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Clelia Dallanoce Mara Canovi Carlo Matera Tiziana Mennini Marco De Amici Marco Gobbi Carlo De Micheli 《Bioorganic & medicinal chemistry》2012,20(21):6344-6355
A group of spirocyclic tropanyl-Δ2-isoxazolines was synthesized exploiting the 1,3-dipolar cycloaddition of nitrile oxides to olefins. Their interaction with the dopamine and serotonin transporters (DAT and SERT, respectively) was evaluated through binding experiments. The majority of the compounds had no inhibitory effects (IC50 >> 10 μM), while some had an IC50 value in the range 5–10 μM (8a–c, 10b and 11c on DAT, 12b on SERT). Unexpectedly, one of the tertiary amines under investigation, that is 3′-methoxy-8-methyl-spiro{8-azabicyclo[3.2.1]octane-3,5′(4′H)-isoxazole 7a, was able to enhance at a concentration of 10 μM both [3H]citalopram and [3H]paroxetine binding to SERT in rat brain homogenate (up to 25%, due to an increase of Bmax) and [3H]serotonin uptake (up to 30%) in cortical synaptosomes. This peculiar pharmacological profile of 7a suggests it binds to an allosteric site on SERT, and positions derivative 7a as a very useful tool to investigate SERT machinery. 相似文献
104.
Giorgio Ortar Luciano De Petrocellis Aniello Schiano Moriello Marco Allarà Enrico Morera Marianna Nalli Vincenzo Di Marzo 《Bioorganic & medicinal chemistry letters》2013,23(1):138-142
A series of twenty-five derivatives of tetrahydro-β-carbolines 1–3 was synthesized and assayed on FAAH and TRPV1 and TRPA1 channels. Four carbamates, that is, 5a,c,e, and 9b inhibited FAAH with significant potency and interacted also effectively with TRPV1 and TRPA1 nociceptive receptors, while ureas 7b,d,f, and 8a,b were endowed with specific submicromolar TRPV1 modulating activities. 相似文献
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Effective coordination is key to many situations that affect the well-being of two or more humans. Social coordination can be studied in coordination games between individuals located on networks of contacts. We study the behavior of humans in the laboratory when they play the Stag Hunt game – a game that has a risky but socially efficient equilibrium and an inefficient but safe equilibrium. We contrast behavior on a cliquish network to behavior on a random network. The cliquish network is highly clustered and resembles more closely to actual social networks than the random network. In contrast to simulations, we find that human players dynamics do not converge to the efficient outcome more often in the cliquish network than in the random network. Subjects do not use pure myopic best-reply as an individual update rule. Numerical simulations agree with laboratory results once we implement the actual individual updating rule that human subjects use in our laboratory experiments. 相似文献
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Ernesto Orme?o-Orrillo Marco A. Rogel Ligia Maria Oliveira Chueire James M. Tiedje Esperanza Martínez-Romero Mariangela Hungria 《Journal of bacteriology》2012,194(24):6927
The genome sequences of Burkholderia sp. strains CCGE1002 from Mexico and H160 from Brazil, isolated from legume nodules, are reported. Their gene contents in relation to plant-microbe interactions and xenobiotic degradation are discussed. 相似文献
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Andreagiovanni Reina Gabriele Valentini Cristian Fernández-Oto Marco Dorigo Vito Trianni 《PloS one》2015,10(10)
The engineering of large-scale decentralised systems requires sound methodologies to guarantee the attainment of the desired macroscopic system-level behaviour given the microscopic individual-level implementation. While a general-purpose methodology is currently out of reach, specific solutions can be given to broad classes of problems by means of well-conceived design patterns. We propose a design pattern for collective decision making grounded on experimental/theoretical studies of the nest-site selection behaviour observed in honeybee swarms (Apis mellifera). The way in which honeybee swarms arrive at consensus is fairly well-understood at the macroscopic level. We provide formal guidelines for the microscopic implementation of collective decisions to quantitatively match the macroscopic predictions. We discuss implementation strategies based on both homogeneous and heterogeneous multiagent systems, and we provide means to deal with spatial and topological factors that have a bearing on the micro-macro link. Finally, we exploit the design pattern in two case studies that showcase the viability of the approach. Besides engineering, such a design pattern can prove useful for a deeper understanding of decision making in natural systems thanks to the inclusion of individual heterogeneities and spatial factors, which are often disregarded in theoretical modelling. 相似文献
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Juan Antonio Surez‐Cuenca Rogelio Robledo‐Nolasco Marco Antonio Alcntara‐Melndez Luis Javier Díaz Hernndez Eduardo Vera‐Gmez Alejandro Hernndez‐Patricio Karla Susana Snchez‐Díaz Juan Ariel Buendía‐Gutirrez Alejandra Contreras‐Ramos Atzin Su Ruíz‐Hernndez Rebeca Prez‐Cabeza de Vaca Paul Mondragn‐Tern 《Journal of cellular and molecular medicine》2019,23(7):4844-4849