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Biological evaluation on ^(125)I-ADAM as serotonin transporter ligand

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Nuclear Science and Techniques 2007年第4期18卷 218-222页

作者： LEI Bei ZHU Junqing lu chunxiong JIANG Quanfu ZOU Meifeng WANG Songpei LI Xiaomin WU Chunying The Key Laboratory of Nuclear Medicine Ministry of Health Jiangsu Institute of Nuclear Medicine Wuxi 214063 China Huashan Hospital Fudan University Shanghai 200040 China

ADAM (2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine) is suggested as a promising serotonin transporter (SERT) imaging agent for central nervous system. In this paper, biodistribution studies in rats showed that the initial uptake of 131I-ADAM in the brain was high (1.087%ID at 2 min post-injection), and consistently displayed the highest binding (between 60~240 min post-injection) in hypothalamus, a region known with the highest density of SERT. The specific binding((T/CB)-1) of 131I-ADAM in hypothalamus were 2.94, 3.03 and 3.09 at 60, 120 and 240 min post-injection, respectively. The (T/CB)-1 was significantly blocked by pretreatment with paroxetine, which is known as a serotonin site reuptake inhibitor, while another nonselective competing drug (5HT2A antagonist) Ketanserin, showed no block effect. The rat brain autoradiography and analysis showed that there was a high 131I-ADAM uptake in hypothalamus, the ratio of hypothalamus/cerebellum was significantly reduced from 7.94±0.39 to 1.30±0.56 by pretreatment with paroxetine at 60 min post-injection. Blood clearance kinetics was performed in rats, and the initial half-life of 13.79 min and late half-life of 357.14 min were obtained. The kinetic equation is: C=3.6147e-0.0725t + 1.0413e-0.0028t. The thyroid uptake was 0.009% ID and 1.421% ID at 2 min and 120 min post-injection, respectively, suggesting that in vivo deiodination may be the major route of metabolism. Toxicity trial showed that the dose per kilogram administered to mice was 1000 times greater than that to humans, assuming a weight of 50kg. These data suggest that 131I-ADAM may be useful for SPECT imaging of SERT binding sites in the brain.

关键词：抑郁症 SERT ADAM 放射诊断复合胺生物分布

Animal biodistribution, safety and validation study of dopamine transporter PET imaging agent ^(18)F-FECNT

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Nuclear Science and Techniques 2009年第1期20卷 11-16页

作者： WANG Songpei CHEN Zhengping LI Xiaomin TANG Jie LIU Chunyi ZOU Meifen PAN Donghui lu chunxiong XU Yuping XU Xijie ZHOU Xingqin JIN Jian The Key Laboratory of Nuclear Medicine Ministry of Health PRC Jiangsu Institute of Nuclear Medicine Wuxi 214063 PR China School of Medicine and Pharmaceutics Jiangnan University Wuxi 214122 PR China

This work was to investigate the pharmacologic characteristics of 18F-FECNT (2β-carbomethoxy-3β- (4-chlorophenyl)-8-(2-[18F]fluoroethyl)nortropane) as a dopamine transporter (DAT) PET imaging agent. Its partition coefficients were determined in n-octanol and phosphate buffer (PB) (pH 7.0 and pH 7.4). 6-Hydroxydopamine (6-OHDA) left-sided lesioned Parkinsonian rats were established and validated by rotational behavior tests. Biodistribution in vivo in mice, autoradiography in normal and hemi-Parkinsonian rat brains, and toxicity test were performed. The results showed that partition coefficients were 34.14 (pH 7.0) and 56.41 (pH 7.4), respectively. Biodistribution exhibited rapid uptake and favorable retention in the mice brains. The major radioactivity was metabolized by the hepatic system. The autoradiography showed that 18F-FECNT was highly concentrated in striatum, and that the left and the right striatal uptake were symmetrical in normal SD rat brains. In left-sided lesioned PD rat brains, the striatal uptake of 18F-FECNT bilaterally decreased in comparison with normal rats. No significant uptake was visible in the 6-OHDA lesioned-sided striatal areas. The results demonstrated that 18F-FECNT binds to DAT was specific. Toxicity trial displayed that the acceptable dose per kilogram to mice was 625 times greater than that to human. These indicate that 18F-FECNT is a potentially safe and useful DAT PET imaging agent in the brain.

关键词： DAT PET ^18F-FECNT PD 原子核

ASYMPTOTIC THEORY FOR THE CIRCUIT ENVELOPE ANALYSIS

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Journal of Computational Mathematics 2024年第4期42卷 955-978页

作者： chunxiong Zheng Xianwei Wen Jinyu Zhang Zhenya Zhou College of Mathematics and Systems Science Xinjiang UniversityUrumqi 830046China Department of Mathematical Sciences Tsinghua UniversityBeijing 100084China Empyrean Software Empyrean Technology Co.Ltd.Beijing 100102China

Asymptotic theory for the circuit envelope analysis is developed in this paper.A typical feature of circuit envelope analysis is the existence of two significantly distinct timescales:one is the fast timescale of carrier wave,and the other is the slow timescale of modulation *** first perform pro forma asymptotic analysis for both the driven and autonomous *** resorting to the Floquet theory of periodic operators,we make a rigorous justification for first-order asymptotic *** turns out that these asymptotic results are valid at least on the slow *** speed up the computation of asymptotic approximations,we propose a periodization technique,which renders the possibility of utilizing the NUFFT *** experiments are presented,and the results validate the theoretical findings.

关键词： Asymptotic analysis Circuit envelope analysis Floquet theory Singularly perturbed problem

Tuning the diffusion constant to optimize the readout of positional information of spatial concentration patterns

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Chinese Physics B 2024年第8期33卷 579-586页

作者：江嘉杰罗春雄刘峰 The State Key Laboratory for Artificial Microstructures and Mesoscopic Physics School of PhysicsPeking UniversityBeijing 100871China Center for Quantitative Biology Peking UniversityBeijing 100871China Wenzhou Institute University of Chinese Academy of Sciences Wenzhou 325001China Key Laboratory of Hebei Province for Molecular Biophysics Institute of BiophysicsSchool of Health Science&Biomedical EngineeringHebei University of TechnologyTianjin 300130China

Positional information encoded in spatial concentration patterns is crucial for the development of multicellular ***,it is still unclear how such information is affected by the physically dissipative diffusion *** we study one-dimensional patterning systems with analytical derivation and numerical *** find that the diffusion constant of the patterning molecules exhibits a nonmonotonic effect on the readout of the positional information from the concentration ***,there exists an optimal diffusion constant that maximizes the positional ***,we find that the energy dissipation due to the physical diffusion imposes a fundamental upper limit on the positional information.

关键词： pattern formation positional information mutual information diffusion

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^18F-FLT的标记前体Nosyl-FLT的HPLC-ELSD法测定

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中国医药工业杂志 2010年第1期41卷 38-40页

作者：蒋泉福陆春雄周杏琴江苏省原子医学研究所卫生部核医学重点实验室江苏无锡214063 江南大学化学与材料工程学院江苏无锡214122

建立了HPLC-ELSD法测定Nosyl-FLT,采用C_8色谱柱,流动相为甲醇-水-三氟乙酸(90:10:0.1)。Nosyl-FLT在0.2～2 mg/ml浓度范围内线性关系良好,检测限为5 ng,RSD小于1.25%。

关键词： Nosyl—FLT 高效液相色谱蒸发光散射检测器测定

5-羟色胺转运体显像剂[^(125)I]-ADAM的合成以及初步生物学分布

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核技术 2005年第10期28卷 766-770页

作者：蒋泉福吴春英陆春雄陈正平王颂佩张同兴李晓敏朱钧清江苏省原子医学研究所卫生部核医学重点实验室无锡214063

完成了5-羟色胺转运体显像剂[125I]-2-((2-((二甲基氨基)甲基)苯基)巯基)5-碘苯胺([125I]-2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine,[125I]ADAM)的制备和初步生物学特性的评价。以2,5-二溴-硝基苯和2-巯基苯甲酸为起始原料,合成标记前体5-三丁基锡-2-[2-(二甲基氨基甲基苯基巯基)]苯胺,采用双氧水标记法标记;并进行了大鼠体内和脑内的初步生物分布研究。合成标记前体5-三丁基锡-2-[2-(二甲基氨基甲基苯基巯基)]苯胺的总产率为42%,用[125I]NaI标记后,TLC测放射化学纯度(RCP)大于95%;125I-ADAM大鼠脑摄取高,在富含5-羟色胺转运蛋白的丘脑中的摄取随时间延长而增加,滞留时间长,其特异结合在注射后60min、120min和240min分别为3.38,3.62和4.36。本合成方法总收率高,标记方法简便,放射化学纯度高,125I-ADAM初始进脑量高,与SERT结合特异,可望用于研究脑内SERT功能。

关键词： 5-羟色胺转运体,[^125I]ADAM,合成,生物分布

APPROXIMATION, STABILITY AND FAST EVAluATION OF EXACT ARTIFICIAL BOUNDARY CONDITION FOR THE ONE-DIMENSIONAL HEAT EQUATION

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Journal of Computational Mathematics 2007年第6期25卷 730-745页

作者： chunxiong Zheng Department of Mathematical Sciences Tsinghua University Beijing 100084 China Institut für Numerische Mathematik Universitaet Miinster Germany

In this paper we consider the numerical solution of the one-dimensional heat equation on unbounded domains. First an exact semi-discrete artificial boundary condition is derived by discretizing the time variable with the Crank-Nicolson method. The semi-discretized heat equation equipped with this boundary condition is then proved to be unconditionally stable, and its solution is shown to have second-order accuracy. In order to reduce the computational cost, we develop a new fast evaluation method for the convolution operation involved in the exact semi-discrete artificial boundary condition. A great advantage of this method is that the unconditional stability held by the semi-discretized heat equation is preserved. An error estimate is also given to show the dependence of numerical errors on the time step and the approximation accuracy of the convolution kernel. Finally, a simple numerical example is presented to validate the theoretical results.

关键词： Heat equation Artificial boundary conditions Fast evaluation Unbounded domains.

脂肪酸心肌显像剂14(R,S)-氟-18-6-硫十七烷酸的制备和生物分布

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上海医学 2004年第1期27卷 26-29页

作者：吴春英林祥通陆春雄张政伟薛方平刘平复旦大学附属华山医院PET中心上海200040 江苏省原子医学研究所

目的　制备脂肪酸心肌显像剂 14 (R ,S) 氟 18 6 硫十七烷酸 ( 18F FTHA) ,并在小鼠体内进行初步评价。方法　以 8 溴 1 辛醇为原料 ,经醇氧化、丙基溴化镁格反应、水解、巯基取代、烷基化、酯化、酯水解等反应 ,合成标记前体FTHA OT... 详细信息

目的　制备脂肪酸心肌显像剂 14 (R ,S) 氟 18 6 硫十七烷酸 ( 18F FTHA) ,并在小鼠体内进行初步评价。方法　以 8 溴 1 辛醇为原料 ,经醇氧化、丙基溴化镁格反应、水解、巯基取代、烷基化、酯化、酯水解等反应 ,合成标记前体FTHA OTs( 5 )。以氟化聚铵 (kryptofix/K + 18F)为亲核试剂 ,在乙腈溶液中与FTHA Cts( 5 )进行氟代亲核反应 ,经水解生成18F FTHA ,采用薄层层析 (TLC)和高效液相色谱 (HPLC)法检测放射化学纯度(RCP)。结果　RCP大于 92 % ,稳定性好。小鼠心肌摄取高 [( 2 8.70± 3.5 2 ) %ID/g ,10min],滞留时间长[( 18.6 3± 2 .98) %ID/ g ,12 0min],注药后 10和 12 0min的心 /血比值分别为 9.4 5和 17.2 5。结论　制备的18F FTHA放化纯高 ,稳定性好。

关键词：脂肪酸心肌显像剂 14(R,S)-氟-18-6-硫十七烷酸制备生物分布小鼠

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BMIPP的合成与^(125)I标记

同位素 1999年第4期12卷 217-220,221页

作者：纪书仁吴春英陆春雄方平江苏省原子医学研究所核医学国家重点实验室无锡214063

报道了由ω溴十一烷酸制备β甲基对碘苯代十五烷酸(BMIPP)的合成方法。终产物经红外、核磁共振、元素分析和质谱等方法确证。同时报道了BMIPP的125I标记方法,经TLC检测,标记率和放化纯度分别大于80%和98%。

关键词： BMIPP 心肌代谢显像剂合成碘标记化合物