Novel BQCA- and TBPB-Derived M1 Receptor Hybrid Ligands: Orthosteric Carbachol Differentially Regulates Partial Agonism

Recently, investigations of the complex mechanisms of allostery have led to a deeper understanding of G protein-coupled receptor (GPCR) activation and signaling processes. In this context, muscarinic acetylcholine receptors (mAChRs) are highly relevant due to their exemplary role in the study of allosteric modulation. In this work, we compare and discuss two sets of putatively dualsteric ligands, which were designed to connect carbachol to different types of allosteric ligands. We chose derivatives of TBPB [1-(1′-(2-tolyl)-1,4′-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one] as M₁-selective putative bitopic ligands, and derivatives of benzyl quinolone carboxylic acid (BQCA) as an M₁ positive allosteric modulator, varying the distance between the allosteric and orthosteric building blocks. Luciferase protein complementation assays demonstrated that linker length must be carefully chosen to yield either agonist or antagonist behavior. These findings may help to design biased signaling and/or different extents of efficacy.     

An enhanced state estimation for linear parabolic PDE systems with mobile sensors

This paper studies an enhanced state estimation problem of distributed parameter processes modeled by a linear parabolic partial differential equation using mobile sensors. The proposed estimation scheme contains a state estimator and the guidance of mobile sensors, where the spatial domain is decomposed into multiple subdomains according to the number of sensors and each sensor is capable of moving within the respective subdomain. The state estimator is desired to make the state estimation error system exponentially stable while providing an performance bound. The mobile sensor guidance is used to enhance the transient performance of the error system. By the Lyapunov direct technique, an integrated design of state estimator and mobile sensor guidance laws is developed in the form of bilinear matrix inequalities (BMIs) to meet the desired design objectives. Moreover, to make the performance bound as small as possible, a suboptimal enhanced state estimation problem is formulated as a BMI optimization one, which can be solved via an iterative linear matrix inequality algorithm. Finally, numerical simulations are given to show the effectiveness of the proposed method.     

Effects of isothermal treatment parameters on the microstructure of semisolid alloys

Cold-rolled 6061 aluminium alloys are used to prepare semisolid billets by recrystallisation and partial melting. The effects of isothermal treatment parameters on the microstructures were investigated. The results indicated that the high isothermal holding temperature increases the experimental liquid fraction, average grain size and shape factor. A long isothermal holding time also increases the experimental liquid fraction and improves the spheroidisation degree of solid grains, but the average grain size also increases. Moreover, when the isothermal holding time at high temperature is increased, the size of intragranular liquid droplets increases, but their quantity decreases. The optimal isothermal holding temperature and time during semisolid isothermal treatment were 635°C and 5?–?10?min, respectively.     

合金组元过量焓与真空蒸馏气液相平衡的关联

基于Wilson方程，通过组元的摩尔体积和无限稀偏摩尔过量焓获得Wilson方程的相互作用参数，预测了Sn-X（X=Bi, Cd, Ga, Ge, In, Pb, 和 Sb）体系在5 Pa时的VLE（气-液平衡）相图。结果表明预测值与实验数据具有很好的一致性，在缺乏组元活度的情况下，该方法可以有效预测合金真空蒸馏的气液平衡，为粗金属的真空分离与提纯提供理论指导。     

基于局部放电法的矿用高压电缆信号去噪算法研究

干扰噪声直接影响局部放电法有效检测矿用高压电缆故障。基于局部放电法，综合采用理论计算、仿真实验、现场试验的方法，对比分析了短时傅里叶变换和傅里叶分析去噪法的原理和优缺点，提出了一种矿用高压电缆的局部放电去噪算法——小波阈值去噪法，同时，选择了合理的阈值函数和去噪流程。基于此，采用白噪声和连续周期信号作为高压电缆的干扰噪声，进行了模拟仿真实验。结果表明，小波阈值去噪法可有效抑制白噪声，其中，Db2小波性能和去噪效果最好；同时，现场试验结果显示，去噪后信噪比得到了显著增加，验证了小波阈值去噪法的合理性和可靠性。     

Application of thermophilic temperatures,low hydraulic retention times and high recycling of de-gassed effluent for higher biohydrogen production

This study investigated the external operational factors that would reduce the thermodynamic constrains preventing the simultaneous achievement of high hydrogen productivities (HPs) and hydrogen yields (HYs) in the bioreactor. At hydraulic retention time (HRT) of 1, the maximum HPs and HYs achieved was 35 L H₂/h and 3.91 mol H₂/mol glucose, respectively. At this stage, the bacterial granules occupied approximately 75% of the bioreactor and consisted of the settled biomass density of 40.6 g/L (settled granule bed height = 13.8 cm). The formation of bacterial granules improved the bioreactor performance and resulted in higher substrate conversion efficiency (95%), nutrient influent (7.5 L/h) and de-gassed effluent recycle rates (3.5 L/min). In conclusion, this study demonstrated that high nutrient influent and high de-gassed effluent recycle rates reduced the thermodynamic constrains preventing the achievement of higher H₂ productivities in the bioreactor system.     

In situ monitoring of the biocatalysed partial hydrolysis of cocoa butter and palm oil fraction

Partial glycerides are widely used ingredients in confectionery products that can be produced from natural fats. In a biocatalytic partial hydrolysis of cocoa butter and palm oil fractions, a product mixture containing 1.5% monoglycerides and 5.5% diglycerides intended for the use in confectionery products was created. This study is a proof of principle that shows the feasibility of monitoring the biocatalytic partial hydrolysis of these two natural fats in situ with ATR-FTIR spectroscopy. An economic approach was utilised for calibration since partial glyceride calibration standards are costly and poorly available. The released compounds were quantified by means of chemometric modelling, and the model was validated with gas chromatography. Resulting root mean square errors were in the low per cent range. Additionally, the results indicate that distinction of the released free fatty acids is possible with ATR-FTIR spectroscopy.     

Proposed network structures and combined adaptive algorithms for electrocardiogram signal denoising

An electrocardiogram (ECG) signal is a record of the electrical activities of heart muscle and is used clinically to diagnose heart diseases. An ECG signal should be presented as clear as possible to support accurate decisions made by doctors. This article proposes different combinations of combined adaptive algorithms to derive different noise-cancelling structures to remove (denoise) different kinds of noise from ECG signals. The algorithms are applied to the following types of noise: power line interference, baseline wander, electrode motion artifact, and muscle artifacts. Moreover, the results of the suggested models and algorithms are compared with those of conventional denoising tools such as the discrete wavelet transform, an adaptive filter, and a multilayer neural network (NN) to ensure the superiority of the proposed combined structures and algorithms. Furthermore, the hybrid concept is based on dual, triple, and quadruple combinations of well-known algorithms that derive adaptive filters, such as the least mean squares, normalized least mean squares and recursive least squares algorithms. The combinations are formulated based on partial update, variable step-size (VSS), and second iterative VSS algorithms, which are considered in different combinations. In addition, biased NN and unbiased linear neural network (ULNN) structures are considered. The performance of the different structures and related algorithms are evaluated by measuring the post-signal-to-noise ratio, mean square error, and percentage root mean square difference.     

某型号收割机割刀机构及其传动部件惯性力平衡的研究

针对某型号收割机割刀执行及传动机构的实际工作中的性能需求,在完成机构惯性力最小的基础上,考虑实际工作情况权衡各方面因素的部分平衡的最优方案,最终得出了最优的设计参数,其研究方案可为类似杆机构惯性力平衡问题提供有益的参考。     

Polarity Effect and Electromagnetic Radiation of Partial Discharge Accompanying Growth of Electrical Tree

We have investigated the characteristics of radiated electromagnetic (EM) waves from positive and negative partial discharges (PD) in epoxy resin and cross‐linked polyethylene. We found that there is a correlation among the EM level from PD, the positive PD current, and electrical trees. Therefore, the growth of an electrical tree produces a lot of positive PD. We have also investigated the characteristics of the frequency region of EM waves from PD in air, insulating oil, and liquid epoxy in addition to the above insulators. EM waves were detected in the frequency region of 40 MHz to 300 MHz from positive and negative PD in epoxy resin and cross‐linked polyethylene. EM waves were also detected in the frequency region of 40 MHz to 150 MHz from positive and negative PD in air. In the case of insulating oil and liquid epoxy, EM waves were detected in the frequency regions of 40 MHz to 150 MHz from positive PD, and 40 MHz to 250 MHz from negative PD. The frequency region differed depending on the material and the discharge polarity. Our investigation indicates that the cause is differences in electric field strength at the time of PD occurrence.