Cardiac metabolism: A technical spectrum of modalities including positron emission tomography,single-photon emission computed tomography,and magnetic resonance spectroscopy

Noninvasive techniques for the assessment of cardiac metabolism are important for the detection of potentially salvageable tissue in jeopardized areas of the myocardium. The correct identification of hibernating and stunned myocardium in patients with severely depressed cardiac function can have vital therapeutic consequences for the patient. Changes in myocardial fatty acid and glucose metabolism during acute and prolonged ischemia can be traced by positron-emitting or gamma-emitting radiopharmaceuticals. Alternatively,³¹P-labeled magnetic resonance spectroscopy can be used for the assessment of high-energy phosphate metabolism. It is not yet clear which modality will emerge as the most useful in the clinical setting. Positron emission tomography (PET) that uses combinations of flow tracers and metabolic tracers offers unique opportunities for quantification and high-resolution static and rapid dynamic studies. Currently, assessment of glucose metabolism with¹⁸F-fluorodeoxyglucose is regarded as the gold standard for myocardial viability and prediction of improvement of impaired contractile function after revascularization. However, preserved oxidative metabolism may be required for potential functional improvement, and therefore assessment of residual oxidative metabolism by¹¹C-labeled acetate PET may prove to be more accurate than¹⁸F-fluorodeoxyglucose PET, which reflects both anaerobic and oxidative metabolism. Moreover, because fatty acids are metabolized only aerobically, they are excellent candidates for the clinical assessment of myocardial viability and prediction of functional improvement after revascularization. Especially derivatives of fatty acids that are not metabolized but accumulate in the myocyte are attractive for myocardial imaging. Examples are¹²³I-beta-methyl-p-iodophenyl pentadecanoic acid and 15-(o-¹²³I-phenyl)-pentadecanoic acid. These tracers can be detected by planar scintigraphy and single-photon emission computed tomography, which are more economical and widely available than PET. In addition, 511 keV collimators have been developed recently, making the detection of positron emitters by planar scintigraphy and single-photon emission computed tomography feasible. The experience with³¹P-labeled magnetic resonance spectroscopy in humans is still limited. With current magnetic resonance spectroscopic techniques, insufficient spatial resolution is achieved for clinical purposes, but the possibility of serial measurements to monitor rapid changes of phosphate-containing molecules in time makes magnetic resonance spectroscopy very valuable for the research of myocardial metabolism.     

缺碘和氟中毒对大鼠甲状腺的协同作用

实验用Wistar大鼠212只,按饮食中碘和氟含量不同随机分为五组,实验期为7个月。结果显示:摄碘正常的大鼠长期饮用30ppm氟水后引起甲状腺功能和形态的严重损害,而饮用10ppm氟水的大鼠仅见甲状腺滤泡上皮超微结构的轻度异常变化;单纯性缺碘大鼠甲状腺肿大并伴有代偿性功能变化,缺碘并饮用10ppm氟水的大鼠在其甲状腺肿大的同时伴有明显的形态结构损伤及甲状腺代偿功能抑制,甚至功能低下。     

应用Opalescence脱色方法治疗色素牙的疗效观察(附112例临床分析)

目的 :研究 Opalescence脱色方法对色素牙脱色的疗效。方法 :将 Opalescence脱色剂涂于个别托模唇、颊侧内 ,病人每晚睡前刷牙后擦干牙面 ,戴上托模 ,晨起摘下冲洗干净 ,每天 1次 ,疗程一般为 2周 ,视疗效及患者反应增减用药时间。结果 :1 1 2例患者脱色治疗后氟斑牙的显效率( 80 .8%)高于四环素牙的显效率 ( 66.7%)。有 2 3例病人疗效不甚满意。结论 :应用 Opalescence脱色治疗活髓色素牙效果明显 ,脱色后牙体呈自然色泽 ,透明感好 ,特别适用于年龄较轻、无牙体缺损的氟斑牙及四环素牙的脱色。     

Synthesis of [18F]‐labeled adenosine analogues as potential PET imaging agents

The syntheses of adenosine analogues, 2′‐deoxy‐2′‐[¹⁸F]fluoro‐9‐β‐D ‐arabinofuranosyladenine ([¹⁸F]‐FAA) and 3′‐deoxy‐3′‐[¹⁸F]fluoro‐9‐β‐D ‐xylofuranosyladenine ([¹⁸F]‐FXA) are reported. Adenosine ( 1 ) was converted to its methoxytrityl derivatives 2 and 3 as a mixture. After separation, these derivatives were converted to their respective triflates 4 and 5 . Each triflate was reacted with tetrabutylammonium[¹⁸F]fluoride to produce 6b or 7b , which by acidic hydrolysis yielded compounds 8b and 9b . Crude preparations were purified by HPLC to obtain the desired pure products. The radiochemical yields were 10‐18% decay corrected (d. c.) for 8b and 30‐40% (d. c.) for 9b in 4 and 3 runs, respectively. Radiochemical purity was >99% and specific activity was >74 GBq/μmol at the end of synthesis (EOS). The synthesis time was 90‐95 min from the end of bombardment (EOB). Copyright © 2003 John Wiley & Sons, Ltd.     

Preparation of fluorine‐18‐labelled fluoromisonidazole using two different synthesis methods

¹⁸F‐labelled fluoromisonidazole [1H‐1‐(3‐[¹⁸F]fluoro‐2‐hydroxypropyl)‐2‐nitroimida‐zole; ([¹⁸F]FMISO)] is used as an in vivo marker of hypoxic cells in tumours and ischaemic areas of the heart and the brain. The compound plays an important role in evaluating the oxygenation status in tumours during radiotherapy. In this paper, we report experiments carried out in our laboratory in synthesizing [¹⁸F]FMISO using two different methods. The first method (I) for the [¹⁸F]FMISO synthesis was the fluorination of (2R)‐(?)‐glycidyl tosylate to [¹⁸F]epifluorohydrin. The subsequent nucleophilic ring opening, achieved with 2‐nitroimidazole, leads to labelled FMISO. The second method (II) was the fluorination of the protected precursor 1‐(2′‐nitro‐1′‐imidazolyl)‐2‐O‐tetrahydropyranyl‐3‐O‐toluenesulphonyl‐propanediol, followed by a rapid removal of the protecting group. With the first method, the radiochemical yield was about 10% at the end of the synthesis (EOS), and the radiochemical purity was over 99%. The radiochemical yield in the second method was 21% (EOS) on an average, and the radiochemical purity was over 97%. When an automated commercial synthesis module was used with method II, slightly better and more reproducible yields were achieved. The improvement in the synthesis yield with the automated apparatus will be valuable when working with high activities, and therefore it is under further development. Copyright © 2003 John Wiley & Sons, Ltd.     

18F-FDG符合线路SPECT显像在胃肠道恶性肿瘤术后的应用

目的探讨^18F—FDG符合线路SPECT显像在探测胃肠道恶性肿瘤术后复发和远处转移中的应用价值。方法24例胃肠道恶性肿瘤术后患者，其中食管癌4例，胃癌7例，结肠癌6例，直肠癌7例，运用SIEMENS ECAM^deut SPECT仪进行^18F—FDG显像。结果^18F—FDG显像诊断胃肠道恶性肿瘤术后转移和复发的灵敏度为94．7％，特异性80．0％，准确性91．7％。在^18F—FDG显像真阳性18例中，2例为局部复发，5例为局部复发伴转移，11例为远处转移。在有复发的7例患者中，5例^18F—FDG显像结果与CT检查结果一致，2例CT检查局部未见异常，在有转移的16例患者中，共检出转移灶55处。结论符合线路SPECT仪^18F—FDG显像是检测胃肠道恶性肿瘤术后复发和转移的敏感而有效的方法。     

不同氟浓度与老年人群骨折关系调查研究

目的 了解不同饮水氟浓度与老年人群骨折的关系。方法 选择6个不同的水氟浓度组(0．25mg／L-7．97mg／L)，采用整群抽样的方法，每个组抽取1500人左右，对≥50岁且居住于本地的人群进行骨折及有关情况的回顾性流行病学调查。结果 本次共调查8260人，共发生骨折531人，总骨折率为6．42％，男性骨折率(7．46％)高于女性(5．51％)，差异有显著性。低饮水氟和高饮水氟两组人群的骨折率高于正常饮水氟组的骨折率，差异有显著性，饮水氟浓度与接触人群的骨折率之间呈现U型曲线相关，饮水氟浓度与接触人群的自然骨折仍然呈现U型曲线分布。在髋部骨折病例中，饮水氟最高浓度组的髋部骨折率高于正常饮水氟浓度组。饮水氟正常组(1．00mg／L～1．06mg／L)的二次骨折率和二个部位骨折率低于其他饮水氟组。结论 低氟或超量摄氟都会增加骨折的危险，适宜的饮水氟有益于降低骨折的危险。     

曲靖市某磷酸盐厂"三废"中的氟对周围人群健康的影响

目的了解曲靖市某磷酸盐厂排出“三废”中的氟对周围人群影响情况。方法当地疾病控制与监督部门于1998年对该厂周围的虹桥、耿屯、望城、螃蟹坡4个村人群进行随机抽样调查。结果尿氟>3 mg/L检出率分别为1.72%、23.44%、33.33%,16.13%。发现低年龄组患氟斑牙比较严重,4个村检出率分别为45.16%、64.52%、72.73%、81.25%,而高年龄组患氟骨症比较明显。结论有关部门必须加强对该厂废气排放的管理。     

New radiolabelling chemistry: synthesis of phosphorus–[18F]fluorine compounds

The feasibility of synthesizing compounds containing the P–¹⁸F bond has been demonstrated by labelling the pesticide, cholinesterase inhibitor Dimefox (N,N,N′N′‐tetramethylphosphorodiamidic fluoride) with F‐18. Radiolabelling was achieved in high radiochemical yield (96%) by nucleophilic substitution of the chloro group attached to phosphorus, in the oxidation state P(V), by ¹⁸F^? (activated with tetrabutylammonium carbonate in acetonitrile). Given the large number of important biological molecules possessing phosphorus such as oligonucleotides, phospholipids as well as phosphorylated proteins, sugars and steroids, this new labelling chemistry may provide an additional route to radiolabelling these biologically important compounds for use in PET. Copyright © 2005 John Wiley & Sons, Ltd.     

Synthesis of 2‐[(2‐chloro‐2′‐[18F]fluoroethyl)amino]‐2H‐1,3,2‐oxazaphosphorinane‐2‐oxide (18F‐fluorocyclophosphamide), a potential tracer for breast tumor prognostic imaging with PET

A fluorine‐18 labeled analog of the widely used chemotherapeutic agent cyclophosphamide was synthesized as a tracer for prognostic imaging with positron emission tomography. 2‐[(2‐Chloro‐2′‐[¹⁸F]fluoroethyl)amino]‐2H‐1,3,2‐oxazaphosphorinane‐2‐oxide (¹⁸F‐fluorocyclophosphamide), was prepared by direct halogen exchange reaction from the parent cyclophosphamide. In small‐scale syntheses, radiochemical yields of up to 4.9% and specific activities of 960 Ci/mmol were achieved in a total synthesis time of 60–75 min. The [¹⁸F]‐labeled cyclophosphamide analog with radioactive purity >99% and chemical purity >96% was suitable for in vivo (microPET imaging) and ex vivo studies of a murine model of human breast tumors. Copyright © 2005 John Wiley & Sons, Ltd.