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1.
Mar Drugs ; 21(7)2023 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-37504932

RESUMO

In this perspective, we showcase the benefits of continuous flow chemistry and photochemistry and how these valuable tools have contributed to the synthesis of organic scaffolds from the marine environment. These technologies have not only facilitated previously described synthetic pathways, but also opened new opportunities in the preparation of novel organic molecules with remarkable pharmacological properties which can be used in drug discovery programs.


Assuntos
Descoberta de Drogas , Tecnologia , Química Farmacêutica
2.
Transl Psychiatry ; 11(1): 324, 2021 05 27.
Artigo em Inglês | MEDLINE | ID: mdl-34045447

RESUMO

The real-time live fluorescent monitoring of surface AMPA receptors (AMPARs) could open new opportunities for drug discovery and phenotypic screening concerning neuropsychiatric disorders. We have developed FORTIS, a tool based on pH sensitivity capable of detecting subtle changes in surface AMPARs at a neuronal population level. The expression of SEP-GluA1 or pHuji-GluA1 recombinant AMPAR subunits in mammalian neurons cultured in 96-well plates enables surface AMPARs to be monitored with a microplate reader. Thus, FORTIS can register rapid changes in surface AMPARs induced by drugs or genetic modifications without having to rely on conventional electrophysiology or imaging. By combining FORTIS with pharmacological manipulations, basal surface AMPARs, and plasticity-like changes can be monitored. We expect that employing FORTIS to screen for changes in surface AMPARs will accelerate both neuroscience research and drug discovery.


Assuntos
Neurônios , Receptores de AMPA , Animais , Células Cultivadas , Fluorescência , Humanos , Concentração de Íons de Hidrogênio , Receptores de AMPA/genética
3.
Materials (Basel) ; 9(11)2016 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-28774026

RESUMO

Nowadays, the use of micropiles has undergone a great development. In general, they are made with cement grout, reinforced with steel tubing. In Spain, these grouts are prepared using OPC, although the standards do not forbid the use of other cements, like sustainable ones. Micropiles are in contact with soils and groundwater, in which the presence of sulphates is common. Their deleterious effects firstly affect to the microstructure. Then, the aim of this research is to study the effects of sulphate attack in the microstructure of micropiles grouts, prepared with OPC, fly ash and slag commercial cements, compared to their behaviour when they are exposed to an optimum hardening condition. The microstructure evolution has been studied with the non-destructive impedance spectroscopy technique, which has never been used for detecting the effects of sulphate attack when slag and fly ash cements are used. Its results have been contrasted with mercury intrusion porosimetry and "Wenner" resistivity ones. The 28-day compressive strength of grouts has been also determined. The results of microstructure characterization techniques are in agreement, although impedance spectroscopy is the most sensitive for following the changes in the porous network of grouts. The results showed that micropiles made using fly ash and slag cements could have a good performance in contact with aggressive sodium sulphate media, even better than OPC ones.

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