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Zusammenfassung: In den 1990er Jahren kam es zu einem Wiederaufleben in der Oberflächenendoprothetik des Hüftgelenks. Die Metall-Metall-Gleitpaarung stellt heute besonders bei jüngeren, aktiven Patienten eine Therapieoption dar. Im Vergleich zu den Totalendoprothesen mit gestielten Hüftschäften bietet der Oberflächenersatz Vorteile, insbesondere in Hinblick auf den femoralen Knochenverlust. Die kurzfristigen Resultate sind sehr gut. In der aktuellen Literatur wird über Revisionsraten von <1% berichtet. Im Vergleich zur konventionellen Hüftendoprothetik stellt die Luxation eine seltene Komplikation dar. Bei konventioneller Versorgung ist mit einer Luxationsrate von 2–5% zu rechnen. In Auswertung der internationalen Literatur ist hier im Vergleich bei der Oberflächenendoprothetik nur eine durchschnittliche Luxationsrate von 0,21% zu finden.

In the digital era of big data, data analytics and smart cities, a new generation of planning support systems is emerging. The Rapid Analytics Interactive Scenario Explorer is a novel planning support system developed to help planners and policy-makers determine the likely land value uplift associated with the provision of new city infrastructure. The Rapid Analytics Interactive Scenario Explorer toolkit was developed following a user-centred research approach including iterative design, prototyping and evaluation. Tool development was informed by user inputs obtained through a series of co-design workshops with two end-user groups: land valuers and urban planners. The paper outlines the underlying technical architecture of the toolkit, which has the ability to perform rapid calculations and visualise the results, for the end-users, through an online mapping interface. The toolkit incorporates an ensemble of hedonic pricing models to calculate and visualise value uplift and so enable the user to explore what if?scenarios. The toolkit has been validated through an iterative case study approach. Use cases were related to two policy areas: property and land valuation processes (for land taxation purposes) and value uplift scenarios (for value capture purposes). The cases tested were in Western Sydney, Australia. The paper reports on the results of the ordinary least square linear regressions – used to explore the impacts of hedonic attributes on property value at the global level – and geographically weighted regressions – developed to provide local estimates and explore the varying spatial relationships between attributes and house price across the study area. Building upon the hedonic modelling, the paper also reports the value uplift functionality of the Rapid Analytics Interactive Scenario Explorer toolkit that enables users to drag and drop new train stations and rapidly calculate expected property prices under a range of future transport scenarios. The Rapid Analytics Interactive Scenario Explorer toolkit is believed to be the first of its kind to provide this specific functionality. As it is problem and policy specific, it can be considered an example of the next generation of data-driven planning support system.

Ten 3β-ecgonine analogues were synthesized and characterized by ¹H and ¹³C NMR, MS, and elemental analysis. The compounds were synthesized as (−)-stereoisomers from (−)-cocaine. These compounds were assessed for their ability to inhibit [³H]cocaine binding to rat striatal tissue and to inhibit [³H]DA uptake into rat striatal synaptosomes. In this series of compounds, the length of the spacer between the aryl group and the tropane skeleton ranged from 1 to 4 bond distances, and conformational flexibility of the linkage and orientation of the aryl ring system were controlled by various types of linkages. The most potent of the analogues was methyl-(1R-2-exo-3-exo)-8-methyl-3-(β-styrenyl)-8-azabicyclo[3.2.1]octane-2-carboxylate. One of the less potent compounds was found to inhibit [³H]cocaine binding and [³H]DA uptake with significantly different IC50 values, in contrast to 14 other 3β-substituted analogues. Molecular modeling and CoMFA analysis were used to obtain a rigorous structure−function relationship for the studied compounds. The results showed that the potencies of these 3β-substituted ecgonine methyl esters were dominated by steric effects and were acutely sensitive to the distance between the aryl ring and the tropane skeleton and to the orientation of the aryl ring system relative to the tropane skeleton. The current study provides a clearer picture of the shape and size of the putative hydrophobic binding pocket for the 3β substituent at the cocaine receptor as well as emphasizing the importance of a drug's free energy of solvation in obtaining structure−activity relationships.