009. ISBN 978-3-407-36486-9. 6) Kuhlenkamp, Detlef: Lifelong Learning: Programmatik, Realität, Perspektiven. Studienreihe Bildungs- und Wissenschaftsmanagement, Bd. 11. Münster: Waxmann 2010. ISBN 978-3-8309-2244-5. 7) Oliver, Esther: Research and Development in Adult Education: Fields and Trends. Leverkusen: B. Budrich 2010. ISBN 978-3-88649-304-9.

By means of a newly developed device, collision time and deformation depth have been determined as functions of the radius or the energy of glass and lead spheres with a diameter lying between 0.2 and 0.9 mm, which collide with an air/water or air/DCA-solution interface in normal direction. The best resolution of time and amplitude reached was 0.2539 ms and 3 μm, respectively. Results verify the assumption concerning the calculation of collision time that collision of a spherical particle in normal direction with a large bubble can be considered small elastic oscillation of a system with one degree of freedom in a first approximation. Collision times presented are about 130% greater than those calculated by Evans in 1954.

Thieno-triazolo-1,4-diazepines (hetrazepines) antagonize platelet-activating factor (PAF) induced platelet aggregation and inhibit the binding of [3H]-PAF. Introduction of a carboxamide alkyl side chain into the thiophene ring leads to compounds with less affinity to the benzodiazepine receptor and without sedative effects on the central nervous system (e.g., WEB 2086). By ring closure of the side chain, new tetracyclic compounds have been obtained. A parabolic relationship between either [3H]-PAF binding or PAF activity and the bulkiness of the alkyl substituents to the triazolo ring of the hetrazepines or of the bulkiness the 2-acyl moiety of the PAF analogues was found in quantitative structure-activity relationships. This suggests that perhaps the alkyl substituent of the hetrazepines fits the same receptor pocket as the 2-acyl moiety of the PAF agonists.

Review of pharmacological effects, structure-activity relationship of hetrazepines: oxazepines, thiazepines, diazepines

1,4-Diazepines with two annelated heterocycles (‘hetrazepines’) such as brotizolam (WE 941), WE 973 and WE 1008 bind with high affinities to benzodiazepine receptors in the central nervous system. Brotizolam has a pharmacologic spectrum of action similar to clinically useful benzodiazepines, while the closely related derivatives WE 973 and WE 1008 appear to lack hypnotic action. Unlike other benzodiazepine receptor ligands which share common pharmacologic properties with the benzodiazepines, the apparent affinities of WE 973 and WE 1008 are not increased significantly in the presence of GABA, even at an elevated incubation temperature. Furthermore, the apparent affinities of these compounds do not appear to be reduced as a result of increasing the incubation temperature. Brotizolam, like the benzodiazepines, facilitates GABAergic transmission in zona recitulata neurons of the substantia nigra. In contrast, at a dose which inhibits cell firing, WE 973 does not appear to significantly augment the inhibitory action of GABA in these cells. These observations suggest that the so-called ‘GABA shift’ may not be a valid means of distinguishing benzodiazepine-like compounds in vitro. Furthermore, these data suggest that facilitation of GABAergic transmission may be necessary for the hypnotic action of benzodiazepine receptor ligands, but not for the anticonflict or the anticonvulsant actions of such compounds.

A series of substituted 4-aryltetrahydrothieno[2,3-c]pyridines was prepared by acid-catalyzed cyclization of 1-aryl-2-[(2-thienylmethyl)amino]ethanol derivatives. The compounds were examined for their antidepressant activity, as demonstrated by their ability to inhibit the uptake of norepinephrine (NE) and serotonin (5-HT) and to prevent tetrabenazine-induced ptosis (TBZ) in mice. Significant inhibition of both neurotransmitters is observed for several of the tested compounds, while some of them are selective inhibitors of either NE or 5-HT uptake. Optimal activity is associated with the introduction of lipophilic substituents into the 4-position of the phenyl ring and less lipophilic substituents into the 2-position of the thiophene ring (11, 23). Compound 33 bearing substituents in positions 2 and 6 of the phenyl ring is inactive. This might be a consequence of an out of plane conformation of this compound.

Summary The effects of 1, 4-diazepines with two annelated heterocyles [brotizolam (WE 941), ciclotizolam (WE 973) and WE 1008] on gamma-aminobutyric acid (GABA) -stimulated chloride influx into rat brain membrane vesicles were examined. Brotizolam enhanced GABA (30 μM) -stimulated 36 Cl − influx (146.1% of control), while ciclotizolam and WE 1008 showed only a small enhancement (119.3% and 119.1%, respectively) of GABA-stimulated 36 Cl − uptake. Brotizolam resulted in a left shift of the GABA dose response curve at lower concentrations of GABA (10 μM), while at higher concentrations of GABA (1 mM), brotizolam caused a reduction of the maximal response. The enhancement of GABA-stimulated 36 Cl − uptake by brotizolam (0.1 μM) was antagonized by Ro 15–1788. At higher concentration of GABA (300 μM), brotizolam inhibited GABA-stimulated 36 Cl − uptake in a dose dependent manner and Ro15–1788 failed to antagonize this effect. These results suggest that 1) brotizolam produces an enhancement of GABA (30 μM) -stimulated chloride influx through the benzodiazepine receptor. 2) brotizolam inhibition of GABA (300 μM) -stimulated chloride influx involves an additional mechanism, and 3) the sedativehypnotic action of brotizolam may be related to its high efficacy at the benzodiazepine/GABA-gated chloride channel.

A radioimmunoassay for the determination of the hypnotic agent brotizolam (11) was developed. With this procedure, an antiserum was used which was obtained from rabbits immunized with the hapten 10 (We 934) covalently bound to bovine serum albumin and tritium-labeled brotizolam as the radioligand. Compound 10 represents a structural analogue of brotizolam: the bromine was replaced by a carboxyethyl group. By such manipulation high assay specificity against the primary human metabolites was achieved. The sensitivity limit of the assay was about 100 pg of brotizolam per mL of plasma when 0.1-mL samples were used. The assay showed good accuracy and high precision. Repeated assays after keeping plasma samples frozen for various periods again indicated high precision as well as the stability of the brotizolam molecule under these conditions. Application of the assay to plasma samples of eight subjects who received single oral 0.25-mg doses of brotizolam showed a mean maximum plasma concentration of 4.6 ng of unchanged drug per mL at 0.9 h after administration. The brotizolam plasma concentration declined with a mean elimination half-life of 5.1 h. The pharmacokinetic parameters estimated by RIA agree well with those obtained with other specific brotizolam determination procedures.

A series of substituted 4-aryltetrahydrothieno[2,3-c]pyridines was prepared by acid-catalyzed cyclization of 1-aryl-2-[(2-thienylmethyl)amino]ethanol derivatives. The compounds were examined for their antidepressant activity, as demonstrated by their ability to inhibit the uptake of norepinephrine (NE) and serotonin (5-HT) and to prevent tetrabenazine-induced ptosis (TBZ) in mice. Significant inhibition of both neurotransmitters is observed for several of the tested compounds, while some of them are selective inhibitors of either NE or 5-HT uptake. Optimal activity is associated with the introduction of lipophilic substituents into the 4-position of the phenyl ring and less lipophilic substituents into the 2-position of the thiophene ring (11, 23). Compound 33 bearing substituents in positions 2 and 6 of the phenyl ring is inactive. This might be a consequence of an out of plane conformation of this compound.

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