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Thienorphine induces analgesia by binding κ -and δ-, or by partially binding μ-opioid receptor,thus further regulating cAMP-PKA activity

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中国药理学与毒理学杂志 2018年第9期32卷 721-722页

作者： zhou pei-lan LI Yu-lei YONG Zheng SU Rui-bin GONG Ze-hui State Key Laboratory of Toxicology and Medical Countermeasures Beijing Key Laboratory of Neuropsychopharmacology Beijing Institute of Pharmacology and Toxicology Beijing 100850 China

OBJECTIVE Thienorphine,a new oripavine derivative,has shown to possess stronger antinociceptive effects and better oral bioavailability compared to buprenorphine.The present study examines the effect of thienorphine on c AMP-dependent protein kinase A(PKA) activity in CHO cells expressing μ-,κ-,δ-and ORL1 receptors.In addition,we further examined its analgesic effect in vivo.METHODS The effect of thienorphine on cA MP-dependent PKA redistribution and cA MP inhibition were analyzed in CHO-PKAcatEGFP cells.PKA redistribution assays in CHO-PKAcatEGFP cells stably expressing μ-,κ-,δ-and ORL1 receptors were analyzed by high-throughput screening system to elucidate the efficacy of agonists or antagonists on opioid receptors.Moroever,the antinociceptive effects of thienorphine in vivo were examined using hot plate test.RESULTS Briefly,the maximum inhibition of thienorphine on PKA activity was about 36%,100%,100%and 12% in CHO-μ/κ/δ/ORL1-PKAcatE GFP cel s,respectively.In addition,thienorphine concentrationdependently inhibited the PKA activity with EC50 value of(22.7±18.1) nmol·L^(-1) in CHO-κ-PKAcatE GFP cels and(12.4±7.7) nmol·L^(-1) in CHO-δ-PKAcatE GFP cells.Thienorphine induced approximately 50%antinociceptive effect in mice lacking μ receptors compared to their wild-type controls(P<0.05).Also,the κ and δ selective antagonist nor-binaltorphimine,naltrindole decreased approximately 50%-60% in % MPE of theinorphine in μ-KO mice,respectively.The ORL1 receptor selective antagonist J113397 had no effect in %MPE of theinorphine in μ-KO mice.CONCLUSION Thienorphine induces analgesia through bindingκ-and δ-,or by partially binding μ-opioid receptor,thus further regulating the cAMP-PKA activity.Therefore,thienorphine may be used in acute or chronic pain with minimal addictive potential.

关键词： thienorphine opioid receptor analgesia cAMP protein kinase A

S4A-5 Screening ofμOpioid Receptor-Interacting Proteins and Effects of ABIN-1 on Receptor Function

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神经药理学报 2018年第4期8卷 67-69页

作者： zhou pei-lan JIANG Jie-bing YAN Hui LI Yu-lei ZHAO Jun-ru WANG Xiao GONG Ze-hui SU Rui-bin State Key Laboratory of Toxicology and Medical Countermeasures Beijing Key Laboratory of NeuropsychopharmacologyBeijing Institute of Pharmacology and ToxicologyBeijingChina

Aim:To determine the proteins that interact with the carboxyl-terminal of theμopioid receptor(MOR-C)after chronic morphine exposure.Methods:The brain cDNA library of chronic morphine treatment rats was screened using rat MOR-C to investigate the regulator of opioids dependence in the present study.The brain cDNA library from chronic morphine-dependent rats was constructed using the SMART(Switching Mechanism At 5′end of RNA Transcript)technique.Bacterial two-hybrid system was used to screening the rat MOR-C interacting proteins from the cDNA library.RT-qPCR and immunoblotting were used to determine the variation of MOR-C interacting proteins in rat brain after chronic morphine treatment.Column overlay assays,immunocytochemistry and coimmunoprecipitation were used to demonstrate the interaction of MOR-C and p75NTR-associated cell death executor(NADE)or A20-binding inhibitor of nuclear factor kB(ABIN-1).Results:21 positive proteins,including 19 known proteins were screened to interact with rat MOR-C.Expression of several of these proteins was altered in specific rat brain regions after chronic morphine treatment.Among these proteins,ABIN-1 and NADE were confirmed to interact with rat MOR-C by in vitro proteinprotein binding and coimmunoprecipitation in Chinese hamster ovary(CHO)cells and rat brain with or without chronic morphine treatment.Saturation binding studies showed that ABIN-1 had no effect on MOR binding.However,the interaction of ABIN-1 and MOR inhibited the activation of G proteins induced by DAMGO([D-Ala2,N-Me-Phe4,Gly5-ol]-Enkephalin).MOR phosphorylation,ubiquitination,and internalization induced by DAMGO were decreased in Chinese hamster ovary cells that coexpressed MOR and ABIN-1.The suppression of forskolinstimulated adenylylcyclase by DAMGO was also inhibited by the interaction of ABIN-1with MOR.In addition,extracellular signal-regulated kinase activation was also negatively regulated by overexpression of ABIN-1.These data suggest that ABIN-1 is a negative coregulator of MOR activation,phosphorylati

关键词： Effects treatment Switching after overlay cDNA was MOR

Demonstration of high-dimensional controlled quantum teleportation for the first time

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Science China(Physics,Mechanics & Astronomy) 2024年第3期67卷 163-164页

作者： Yu-Bo Sheng lan zhou College of Electronic and Optical Engineering and College of Flexible Electronics(Future Technology) Nanjing University of Posts and TelecommunicationsNanjing 210023China College of Science Nanjing University of Posts and TelecommunicationsNanjing 210023China

Controlled quantum teleportation(CQT) [1] is the tripartite version of quantum teleportation and it allows the teleportation of an unknown quantum state under the control of a third party. Compared with low-dimensional counterparts,high-dimensional CQT can exhibit larger information transmission capacity and a higher control power [2,3].

关键词： quantum dimensional high

Imaging characteristics and treatment strategies for carotid artery occlusion caused by skull base fracture:Three case reports

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World Journal of Clinical Cases 2024年第15期12卷 2664-2671页

作者： pei-Xin Shangguan Ke-Chun zhou Department of Emergency Lishui Municipal Central HospitalLishui 323000Zhejiang ProvinceChina

BACKGROUND Traumatic internal carotid artery(ICA)occlusion is a rare complication of skull base fractures,characterized by high mortality and disability rates,and poor prognosis.Therefore,timely discovery and correct management are crucial for saving the lives of such patients and improving their prognosis.This article retrospectively analyzed the imaging and clinical data of three patients,to explore the imaging characteristics and treatment strategies for carotid artery occlusion,combined with severe skull base fractures.CASE SUMMARY This case included three patients,all male,aged 21,63,and 16 years.They underwent plain film skull computed tomography(CT)examination at the onset of their illnesses,which revealed fractures at the bases of their skulls.Ultimately,these cases were definitively diagnosed through CT angiography(CTA)examinations.The first patient did not receive surgical treatment,only anticoagulation therapy,and recovered smoothly with no residual limb dysfunction(Case 1).The other two patients both developed intracranial hypertension and underwent decompressive craniectomy.One of these patients had high intracranial pressure and significant brain swelling postoperatively,leading the family to choose to take him home(Case 2).The other patient also underwent decompressive craniectomy and recovered well postoperatively with only mild limb motor dysfunction(Case 3).We retrieved literature from PubMed on skull base fractures causing ICA occlusion to determine the imaging characteristics and treatment strategies for this type of disease.CONCLUSION For patients with cranial trauma combined with skull base fractures,it is essential to complete a CTA examination as soon as possible,to screen for blunt cerebrovascular injury.

关键词： Skull base fracture Traumatic internal carotid artery occlusion Blunt cerebrovascular injury Imaging Case report

ABIN-1 targetsβ-arrestin-2 to attenuate opioids tolerance

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中国药理学与毒理学杂志 2021年第9期35卷 670-670页

作者： ZHANG Yi-xin zhou pei-lan LU Feng-feng SU Rui-bin GONG Ze-hui State Key Laboratory of Toxicology and Medical Countermeasures Beijing Key Laboratory of Neu-ropsychopharmacologyBeijing Institute of Phar-macology and ToxicologyBeijing 100850China

OBJECTIVE Chronic morphine exposure reduced analgesic efficiency leads to morphine tolerance which was mediated byβ-arrestin signaling of MOR,but the further mecha⁃nism remains unclear.METHODS AND RESULTS Morphine tolerance and dependence was attenuated by overexpression of ABIN-1 in mice brain.ABIN-1 in hippocampus or vascular nucleus participated in morphine tolerance and physical dependence.ABIN-1 through AHD2 re⁃gion interacted with MOR to regulate its function.As the result,the peptide of AHD2 could also de⁃lay morphine tolerance as ABIN-1.Two lines of evidence may explain the function of ABIN-1 on morphine tolerance.First,ABIN-1 inhibited the phosphorylation and internalization of MOR after acute or chronic agonists treatment through inter⁃action with MOR.Second,The formation of ABIN-1-β-arrestin-2 complexes promoted the translocation ofβ-arrestin-2 to plasma mem⁃brane and accelerated the ubiquitination ofβ-ar⁃restin-2 to degrade it.However,the function kjj⁃mice brain.CONCLUSION ABIN-1 may targetβ-arrestin-2 to regulate MOR function and provides a potential strategy for enhancing morphine anal⁃gesia without increasing analgesic tolerance.

关键词： MOR ABIN-1 β-arrestin-2 tolerance

Early-diverging Titanosauriform(Dinosauria,Sauropoda)Teeth from the Lower Cretaceous Yixian Formation of Southeastern Inner Mongolia,Northeast China

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Acta Geologica Sinica(English Edition) 2024年第2期98卷 303-310页

作者： ZHANG Honggang YIN Yalei pei Rui zhou Changfu College of Earth Science and Engineering Shandong University of Science and TechnologyQingdaoShandong 266570China College of Paleontology Shenyang Normal UniversityShenyang 110034China Key Laboratory of Evolution of Past Life in NE Asia Ministry of Natural ResourcesShenyang 110034China Key Laboratory of Evolutionary Systematics of Vertebrates Institute of Vertebrate Paleontology and PaleoanthropologyChinese Academy of SciencesBeijing 100044China CAS Center for Excellence in Life and Paleoenvironment Beijing 100044China

Three eusauropod teeth(SDUST-V1064,PMOL-AD00176,PMOL-ADt0005)are reported from the Lower Cretaceous Yixian Formation of Ningcheng,southeastern Inner Mongolia,China.Two of them(SDUST-V1064,PMOL-AD00176)are assigned to early-diverging titanosauriforms in having slightly mesiodistal expansion at the base of the tooth crown,a slenderness index value>2.0 andlants apically,respectively.CT scan data of SDUST-V1064 reveals new dental information of early-diverging titanosauriforms,for example,the enamel on the labial side thicker than that on the lingual side,an enamel/dentine ratio of 0.26 and a boss present on the lingual side of the dentine of the crown.

关键词： teeth Titanosauriformes Lower Cretaceous Yixian Formation Ningcheng

Recent Advances in Asymmetric Structural Composites for Excellent Electromagnetic Interference Shielding: A Review

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Chinese Journal of Polymer Science 2024年第6期42卷 693-710页

作者： Ying zhou Bai Xue lan Xie Chang-Mei Wu Qiang Zheng Department of Polymer Materials and Engineering College of Materials and Metallurgy Guizhou University National Engineering Research Center for Compounding and Modification of Polymer Materials National and Local Joint Engineering Research Center for Functional Polymer Membrane Materials and Membrane Processes State Key Laboratory of Public Big Data Guizhou University Department of Polymer Science and Engineering Zhejiang University

Since electromagnetic pollution is detrimental to human health and the environment, numerous efforts have been successively made to achieve excellent electromagnetic interference shielding effectiveness(EMI SE) via designing the hierarchical structures for electromagnetic interference(EMI) shielding polymer composites. Among the plentiful structures, the asymmetric structures are currently a hot spot, principally categorizing into multi-layered, porous, fibrous, and segregated asymmetric structures, which endows the high EMI shielding performance for polymer composites incorporated with magnetic, conductive, and/or dielectric micro/nano-fillers, due to the “absorption-reflection-reabsorption” shielding mechanism. Therefore, this review provides the retrospection and summary of the efforts with respect to abundant asymmetric structures and multifunctional micro/nano-fillers for enhancing EMI shielding properties, which is conducive to the booming development of polymeric EMI shielding materials for the promising prospect in modern electronics and 5-generation(5G) technology.

关键词： Asymmetric structure Microano functional filler Polymer composite Electromagnetic interference shielding

Multi-junction cascaded vertical-cavity surface-emitting laser with a high power conversion efficiency of 74%

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Light(Science & Applications) 2024年第3期13卷 555-565页

作者： Yao Xiao Jun Wang Heng Liu pei Miao Yudan Gou Zhicheng Zhang Guoliang Deng Shouhuan zhou College of Electronics and Information Engineering Sichuan UniversityChengdu 610064China Suzhou Everbright Photonics Co. LtdSuzhou 215163China

High electro-optical conversion efficiency is one of the most distinctive features of semiconductor lasers as compared to other types of lasers.Its further increase remains a significant objective.Further enhancing the efficiency of edgeemitting lasers(EEL),which represent the highest efficiency among semiconductor lasers at present,is challenging.The efficiency of vertical cavity surface emitting lasers(VCSELs)has always been relatively low compared to EEL.This paper,combining modeling with experiments,demonstrates the potential of multi-junction cascaded VCSELs to achieve high efficiency beyond that of EELs,our simulations show,that a 20-junction VCSEL can achieve an efficiency of more than 88%at room temperature.We fabricated VCSEL devices with different numbers of junctions and compared their energy efficiency.15-junction VCSELs achieved a maximum efficiency of 74%at room temperature under nanosecond driving current,the corresponding differential quantum efficiency exceeds 1100%,being the largest electro-optical conversion efficiency and differential quantum efficiency reported until now for VCSELs.

关键词： cascaded power cavity

Graph neural network-based scheduling for multi-UAV-enabled communications in D2D networks

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Digital Communications and Networks 2024年第1期10卷 45-52页

作者： pei Li Lingyi Wang Wei Wu Fuhui zhou Baoyun Wang Qihui Wu anjing University of Posts and Telecommunications Nanjing210023China Nanjing University of Aeronautics and Astronautics Nanjing210016China

In this paper,we jointly design the power control and position dispatch for Multi-Unmanned Aerial Vehicle(UAV)-enabled communication in Device-to-Device(D2D)networks.Our objective is to maximize the total transmission rate of Downlink Users(DUs).Meanwhile,the Quality of Service(QoS)of all D2D users must be satisfied.We comprehensively considered the interference among D2D communications and downlink transmissions.The original problem is strongly non-convex,which requires high computational complexity for traditional optimization methods.And to make matters worse,the results are not necessarily globally optimal.In this paper,we propose a novel Graph Neural Networks(GNN)based approach that can map the considered system into a specific graph structure and achieve the optimal solution in a low complexity manner.Particularly,we first construct a GNN-based model for the proposed network,in which the transmission links and interference links are formulated as vertexes and edges,respectively.Then,by taking the channel state information and the coordinates of ground users as the inputs,as well as the location of UAVs and the transmission power of all transmitters as outputs,we obtain the mapping from inputs to outputs through training the parameters of GNN.Simulation results verified that the way to maximize the total transmission rate of DUs can be extracted effectively via the training on samples.Moreover,it also shows that the performance of proposed GNN-based method is better than that of traditional means.

关键词： Unmanned aerial vehicle D2 Dcommunication Graph neural network Power control Position planning