Design, synthesis and structure-activity relationship of novel 1,2,4-triazolopyrimidin-5-one derivatives targeting GABA and Na1.2 with antiepileptic activity.

A novel class of 7-phenyl-[1,2,4]triazol-5(4H)-one derivatives was designed and synthesized, and their in vivo anticonvulsant activities were evaluated using subcutaneous pentylenetetrazole (Sc-PTZ) and maximal electroshock (MES) tests. Compounds 3u, 4f and 4k exhibited significant anticonvulsant activities in the Sc-PTZ model with ED values of 23.7, 17.

Microbial synthesis of m-tyrosine via whole-cell biocatalysis.

Meta-tyrosine (m-tyrosine), a nonproteinogenic amino acid, has shown significant potential for applications as an herbicide in agriculture and for various medical uses. However, the natural abundance of m-tyrosine is very low, limiting its widespread use. In this study, we successfully achieved microbial production of m-tyrosine by establishing the in vivo enzyme activity of phenylalanine 3-hydroxylase (PacX from Streptomyces coeruleoribudus) in E.

Principles of visual cortex excitatory microcircuit organization.

Synapse-specific connectivity and dynamics determine microcircuit function but are challenging to explore with classic paired recordings due to their low throughput. We therefore implemented optomapping, a ∼100-fold faster two-photon optogenetic method. In mouse primary visual cortex (V1), we optomapped 30,454 candidate inputs to reveal 1,790 excitatory inputs to pyramidal, basket, and Martinotti cells.

Altered cortical activation patterns in post-stroke patients during walking with two-channel functional electrical stimulation: a functional near-infrared spectroscopy observational study.

Restoration of independent walking ability is the primary objective of stroke rehabilitation; however, not all patients achieve this goal due to diverse impairments in the paretic lower limb and compensatory mechanisms that lead to an asymmetrical and mechanically inefficient gait. This investigation aimed to examine alterations in cortical activation in post-stroke patients while walking with a wearable two-channel functional electrical stimulation (FES) in comparison to walking without FES. This observational study was conducted to discern distinct activation patterns in 19 stroke patients during sessions with and without FES, while using functional near-infrared spectroscopy (fNIRS) to monitor changes in blood oxygen levels.

Gas sensing by long-wavelength and long-afterglow pectin/melamine-formaldehyde aerogel via resonance energy transfer.

The exploration of pure organic ultra-long room temperature phosphorescence (RTP) materials has emerged as a research hotspot in recent years. Herein, a simple strategy for fabricating long-afterglow polymer aerogels with three-dimensional ordered structures and environmental monitoring capabilities is proposed. Based on the non-covalent interactions between pectin (PC) and melamine formaldehyde (MF), a composite aerogel (PCMF@phenanthrene) (PCMF@PA) doped with phosphorescent organic small molecules was constructed.