^125I—BMIPP在SD鼠体内的分布以及血流改变对其在心肌中分布的影响

报道了＾１２５标记的１５－（对－碘苯）３－（Ｒ，Ｓ）－甲基－十五烷酸（ＢＭＩＰＰ）在ＳＤ鼠体内的分布以血流改变对其在心肌中分布的影响，结果显示：ＳＤ鼠心肌摄取＾１２５Ｉ－ＢＭＩＰＰ在５ｍｉｎ时为３．８６％ＩＤ／ｇ，且５－６０ｍｉｎ保持稳定，３０ｍｉｎ时心／血，心／肺，心／肝比值分别为１．５６，２．０８和１．６２，而＾１２５Ｉ－ＢＭＩＰＰ在肝脏中的清除则较快，对照组心肌摄取＾１２５Ｉ－ＢＭＩＰＰ及心     

BMIPP的合成与125I标记

报道了由ω－溴十一烷酸制备β－甲基－对磺苯代十五烷酸的合成方法。 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％。     

侧链脂肪酸BMIPP的^125I标记和动物体内分布

在乙醇和水的混合溶液中，通过新生存Ｃｕ催化碘同位素交换反应制得＾１２５Ｉ－ＢＭＩＰＰ，经乙醚提取纯化后，其放射化学纯度〉９５％，制备过程中总放射性得率〉４０％，小白鼠体内分布显示２％左右的注射剂量存在于心肌组织，且长时间保持稳定。     

心肌代谢显像剂^123I—HDA制备方法的改进

＾１２３Ｉ标记的十七烷酸（１７－＾１２３Ｉ－Ｈｅｐｔａｄｅｃａｎｏｉｃ Ａｃｉｄ，简称＾１２３Ｉ－ＨＤＡ）是一种较常用的脂肪酸（ＦＦＡ）类心肌代谢显像剂，核医学临床用于评价心肌能量工谢。介绍一种改进的＾１２３Ｉ－ＨＤＡ制备方法，使制备过程缩短至９０ｍｉｎ，总放射性回收率≈７０％，可得到放射化学纯度＞９９％的无载体、无前体＾１２３Ｉ－ＨＤＡ注射液，较目前常用的其它注射液制备方法更适合于临床常规应用。     

加速器制备^123I

介绍了用＾１２４Ｔｅ（ｐ，２ｎ）＾１２３Ｉ、＾１２３Ｔｅ（ｐ，ｎ）＾１２３Ｉ，＾１２７Ｉ（ｐ，ｔｎ）＾１２３Ｘｅ→＾１２３Ｉ，＾１２４Ｘｅ（ｐ，ｘ）＾１２３Ｉ和＾１２４Ｘｅ（γ，）＾１２３Ｘｅ→＾１２３Ｉ等反应制备＾１２３Ｉ的方法，并对各种方法优缺点进行了比较。     

用核素活度计测定^123I的活度

描述了用核素活度计测定含有放性核素杂质＾１２４Ｉ的样品中的＾１２３Ｉ的活度的方法，根据不同的时间由活度计测得的值与样品中＾１２３Ｉ与＾１２４Ｉ活度比的变化相关怀，通过调节活度计的核素因子，直接读出＾１２３Ｉ的活度，分析误差〈５％。     

用（γ,n）反应生产放射性药物^123I的研究

从理论和实验上对光核反应生成放射性药物＾１２３Ｉ进行了研究,给出了有关＾１２４Ｘｅ（γ,ｎ）＾１２３Ｘｅ→＾１２３Ｉ的理论计算公式和计算结果。描述了利用保肥国家同步辐射实验室２００ＭｅＶ电子直线加速器的束流和在其末端建立的实验装置。文中给出了实验得到的反应产物的放射性活度、γ射线的谱图以及化学纯度分析结果。实验结果表明：若用纯的＾１２４Ｘｅ进行生产,在该加速器的经两个半小对照射,将可得到１８．５Ｇ     

白细胞介素2（rIL—2）的碘标记研究

采用Ｉｏｄｏｇｅｎ碘标记法制备了＾１２５Ｉ标记的白细胞介素２（＾１２５Ｉ－ｒＩＬ－２），经高效液相色谱（ＨＰＬＣ）纯化，放射性纯度大于９５％，游离＾１２５Ｉ小于５％；放射性比活度为２．２×１０＾１６－２．８×１０＾１６Ｂｑ／ｍｏｌ。该标记物用于放射免疫测定，与抗体有较高的结合活性和灵敏度。     

^99mTc（V）—DMSA及^99mTc—MIBI肺显像诊断原发性肺癌的应用研究

对３０例原发性肺癌患者分别应用＾９９ｍＴｃ（ｖ）－ＤＭＳＡ及＾９９ｍＴｃ－ＭＩＢＩ显像。结果表明：＾９９ｍＴｃ９Ｖ）－ＤＭＳＡ，＾９９ｍＴｃ－ＭＩＢＩ敏感度分别为９０％，７６．７％。两者结合显像阳性率为９６．７％。鳞状上皮细胞癌对＾９９ｍＴｃ（Ｖ）－ＤＭＳＡ及＾９９ｍＴｃ（Ｖ）－ＤＭＳＡ，＾９９ｍＴｃ－ＭＩＢＩ摄取程度比其它类型的肺癌高。     

~(99)Tc~m-NMIBI的电荷性质及其与~(99)Tc~m-MIBI的比较

采用区带电泳法和阳离子树脂交换法测定了新型潜在心肌灌注显像剂＾９９Ｔｃ＾ｍＮ－ＭＩＢＩ的电荷性质,且在相同条件下测定了＾９９Ｔｃ＾ｍ－ＭＩＢＩ的电荷性质,并将二者的电荷性质进行了比较。电泳实验结果表明,有７５．６３％＾９９Ｔｃ＾ｍ－ＭＩＢＩ移向负极;在阳离子树脂交换实验中,＾９９Ｔｃ＾ｍ－ＭＩＢＩ的ｌｇ Ｄ－ｐＨ直线斜率ｘ＝０．０４,而相应的＾９９Ｔｃ＾ｍ－ＭＩＢＩ的直线斜率ｘ＝０．９９。两种实验     

Preclinical evaluation on ~(125)I-BMIPP

The biodistribution of 125I-BMIPP and the variation of myocardial uptake of 125I-BMIPP using the metabolic intervention drug were reported. Myocardial uptake of the 125I-BMIPP in rats showed a peak of 5.70ID%/g at 2 min. The ratios of myocardium to blood, to liver and to lung at 30 min were 3.40, 2.64 and 2.88 respectively. The initial elimination half time of 4.0 min in rabbits was in accordance with the half elimination time of free fatty acid from blood. Myocardial uptake of 125I-BMIPP in the group of glucose-insulin was significantly increased (p<0.05) than those of the normal control. In vivo and in vitro binding test for 125I-BMIPP to HSA showed a rather constant level of activation up to 2 h. Partition coefficients (1gP) were 1.93 and 1.68, respectively.     

Preparation of β-methyl p-iodophenyl pentadecanoic acid(BMIPP) and ^125I-BMIPP

A method with several steps superior to literature has been developed for the preparation of β-methyl p-iodophenyl pentadecanoic acid (BMIPP),The synthesis and physical properties of BMIPP are described.It is characterized by IR,^1HNMR, elemental analysis and MS,^125I-BMIPP can be prepared by three methods:direct labeling,slid-state transfer labeling and Cu(Ⅰ) assisted labeling,Cu(Ⅰ） assisted labeling is simple and not necessary to purify before clincal use,It can fulfil the requirements for kit labeling.     

β甲基对125碘苯代十五烷酸(125I-BMIPP)的初步动物实验

为了解脂肪酸代谢显像剂 β甲基对12 5碘苯代十五烷酸 (12 5I -BMIPP)在动物体内的分布、清除和代谢干预对其心肌摄取的变化等行为 ,进行了12 5I -BMIPP的动物研究。结果显示 ,禁食SD大鼠心肌对12 5I -BMIPP的摄取高 ,最大吸收值为 5 .70 %/ g ,在心肌中滞留 1h都不变 ,至12 0min心肌摄取仍高达 2 .19± 0 .4 2ID %/ g ;30min心 /血、心 /肝和心 /肺比分别为 3.4 0、2 .6 4和 2 .88;12 5I-BMIPP在肝、肺中的摄取低 ,排泄快 ;甲状腺摄取低 ,至 12 0min ,甲状腺摄取值为 0 .0 2ID %/g ;12 5I-BMIPP与小鼠体内、外血浆蛋白结合稳定 ;异常毒性试验合格 ,每千克小鼠接受的量是人的 5 0 0倍 ;pH为 7.0 0和 7.4 0时的分配系数 (logP)分别为 1.93和 1.6 8;代谢干预研究结果显示 ,葡萄糖胰岛素干预组心肌摄取明显升高 ,与对照组相比差异具有极显著的意义。     

123I的制备及其标记新型小分子融合肽的初步研究

本工作利用天然锑靶,通过121Sb(α,2n)123I核反应,在控制锑靶厚度为62.2～64.3mg/cm2和α粒子能量为26.5MeV的情况下,可以得到11.1TBq/(A.h)以上且核纯度高达98.6%的123I。利用制备的123I进行了小分子融合肽拟似物VHCDR1-VHFR2-VLCDR3的123I标记,并对标记物的体外稳定性及在正常小鼠体内的分布进行了初步研究。结果表明,123I标记VHCDR1-VHFR2-VLCDR3的标记率可达90%以上,123I标记物在体内不易脱碘且具有较高的体外稳定性。     

一种烟碱乙酰胆碱受体(nAChRs)显像前体化合物的合成与125I标记研究

本文介绍一种可用于125/123I标记的A-85380类前体化合物--(S)-5-(三丁基锡烷基)-3-[[1-(叔丁氧基羰基)-2-甲氧基]氮杂环丁基]吡啶的设计、合成及125I标记研究.实验以2-糠胺和(S)-氮杂环丁基甲酸为起始物,先合成(S)-5-(三丁基锡烷基)-3-[[1-(叔丁氧基羰基)-2-氮杂环丁基]甲氧基]吡啶前体化合物,再用125I标记,制得5-[125I]I-A-85380.整个放射性标记的时间为50-55min,标记率大于30%.5-[125I]I-A-85380在室温下放置3天,其放化纯度仍在95%以上,表明其在体外具有较高的稳定性.     

Determination of 125I impurities in [123I]labelled radiopharmaceuticals,by liquid scintillation counting: sensitivity of the method

Iodine-125 is a radioisotopic impurity “always” present in iodine-123, produced by nuclear reactions induced either on natural or “highly” enriched targets. Liquid scintillation counting is a very sensitive tool to determine low level impurities of both low energy electrons and photons in aqueous and organic solutions of radiopharmaceutical compounds. With this technique it was possible to determine, on commercial samples, that the content of ¹²⁵I was of the order of not less than 0.1% for ¹²³I produced via ¹²⁷I(p,5n) reactions and not less than 0.01% for ¹²³I produced via “highly” enriched ¹²⁴Xe(p,X) nuclear reactions.     

3H11的~(123)I标记及其生物分布

采用Iodogen氧化法对胃癌单克隆抗体3 H11进行了123I标记,用PD-10层析柱分离纯化标记物,纸层析法测定标记物的标记率和放化纯度,评价标记物的体外稳定性,并观察了标记物在正常小鼠体内的生物分布。标记结果显示,123I-3 H11的优化标记条件为:Iodogen 10μg、3 H11 30μg、Na123I溶液20μL(13.3 MBq)、磷酸盐缓冲溶液100μL(pH7.4、0.2 mol/L)、常温下反应8 min,123I-3 H11标记率70%~80%;稳定性结果显示,标记物在4℃人血清中的体外稳定性较好,放置48 h后放化纯度92%;正常昆明鼠体内生物学分布显示,全抗3 H11血液半清除时间为12.25±0.25 h,胃组织有明显摄取。以上结果提示,123I-3 H11是一种很有前景的肿瘤放射免疫显像剂。     

Synthesis and structural analysis of ^13C-fatty acids

The ^13C-labeled fatty acids octanoic-1-^13C acid and palmitic-1-^13C acid were synthetically prepared from Ba ^13CO3,The yield of the former was more than 90% and that of the latter was above 85%,MS,IR,^1H-NMR and ^13NMR were performed to analyze the structures of the two ^13C-fatty acids,compared with their unlabeled fatty acids.     

The Property and Application of Arachidonic Acid

Arachidonic acid(AA) is one of the most important PUFAs(polyunsaturated fatty acids) in human body.A high-yield arachidonic acid-producing strain(mortierella aplina) was selected by ion implantation(the relative content of arachidonic acid is 70.2% among all fatty acids).This paper mainly introduced the structure,distribution,source,physiologic healthcare function and application of AA.     

Production of123I by irradiating124Xe with 20–30-MeV protons

Conclusion The method of obtaining¹²³I by irradiating highly enriched¹²⁴Xe with protons in the energy range from 28 to 30 MeV ensures a, high efficiency in producing the radioisotope, which is twice as high as that achieved in the reaction¹²⁷I(p, 5n) with a proton energy of 65 MeV [1]. In this, there is hardly any¹²⁴I impurity, while the amount of the¹²⁵I impurity is much smaller. An efficiency of¹²³I production that is entirely acceptable for practical purposes is also achieved with a proton energy of 22 MeV: 11.7 Ci (1 Ci=3.7·10¹⁰ Bq) after 26-h irradiation with a 50-A beam.Calculations of the excitation functions performed in [12] according to the ALICE program yielded results somewhat different from ours, but the integral¹²³I yield for a proton energy of 28 MeV was practically the same.Thus, the above method of¹²³I production makes it possible to use 22-30-MeV cyclotrons, i. e., the great majority of cyclotrons presently utilized for the production of medical radioisotopes [11]. This could probably solve the problem of adequate supply of the medically important¹²³I radioisotope that would be free from the¹²⁴I impurity.Translated from Atomnaya Énergiya, Vol. 60, No. 5, pp. 337–340, May, 1986.