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Ionotropic γ-aminobutyric acid (GABA) receptors (iGABARs) are validated targets of drugs and insecticides. Our previous studies showed that the competitive antagonists of insect iGABARs exhibit insecticidal activities and that the 3-isothiazolol scaffold is used as a lead for developing novel iGABAR antagonists. Here, we designed a novel series of 4-aryl-5-(4-pyridinyl)-3-isothiazolol (4-API) analogs that have various aromatic substituents at the 4-position. Two-electrode voltage clamp experiments showed that all synthesized 4-APIs exhibited antagonistic activity against

Although the Xinzhai period (1850–1750 cal bce) has been widely regarded as a critical time for the development of urbanization in China, little is known about the labour and social organization of the time. In this paper, archaeobotanical assemblages have been used to explore evidence of crop processing and they have provided further insights into the organization of labour and society at the Xinzhai site on the Central Plain of China. This is the first case study linking agricultural activities and social organization in the Xinzhai period. By discussing macro-botanical and phytolith results together, we conclude that the hulled cereals Setaria italica (foxtail millet), Panicum miliaceum (common or broomcorn millet) and Oryza sativa (rice), and the free-threshing pulse Glycine max (soybean) were all partly processed before storage to reduce labour demand in the harvest period. Since these summer-sown crops are all harvested in autumn, the practice of partial processing might imply that less labour was needed before storage. Thus, the labour for crop processing appears to have been organized on the basis of small production units such as households. This pattern is different from the communal bulk processing of crops before storage by the contemporary inhabitants of Dongzhao. Different patterns of social organization in various settlements in the Xinzhai period can thus be suggested. This conclusion contributes to a comprehensive understanding of the social development of communities living on the Central Plain and indicates that a steady increase in social complexity was very likely in the period before urbanization.

Fluxametamide is a completely novel and the first isoxazoline insecticide used to control agricultural pests and has high insecticidal properties. To expand its usage in the paddy field, its potential toxicological effects on fish are necessary to make clear. In this study, the acute toxicity, bioconcentration and elimination of fluxametamide to zebrafish Danio rerio, and the action mode of it on the heteromeric Drα1β2Sγ2 and Drα1β2S GABA receptor was respectively determined by HPLC and two-electrode voltage clamp technique. Fluxametamide exhibited high toxicity to D. rerio, whereas slightly inhibited the GABA-stimulated current of Drα1β2Sγ2 or Drα1β2S. It showed high bioconcentration level in D. rerio at 0.0314 mg L

Currently a two-step designing method of sequential neutronic physics and Stirling physical analysis was used for a Miniature Integrated nuclear Reactor design with gravity independent Autonomous Circulation (ACMIR). It was proposed in this article to optimize the intermediate/transitive variables of dead volume and heat exchange area/dead volume ratio as much as possible in the first step so that the system objectives in the second step can be better achieved. The ACMIR core was modified from using rod typed fuels to using plate typed fuels, making use of the plated core’s advantages of easy compression of coolant flow channel while maintaining large heat transfer area. As applied to a 40kWt cooperative dual Stirling power system design of ACMIR, the output power and efficiency index of the system had been significantly improved from 981W to 6395W (each Stirling), with efficiency from 7.4% to 26.6%.

Broflanilide, a novel insecticide, is classified as a negative allosteric modulator (NAM) of insect γ-aminobutyric acid (GABA) receptors (GABARs) as desmethyl-broflanilide (DMBF) allosterically inhibits the GABA-induced responses. The G277M mutation of the Drosophila melanogaster GABAR subunit has been reported to abolish the inhibitory activity of DMBF. The binding mode of DMBF in insect GABARs needs to be clarified to understand the underlying mechanism of this mutation and to develop novel, efficient NAMs of insect GABARs. Here, we found that a hydrogen bond formed between DMBF and G277 of the D. melanogaster GABAR model might be the key interaction for the antagonism of DMBF by in silico simulations. The volume increase induced by the G277M mutation blocks the entrance of the binding pocket, making it difficult for DMBF to enter the binding pocket and thereby decreasing its activity. The following virtual screening and bioassay results identified a novel NAM candidate of insect GABARs. Overall, we reported a possible binding mode of DMBF in insect GABARs and proposed the insensitivity mechanism of the G277M mutant GABAR to DMBF using molecular simulations. The identified NAM candidates might provide more alternatives or potentials for the design of GABAR-targeting insecticides.

Photopharmacology provides superior temporal and spatial resolution for the study of biological functions of γ-aminobutyric acid receptors (GABARs), and photopharmacology based on GABARs has significantly advanced the research of neurons and cells. Herein, we reported the azobenzene-phenylpyrazole (

The ionotropic γ-aminobutyric acid (GABA) receptor (iGABAR) is an important target for insecticides and parasiticides. Our previous studies showed that competitive antagonists (CAs) of insect iGABARs have the potential to be used for developing novel insecticides and that the structural modification of gabazine (a representative CA of mammalian iGABARs) could lead to the identification of novel CAs of insect iGABARs.In the present study, a novel series of 1,3-di- and 1,3,5-trisubstituted 1,6-dihydro-6-iminopyridazines (DIPs) was designed using a versatile strategy and synthesized using facile methods. Electrophysiological studies showed that several target DIPs (30 μM) exhibited excellent antagonistic activities against common cutworm and housefly iGABARs consisting of RDL subunits. The ICThis systematic study indicated that the presence of a carboxyl side chain shorter by one methylene than that of gabazine at the 1-position of the pyridazine ring is effective for maintaining the stable binding of these DIPs in insect iGABARs. Our study provides important information for the design of novel insect iGABAR CAs. © 2022 Society of Chemical Industry.

To safely and efficiently change lanes among human drivers, autonomous vehicles (AVs) should make human-like decisions and seamlessly cooperate with surrounding vehicles. Both overaggressive and over-conservative cut-in maneuvers will have adverse effects on traffic efficiency and safety. However, it is still not entirely clear how much influence of the AV’s cut-in behavior would lay on the surrounding drivers in urban traffic. To investigate this question, we design a series of driving scenarios and analyze the impact of different cut-in maneuvers performed by the human-like AV on the surrounding drivers’ comfort. Ten volunteer drivers participate in our experiment and take a series of trials in a driving simulator. The experimental results demonstrate that the relative distance between the AV and the target car on the adjacent lane has a more significant effect on the surrounding drivers’ comfort than the relative speed does. In addition, different parameters should be considered with different cut-in scenarios. This conclusion could provide practical support to make a friendly cut-in decision for the AVs.

Objective. To analyze the diagnostic value of luteinizing hormone (LH) peak value of the gonadotropin-releasing hormone (GnRH) stimulation test for girls with precocious puberty and its correlation with body mass index (BMI). Methods. A total of 230 girls with precocious puberty who came to our hospital for testing from June 2019 to June 2021 were selected and divided into a true group ( n = 130 ) and sham group ( n = 100 ) according to the results of the GnRH stimulation test. According to the BMI, the true group was further divided into a normal group (48 cases), overweight group (43 cases), and obese group (39 cases). The GnRH stimulation test was performed on all subjects, and the basal value and peak value of LH and the basal value and peak value of follicle-stimulating hormone (FSH) were recorded. The general data and serological indexes of the true group and the sham group were compared. Indicators of the GnRH stimulation test, breast stage, bone age, BMI, uterine volume, ovarian volume, and serological indicators (leptin, sex hormone-binding protein (SHBG), and adiponectin (APN)) were compared among the normal group, the overweight group, and the obese group. Results. There were no significant differences in age and breast stage between the true group and the sham group ( P > 0.05 ). There were statistically significant differences in bone age, BMI, uterine volume, and ovarian volume between the two groups ( P < 0.05 ). The LH base value, LH peak value, FSH base value, and FSH peak value in the true group were higher than those in the sham group, and the differences were statistically significant ( P < 0.05 ). ROC curve analysis showed that the AUC of LH peak value in diagnosing girls with precocious puberty was 0.973, which was higher than 0.895, 0.875, and 0.912 of LH base value, FSH base value, and FSH peak value, respectively. There were statistically significant differences in LH base value, LH peak value, FSH base value, breast development stage, bone age, BMI, SHBG, leptin, and APN among the normal group, overweight group, and obese group ( P < 0.05 ), but there were no significant differences in FSH peak value, uterine volume, and ovarian volume among the three groups ( P > 0.05 ). There was a negative correlation between BMI, LH peak value, and FSH base value ( P < 0.05 ), but there was no significant correlation between BMI and FSH peak value ( P > 0.05 ). Conclusion. The LH peak value of the GnRH stimulation test has high diagnostic value for girls with precocious puberty, and BMI is negatively correlated with the LH peak value of CPP children.

Broflanilide, a novel insecticide, is classified as a negative allosteric modulator (NAM) of insect γ-aminobutyric acid (GABA) receptors (GABARs) as desmethyl-broflanilide (DMBF) allosterically inhibits the GABA-induced responses. The G277M mutation of the

Artificial neural networks (ANN) based on learning the features of the entire measured gamma energy spectrum has been used for radioisotope identification and proved promising especially for gamma-ray spectroscopy with low energy resolution. The implementation of ANN method, however, requires tedious experimental measurement process in generation of training data for various radioisotopes. In this work, we propose an ANN-based radioisotope identification method with simulated training data. Gamma energy spectra of 27 different radioisotopes were generated with Monte Carlo simulation. A detector energy response model was proposed to match the energy spectra generated from simulation and measured from experiment, thus “pseudo” measured energy spectra of various radioisotopes transformed from simulation can be used for ANN training, which eliminates the tedious experimental measurement process for training data generation. To reduce the complexity of the training process, the principal component analysis (PCA) method was used for dimension reduction of the input energy spectra in ANN and the channel number of the energy spectra was reduced from 2000 to 50. The trained ANN was further used to identify experimentally measured gamma energy spectra of various radioisotopes including 60Co., 137CS., 18F, 131I, 226Ra and 232Th at 103, 104 and 105 count levels. In single isotope identification test, with increased count level, higher correct identification rate is achieved and at 105 count level, all the isotopes are correctly identified for all the samples. In mixed isotope identification test, at 105 count level, all the radioisotope combinations can be identified with a correct identification rate larger than 98%, which demonstrates the feasibility and accuracy of the ANN method. To conclude, the proposed ANN method with simulated training data features good radioisotope identification capability with greatly simplified training data generation process and is feasible for gamma spectroscopy with relatively poor energy resolution.

Laser technology and laser system has more and more important implication in spacecraft engineering. But different from ground environments, space laser system will encounter space environments include vacuum, extreme temperature and thermal cycling, vibration, space radiation environments such as electron, proton, heavy ions, ultraviolet, contamination, and so on. These space environments may have damage or threaten to the space laser system, especially to their optical devices. In this paper, space environments and effects are introduced firstly, and then the influence of space environments such as vacuum, temperature, energetic particles, contamination and vibration on space laser system are analyzed. At last, some advices are proposed to improve the reliability of space laser system are given.

The influence of Eu3+ doping on the structural properties of SnO-containing phosphate glass has been investigated by X-ray photoelectron spectroscopy (XPS) and 31P nuclear magnetic resonance (NMR) spectroscopy. Oxygen 1s XPS data indicates that the Eu3+ doping results in a higher concentration of non-bridging oxygens in the glass matrix, whereas 31P NMR shows an increase in the terminal phosphate chain tetrahedral units, i.e. the amount of Q1 sites with only one bridging oxygen. Accordingly, both techniques agree with a depolymerization effect induced by the Eu3+ ions. Further, XPS reveals that together with the Eu3+ doping, the presence of Sn4+ is supported while the presence of Eu2+ is also indicated. The structural changes are then indicated to be a consequence of redox chemistry between Sn2+ and Eu3+ promoting a transition of tin from Sn2+ with a role as network former to Sn4+ acting as network modifier in the glass system.

During the operation of industrial gasifier, the concentrations of CO2 and H2O in gasification media vary with the change of stages, causing the gasification process being affected accordingly. Therefore, dividing the gasification process into different stages to study the effect of multi-stage switching atmosphere is significant. The conversion rate, reaction characteristics and reaction process for the gasification of Xiaolongtan (XLT) coal char in different atmospheres (CO2/H2O/N2) switching in the early, middle and late reaction stages were investigated using thermo-gravimetric analysis (TGA). The results indicated that the average reaction rate of coal char with H2O was approximately 3 times that of CO2. Increasing H2O concentration improved the reaction and conversion rate of coal char, which was the most obvious in the early stage. With the H2O concentration increasing from 0 to 95%, the increment of conversion rate in the early, middle, and late stages were 7.13%, 4.40%, and 3.92%, respectively. Thus, considering the problem of H2O corrosion in practical production, the H2O concentration could be appropriately increased in the early stage to improve efficiency. Compared with the random pore model, the shrinking core model fitted the gasification process of coal char better in a highly reactive 95% H2O/5% N2 atmosphere.

BACKGROUND Previous studies indicated that constitutive over-expression of cytochrome P450 CYP6B7 was involved in fenvalerate resistance in Helicoverpa armigera. In this study, the CYP6B7 gene from H. armigera (namely HaCYP6B7), was heterologously expressed in Pichia pastoris GS115. A vector pPICZA-HaCYP6B7 was constructed and transformed into P. pastoris GS115, the transformant of pPICZA-HaCYP6B7-GS115 was then cultured and induced by 1% (v/v) methanol and the heterologous expression of HaCYP6B7 protein in P. pastoris was confirmed by SDS-PAGE and western blot. RESULTS Microsomes containing the expressed HaCYP6B7 showed activities against model substrate p-nitroanisole and 7-ethoxycoumarin, with p-nitroanisole O-demethylation (PNOD) and 7-ethoxycoumarin O-deethylation (ECOD) activities of 15.66- and 4.75-fold of the control, respectively. Moreover, it showed degradation activities against the insecticides bifenthrin, fenvalerate and chlorpyrifos, with clearance activities of 6.88-, 1.49- and 2.27-fold of the control, respectively. The interactions of HaCYP6B7 with insecticides were further confirmed by molecular docking in silico with binding scores of 5.450, 5.295 and 2.197 between putative HaCYP6B7 protein and bifenthrin, fenvalerate and chlorpyrifos, respectively. CONCLUSION The results of present study provided more direct and important evidence on the role of HaCYP6B7 conferring pyrethroid resistance in H. armigera. © 2017 Society of Chemical Industry

The energy structure and carbon emissions become more and more important for the sustain-able development of a regional construction. The purpose of this paper is to apply the energy-carbon flow charts to analyze the energy use and carbon emissions in a high-tech industrial park. The characteristics of the charts applied in a park are very different from that of a coun-try, a province or a product. The authors propose a preliminary drawing frame to guide the effective application of the chart for a park. The frame presents the steps and focus of the drafting work. A case application is also introduced to illustrate the applicability of the frame to practical problems, the results are very helpful to optimize the energy structure and reduce the carbon emissions.

Previous bone collagen stable isotope analyses conducted on faunal remains from archaeological sites from the Late Neolithic (Longshan) to the Bronze Age (Xia dynasty) in the Central Plains of China have revealed that C4 plants – most probably cultivated millets – constituted a major part of cattle fodder and also contributed to sheep diet, although to a lower extent. In the present study, this difference between cattle and sheep diet management was investigated at the Xinzhai site (occupation phases 2 and 3, ca. 1800–1705 cal. BC), focusing on the seasonal scale through sequential δ13C and δ18O analysis in tooth enamel. This primary objective related to the reconstruction of Bronze Age husbandry practices required an effort in interpreting δ18O sequences recovered from cattle and sheep molars: potential difficulty in the identification of the seasonal cycle could rise, inherent to a specific climatic regime. This region of China is nowadays under the influence of the East-Asian summer monsoon, whose strength undergoes variability on the annual scale, but also did in the past on decadal to century scales. At Xinzhai, all sheep teeth and one deer tooth delivered δ18O sequences comparable to previously published sequences from locations were rainfall δ18O is temperature controlled (no monsoon influence), revealing minimal influence of the summer monsoon over these animals' lifetime. Some cattle teeth delivered sequences with bimodal distribution of δ18O values on the annual scale, potentially reflecting the influence of a summer monsoon. Such variability among domestic stock could relate to interannual/interdecadal variability in the monsoon intensity at the site location, or to differences in herding practices between sheep and cattle. Concomitant analysis of δ13C values in deer molars confirmed a surrounding wild environment dominated by C3 plants throughout the year, supporting the idea that a C4 signal in cattle and sheep diets resulted from feeding practices involving cultivated millets. Furthermore, sheep had access to millet in late summer time while cattle were constantly foddered throughout the year, to a very high extent. Given the annual growth cycle of millet, with late summer maturity, a year round provisioning to cattle would suppose constitution of fodder. Constant provisioning could also have required cattle to be kept by the settlement all year round, inducing less investment in cattle herding, but in return, a necessarily important input to sustain cattle diet requirements at the daily scale. This could in fine be connected to the privileged status for cattle in social or ritual related activities at Xinzhai.

A series of giant tris(heteroaryl)methanes are easily assembled by one-pot three-component synthesis by simple reflux in ethanol without catalyst or additives. Diversely substituted indoles (Ar1) react with quinoline aldehydes, quinolone aldehydes, chromone aldehydes, and fluorene aldehydes (Ar2CHO) and coumarins (Ar3) in 1:1:1 ratio to form the corresponding tris(heteroaryl)methanes (Ar1Ar2Ar3)CH along with (Ar1Ar1Ar2)CH triads. A series of new 2:1 triads were also synthesized by coupling substituted indoles with Ar2CHO. The coupling reactions could also be carried out in water (at circa 80 °C) but with chemoselectivity favoring (Ar1Ar1Ar2)CH over (Ar1Ar2Ar3)CH. The molecular structure of a representative (Ar1Ar2Ar3)CH triad was confirmed by X-ray analysis. Model tris(heteroaryl/aryl)methylium salts were generated by reaction with DDQ/HPF6 and studied by NMR and by DFT and GIAO-DFT. Fil: Abonia, Rodrigo. Universidad del Valle; Colombia Fil: Gutiérrez, Luisa F.. University Of North Florida; Estados Unidos. Universidad del Valle; Colombia Fil: Insuasty, Braulio. Universidad del Valle; Colombia Fil: Quiroga, Jairo. Universidad del Valle; Colombia Fil: Laali, Kenneth K.. University Of North Florida; Estados Unidos Fil: Zhao, Chunqing. University Of North Florida; Estados Unidos Fil: Borosky, Gabriela Leonor. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones en Físico-química de Córdoba. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Instituto de Investigaciones en Físico-química de Córdoba; Argentina Fil: Horwitz, Samantha M.. Kent State University; Estados Unidos Fil: Bunge, Scott D.. Kent State University; Estados Unidos

Indium (In) nanowires were synthesized on self-ordered hexagonal porous anodic aluminum oxide (AAO) template by electrodepositing In 2 (SO 4 ) 3 in the pores of AAO template. In nanowires obtained are very straight and have uniform-diameter about 45 nm. The ion emission properties of In nanowires were investigated. The onset field of ion emission is observed at about 1.6 V/ μ m, which is much lower than that for a conventional liquid metal ion source (LMIS) consisting of a sharpened metal needle. The I - E curves follow nearly a linear relationship with a slope of about 6.0 μ A/(V/ μ m), indicating a conventional ion emission phenomenon in LMIS. It is proposed that the unique geometry of nanowires may be the reason for their advantages in LMIS.

Multi-wall carbon nanotubes are systematically explored for the first time as a means to obtain an enhanced ultraviolet (UV) transparency in melt-quenched phosphate glasses. An optical characterization is carried out by UV/Vis transmission and photoluminescence spectroscopy including time-resolved measurements. 31P nuclear magnetic resonance, Raman microspectroscopy, differential scanning calorimetry and X-ray photoelectron spectroscopy are employed to further investigate the source of the improved UV light transmission. The data suggest that the formation of P–O–C bonds is connected to the enhanced UV transparency. A model is presented accounting for the incorporation of carbon into the phosphate network facilitated by the creation of intermediate reactive oxygen species.

The Co-60 radiation ground simulation test was conducted on the Mechanical property of polyimide film, thermo gravimetric and XPS was used to analyze the evolution mechanism of polyimide film in different dosages. It was found that the mechanical properties such as tensile force, tensile strength and rupture elongation of polyimide film in gamma ray radiation increase firstly and then exponent decrease. The corresponding initial decomposition temperature of the gamma ray-radiated polyimide film changed from 570°C to 590°C for weight-loss ratio of 2%. From XPS analysis, it can be found that there were rupture and crosslink of chemical bond in polyimide film. In early stage of gamma ray radiation, the rupture of C-N bond and following crosslink is for the increase of mechanical properties of polyimide film, and as the increase of radiation, the rupture of C=O and –N(CO) bond, formation of C-N bond, release of N was for the decrease of mechanical properties of polyimide films.

The deuterium lamp was used as simulation source to study the Mechanical property of polyimide film in space far ultraviolet environment, thermo gravimetric and XPS was used to analyze the evolution mechanism of polyimide film in different exposures. It was found that the mechanical properties such as tensile strength and rupture elongation of polyimide film decrease firstly and then exponent increase until to stable. From XPS analysis, it can be found that there were rupture and crosslink of chemical bond in polyimide film. In early stage of far ultraviolet radiation, the rupture of C-N, C=O, C-O, C-C bond is for the decrease of mechanical properties of polyimide film, and as the increase of far ultraviolet exposure, the release of N, and formation of C-N bond is for the increase of mechanical properties of polyimide film.

Since the moon landings of the 1970’s, researchers have believed that “horizon glow”(HG) observed on the moon are formed by the scattering of sunlight by the electrostatic lofted dust. In order to analyze the characteristics of dust lofting, researchers have proposed different suspension and lofting models. However, due to the neglect of adhesion force, it is impossible to accurately solve the accelerated separation process and the 3D trajectories of lofting particles. Therefore, we regard the dust lofting phenomenon as an electrostatic emission process with adhesion constraint, and propose a new mechanical model of lunar dust lofting, which is suitable for accelerated separation process and ballistic projection process. Using this model, we calculated the conditions of dust lofting, the maximum height, the time period, the characteristics of accelerated separation and the 3D trajectories of particles. The results of calculation and correlation analysis show that: 1) The changing of contact state caused by external factors may be one of the necessary conditions for dust lofting; 2) The maximum lofting height of submicron and micron particles varies from several kilometers to more than 300 ​km; 3) Lunar dust will be accelerated to a high speed in a very short time, in condition of that, it may be difficult for the particles to suspend at the force balanced height; 4) The trajectory of a dust particle is affected by the lofting sequence and the initial position, the boundary of lofting trajectories seems similar to the HG sketch by the astronaut in Apollo 17 mission; 5) Compared with the macroscopic plasma sheath electric field, the microscopic particles are more sensitive to the charging voltage of the lunar surface in the lofting process.

The proposed neutron spectrometer makes use of BLP scintillator to acquire spectrum from those coincidence neutron events who lose most energy through elastic collision(s) and end with a B(n, α)Li reaction by coincidence detection. This technique facilitates a compact, simple, and performance acceptable neutron spectrometer, potential to build portable ones. With a BLP cube equivalent to 3.25cm thick, it achieves an energy range up to 10MeV, with energy resolution 8% to fission sources. The thickness of the detector makes high impact on coincidence detection efficiency, but does not much influence the spectrum resolution.