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中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Chang-Liang LIU,Hui-Kun WANG,Guo-Yuan HU,Guo-Zhang JIN,Xue-Chu ZHEN~* Department of Pharmacology,state key laboratory of drug research,institute of materia medica,shanghai institute for biological sciences,chinese academy of sciences,shanghai,china

Oscillation is an important process in neural system for presenting,integrating and synchronizing neuronal *** only the neuronal networks but also a single neuron can oscillate at a broad band,whereas the mechanisms underlying oscillation are *** depolarized by current injection,most pyramidal neurons in layer V-VI of rat prefrontal cortex(PFC) fire regularly or in single burst at the very ***,when glutamate applied to the apical dendrite,all neurons showed an oscillatory firing,with a frequency of *** oscillation disappeared in the presence of NMDA receptor(NMDAR) antagonist APV,suggesting the dependence of NMDAR *** is further supported by the fact that pressure ejection of NMDA to the apical dendrite evoked a similar oscillation,whereas AMPA or high concentrations of KC1 failed to produce such *** of synaptic transmission by tetrodotoxin (TTX) did not disrupt the oscillatory firing,indicating that the firing is not due to network activities but to the intrinsic properties of individual *** voltage dependence of the NMDA conductance in Mg free solution or preventing Ca influx in Ca free solution completely blocked the ***,we detected parallel changes between intracellular Ca oscillation and oscillating membrane potential in response to dendritic NMDA *** observations demonstrate mat the voltage dependence of the NMDAR and Ca influx play a key role in the generation of the ***,block of SK channels and conductances underlying sAHP resulted in a depolarization plateau,which is the same as when the extracellular Ca is ***,block of either SK channels or sAHP currents respectively failed to prevent the *** results indicate that the repolarization of the membrane potential relies on both SK and sAHP currents and that the intracellular Ca takes effect mainly through these two *** conclusion,our data provide evidenc

关键词： apical dendnte pyramidal neuron prefrontal cortex burst oscillation NMDA receptor SK channel

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Differentiation of rat embryonic stem cells into functional cardiomyocytes

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岭南心血管病杂志 2011年第S1期17卷 18-19页

作者： YANG Huang-tian (key laboratory of Stem Cell Biology,institute of Health sciences,shanghai institutes for biological sciences(SIBS),CAS,shanghai 200031,china.

Rats(Rattus norvegicus) have many advantages over mice in scientific studies,for example, they are more relevant to human in physiological and pharmacological ***,rats are broadly used in experimental *** recent breakthrough in the generation of rat embryonic stem cells(rESCs) opens the door to application of gene targeting to create models for the study of human *** addition,the in vitro differentiation of rESCs into derivatives of three germ lines will serve as a powerful tool and resource for the investigation of mammalian development,cell function, tissue repair,and drug ***, the distinct culture condition and signal inhibitor-depended maintenance of rESCs stand as a considerable challenge for its in vitro *** address it,we investigated whether rESCs are capable of forming terminal differentiated cardiomyocytes. We found that the embryoid bodies(EBs)-based method used in mouse ESC(mESC) differentiation failed to work in the cultivation of *** then modified the differentiation protocol and successfully developed an in vitro differentiation system to differentiate rESCs into three embryonic germ *** using this method,the rESCs form spontaneous beating cardiomyocytes with the properties similar to those derived from fetal rat hearts and *** unique cellular system will provide a new approach to study the early development and cardiac function as well as to perform pharmacological test and cell therapy study(Grants:the state Major research Program of china.2009ZX09503-024,2010CB945603) and CAS(XDA01030000).

关键词： stem Differentiation of rat embryonic stem cells into functional cardiomyocytes

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Discovery of potent and selective c-Met inhibitor

Discovery of potent and selective c-Met inhibitor

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2011年全国药物化学学术会议——药物的源头创新

作者： Fang Chen,~aJing Ai,~b Ying Wang,~b Zhengsheng Zhan,~a Yongcong Lu,~a Yi Chen,~b Jian ding,Meiyu Geng~b and Wenhu Duan~(*,a) a Department of Medicinal Chemistry,shanghai institute of materia medica,chinese academy of sciences,shanghai 201203,PR china.bDivision of Anti-tumor Pharmacology,state key laboratory of drug research,shanghai institute of materia medica,chinese academy of sciences,shanghai 201203,PR china

＜正＞HGF/c-Met signaling pathway mediates a variety of important biological activities but deregulation of the pathway is closely associated with poor prognosis in a number of major human ***,c-Met has been considered as a good target for anti-cancer drug ***,we report the discovery of a series of triazolotriazine derivatives as selective

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Chronic morphine treatment impaired hippocampal long-term potentiation and spatial memory via accumulation of extracellular adenosine acting on adenosine Al receptors

Chronic morphine treatment impaired hippocampal long-term po...

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中国神经科学学会第九届全国学术会议暨第五次会员代表大会

作者： Gang LU~1,Qi-Xin ZHOU~2,Shuo KANG~1,Lin XU~2,Jing-Gen LIU~(1,*) 1 state key laboratory of drug research,shanghai institute of materia medica,shanghai institute For biological sciences,chinese academy of sciences,shanghai 201203,china.2 key laboratory of Animal Models and Human Disease Mechanisms of chinese academy of sciences & Yunnan Province,Kunming institute of Zoology,Kunming 650223,china

＜正＞Chronic exposure to opiates impairs hippocampal long-term potentiation（LTP） and spatial memory, but the underlying mechanisms remain to be *** the well known effects of adenosine,an important neuromodulator,on hippocampal neuronal excitability and synaptic plasticity,we investigated the potential effect of changes in adenosine concentrations on chronic morphine treatment-induced impairment of hippocampal CA1 LTP and spatial *** found that chronic treatment in mice with either increasing doses（20-100 mg/kg） of morphine for 7 d or equal daily dose（20 mg/kg） of morphine for 12 d led to a significant increase of hippocampal extracellular adenosine ***,we found that accumulated adenosine contributed to the inhibition of the hippocampal CA1 LTP and impairment of spatial memory retrieval measured in the Morris water *** A1 receptor antagonist 8-cyclopenty1-1,3-dipropylxanthine significantly reversed chronic morphine-induced impairment of hippocampal CA1 LTP and spatial ***,adenosine deaminase,which converts adenosine into the inactive metabolite inosine,restored impaired hippocampal CA1 *** further found that adenosine accumulation was attributable to the alteration of adenosine uptake but not adenosine *** nucleoside transporters（ENT2） appeared to play a key role in the reduction of adenosine *** in PKC-α/βactivity were correlated with the attenuation of the ENT2 function in the short-term（2 h） but not in the long-term（7 d） period after the termination of morphine *** study reveals a potential mechanism by which chronic exposure to morphine leads to impairment of both hippocampal LTP and spatial memory.

关键词： morphine spatial memory adenosine PKC LTP ENT

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中国红树植物红海榄(Rhizophora stylosa)的化学成分研究

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天然产物研究与开发 2004年第1期16卷 23-25页

作者：赵亚宋国强郭跃伟中国科学院上海生命科学院上海药物研究所国家新药研究重点实验室上海201203

从红树科红海榄 (Rhizophorastylosa)小枝的石油醚提取物中分得 5个三萜化合物 ,通过波谱方法鉴定 ,它们分别是taraxerol (1) ,taraxerone (2 ) ,careaborin (3) ,cis careaborin (4 )和 palmitoyl β amyrin(5 ) ,均为首次从该植物中... 详细信息

从红树科红海榄 (Rhizophorastylosa)小枝的石油醚提取物中分得 5个三萜化合物 ,通过波谱方法鉴定 ,它们分别是taraxerol (1) ,taraxerone (2 ) ,careaborin (3) ,cis careaborin (4 )和 palmitoyl β amyrin(5 ) ,均为首次从该植物中分得。

关键词：中国红树科红海榄药材三萜植物化学成分

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SPR technology and CD spectra in interaction between PPARγ-LBD and LigandsSPR technology and CD spectra in interaction between PPARγ-LBD and Ligands

SPR technology and CD spectra in interaction between PPARγ-...

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华东六省一市生物化学与分子生物学会2003年学术交流会

作者： Chang-ying Yu, Lili Chen, Feng Cheng, Rui-hao Zhang, Jian-hua Shen, Hua-liang Jiang, Xu Shen ( drug Discovery and Design Center, state key laboratory of drug research, shanghai institute of materia medica, shanghai institutes for biological sciences, chinese academy of sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, shanghai 201203, china.

PPAHγis a ligand-dependent transcription factor. It plays an important role in the regulation of adipocytefunction and systemic lipid homeostasis. PPARγparticipates in the biological pathways of basic and clinical inter-est,such as insulin sensitivity, type 2 diabetes and therosclerosis. In this report, the ligand binding characteristicsof a series of commercially available PPARγligands (GW9662, GI 262570, CPA, 15-d-PGJ, LY171883, Indom-ethacin, Linoleic acid, Palmitic acid and Troglitazone) to human PPARγligand-binding domain (LBD) were in-vestigated hy surface plasmon resonance biosensor (SPR) technology BIAcore 3000 and circular dichroism (CD)

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SKF83959-inhibited excitatory neurotransmission in hippocampus is independent of phosphatidylinositol-coupled dopamine D1 receptor but is mediated by inhibiting voltage-gated sodium channels

SKF83959-inhibited excitatory neurotransmission in hippocamp...

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中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Hong-Yuan CHU~1 Xue-Qin CHEN~1 Ao ZHANG~2 Guo-Zhang JIN~1 Guo-Yuan HU~1 Xue-Chu ZHEN~(1 *) 1 state key laboratory of drug research Department of Neuropharmacology shanghai institute of materia medica chinese academy of sciences shanghai china.2 Department of Medicinal chemistry shanghai institute of materia medica chinese academy of sciences shanghai china

＜正＞Objective The central dopamine system exerts a profound influence on excitatory neurotransmission in hippocampal CA1 ***83959,a phenylbenzazepines derivative,produced a potent anti-Parkinsonian effect via selective activation of a putative phosphatidylinositol-coupled dopamine D1 ***,how the atypical D1 receptor agonist SKF83959 regulates the neurotransmission remains *** present study was designed to explore the effects of SKF83959 to glutamate release in hippocampal CA1 *** The influence of SKF83959 to excitatory neurotransmission was studied by recording of extracellular field potentials by whole-cell patch-clamp technique. Results（1） SKF83959 inhibited the excitatory neurotransmission of hippocampal CA1 region in a concentration-dependent manner.（2） SKF83959-induced inhibitory effect was not mediated by dopamine receptors and other related receptors.（3） SKF83959 induced a robust membrane depolarization and a significant reduction of neuronal excitability.（4） SKF83959-induced reduction of neuronal excitability was mediated by inhibition of voltage-gated sodium channels. Conclusion The present study demonstrated that SKF83959-induced inhibition of glutamate release is independent of dopamine *** regulatory effect on excitatory neurotransmission is mediated via inhibition of presynaptic sodium channels.

关键词： SKF83959 dopamine hippocampus PPF sodium channel depolarization Parkinson’s disease

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Structural Basis for Ubiquitin Recognition by a Novel Domain from Human Phospholipase A2 Activating Protein

Structural Basis for Ubiquitin Recognition by a Novel Domain...

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第十一次中国生物物理学术大会暨第九届全国会员代表大会

作者： Qing-Shan Fu ,Chen-Jie Zhou ,Hong-Chang Gao ,Ya-Jun Jiang ,Zi-Ren Zhou ,Jing Hong ,Wen-Ming Yao ,Ai-Xin Song ,Dong-Hai Lin 1 ,and Hong-Yu Hu 1 state key laboratory of Molecular Biology,institute of Biochemistry and Cell Biology,shanghai institutes for biological sciences,chinese academy of sciences, shanghai 200031 china.shanghai institute of materia medica,shanghai institutes for biological sciences, chinese academy of sciences,shanghai 201203,china.$Graduate School of the chinese academy of sciences,19A Yu Quan Road,Beijing 100039,china

＜正＞Ubiquitin（Ub）is an essential modifier conserved in all eukaryotes from yeast to *** A2 activating protein（PLAA）,a mammalian homolog of yeast DOA1/UFD3,

关键词： ubiquitin ubiquitin-binding domain solution structure cis/trans isomerization PLAA.

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Activation of PI-Linked Dl-Like receptor modulates FGF-2 expression in astrocytes via IP3-dependent Ca2+ signaling

Activation of PI-Linked Dl-Like receptor modulates FGF-2 exp...

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中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Xin-Hua ZHANG~(1,2,4),Zheng ZHOU~2,Da-Kui WANG~(2,3),Ai-Qun LI~1,Yan-Qing YIN~2,Xiao-Song GU~3,Fei DING~3,Xue-Chu ZHEN~(5,*),Jia-Wei ZHOU~(2,*) 1 laboratory of Molecular Cell Biology,institute of Biochemistry and Cell Biology 2 institute of Neuroscience,state key laboratory of Neuroscience,shanghai institutes for biological sciences,chinese academy of sciences,shanghai,200031,china.3 Jiangsu key laboratory of Neuroregeneration,Nantong University School of Medicine,Nantong,226001,china.4 Department of Anatomy,Nantong University School of Medicine,Nantong,226001,china.5 state key laboratory of drug research,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of sciences,shanghai,201203,china

FGF-2 is predominantly synthesized and secreted by astrocytes in adult *** previous study showed that activation of classical dopamine receptor D1 or D2 elicits FGF-2 biosynthesis and secretion in ***,we report that astrocytic FGF-2 expression is also regulated by phosphatidylinositol(PI)-linked D1-like ***83959,a selective Pi-linked D1-like receptor agonist,upregulates the levels of FGF-2 protein in striatal astrocyte cultures in classical dopamine D1 and D2 receptor-independent *** conditional medium derived from SKF83959-activated astrocytes promoted the number of TH+ neurons in *** of astrocytes with SKF83959 increased intracellular calcium in two *** of intracellular calcium oscillation by inositol 1,4,5-triphosphate(TP3) inhibitors blocked the SKF83959-induced increase in FGF-2 ***,intraperitoneal administration of SKF83959 reversed MPTP-induced reduction in FGF-2 expression in both the striatum and ventral midbrain and resulted in marked protection of dopaminergic neurons from MPTP-induced *** results indicate that IP3/Ca/calmodulin-dependent protein kinase(CaMK) is an uncharted intracellular signaling pathway that is crucial for the regulation of FGF-2 synthesis in ***-linked Dl-like receptor plays an important role in the regulation of astrocytic FGF-2 expression and neuroprotection which may provide a potential target for the drug discovery in Parkinson’s disease.

关键词： striatum neurotrophic factor Parkinson’s disease signal transduction astrocyte FGF-2

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Silver-Catalyzed Intramolecular Cyclization of o-（1-Alkynyl）benzamides:Efficient Synthesis of （1 H）-Isochromen-1-imines

Silver-Catalyzed Intramolecular Cyclization of o-（1-Alkynyl...

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第六届全国化学生物学学术会议

作者： Guannan Liu,~a Yu Zhou,~a Deju Ye,~a Dengyou Zhang,~a Xiao Ding,~a Hualiang Jiang,~a Hong Liu~(a,*) a drug Discovery and Design Centre,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of Science 555 Zuchongzhi Road,shanghai 201203,china

＜正＞Isocoumarins are key core structural subunits that occur in a wide variety of biologically active natural products and synthetic complex molecules,as well as useful versatile synthetic intermediates. Recently,the activity of isocoumarins as potent anticancer agents invoked additional interest in the investigation of them and their *** there is a remarkable similarity in reactivity and

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