心肌灌注显像剂^99mTc—Tetrofosmin

＾９９ｍｍＴｃ－Ｔｅｔｒｏｆｏｓｍｉｎ以合适的γ射线能量、半衰期和显像质量优于＾２０１Ｔｌ的心肌灌注显像。它具有良好的安全性、动力学和剂量学，标记方法简单，显像时间范围适宜。     

五种^99mTc标记的心肌注显像剂

综述了临床广泛使用以及正在开发和评估的五种＾９９ｍＴｃ标记的心肌灌注显像剂的制备与质量控制，生物学行为及临床用途。     

^99mTc标记的肾功能显像剂研究进展

＾１３１Ｉ－ＯＨＩ旧一种广泛使用的肾脏放射性药物，但是由于＾１３１Ｉ的缺陷，人们一直在寻找＾９９ｍＴｃ标记的肾功能显剂，且发展迅速，主要有ＤＡＤＳ，ＣＯＷ－ＤＡＤＳ，ＰＡＨＩＤＡ，ＭＡＧ３，ＥＣ，ＤＡＣＨ及Ｎ－取代吡哆醛衍生物等。本文扼要介绍这些化合物的化学结构，生物学特征及临床应用情况。     

新型心肌灌注显像剂^99Tc^mN—MIBI的药盒研制及质量控制

目的 建立心肌灌注显像剂^99Tc^mN－甲氧基异丁基异腈（MIBI）的药盒法制备及其质量控制方法。方法 由条件实验确定药盒中各组分的最佳含量。参照《中国药典》（1995年版）方法进行澄清度、pH值、无菌以及急性毒性检查,将药盒置于不同环境下存放不同时间,通过外观、主药含量及配合物标记率的变化来检查药盒的稳定性。结果 药盒的澄清度、pH值、无菌以及急性毒性检查合格,稳定性好。药盒法制备的配合物标记率大于95％。结论 药盒法制备^99Tc^mN－MIBI配合物简便易行,符合临床试用要求。     

心肌显像剂99mTcN(NOEt)2药盒的研制及质量控制

心肌显像剂９９ｍＴｃＮ（ＮＯＥｔ）２药盒的研制及质量控制方平周翔陈正平９９ｍＴｃＮ（ＮＯＥｔ）２（ＮＯＥｔ：Ｎ乙氧基，Ｎ乙基氨荒酸盐）在心肌中摄取高，且有再分布特性〔１，２〕。本研究采用两个药盒进行配体交换反应制备９９ｍＴｃＮ（ＮＯＥｔ）２。本研...     

心肌灌注显像剂~（99m）Tc－Tetrofosmin

￣（９９ｍ）Ｔｃ－Ｔｅｔｒｏｆｏｓｍｉｎ以合适的γ射线能量、半衰期和显像质量优于２０１Ｔｌ的心肌灌注显像。它具有良好的安全性、动力学和剂量学，标记方法简单，显像时间范围适宜。其１８０°ＳＰＥＣＴ采集图像技术比３６０°技术更为有效。对多支冠状动脉病变的敏感性明显优于单支冠状动脉病变。     

心肌显像剂^99mTcN（NOEt）2的临床药理研究

对心肌显像剂＾９９ｍＴｃＮ（ＮＯＥｔ）２（ＮＯＥｔ：Ｎ－乙氧基，Ｎ－乙基氨荒权钠盐）进行了临床前药理研究，主要包括兔备血药清除动力学，大鼠体内分布，狗显像及毒性等。制备的＾９９ｍＴｃＮ（ＮＯＥｔ）２放化纯度大于９０％，室温放置６小时稳定，分布半衰期＝２．５３分钟，清除半衰期＝３３０分钟，清除率＝３７８ｍｌ／ｈ。药物能很快被大鼠心肌摄取并保留，５、３０、６０和９０分钟时分别为４．６９、４．２０、３．     

用于P—gp功能显像的^99mTc显像剂研究进展

肿瘤细胞的多药耐受现象由磷酸糖蛋白过度表达所致，Ｐ－ｇｐ功能显像能在体内无创伤地评价Ｐ－ｇｐ的表达。     

心肌灌注显像剂^99mTc—tetrofosmin的制备和实验研究

进行新型心肌灌注显像剂ｔｅｔｒｏｆｏｓｍｉｎ的化学合成、药盒制备、９９ｍＴｃ标记、质量控制以及药理研究。方法：有机合成显像剂配体ｔｅｔｒｏｆｏｓｍｉｎ，正交实验确定９９ｍＴｃ标记药盒组分及配比，测定药盒及９９ｍＴｃｔｅｔｒｏｆｏｓｍｉｎ的理化性质，并通过药理实验确定其生物性能和安全性。Ｔｅｔｒｏｆｏｓｍｉｎ合成产物经１ＨＮＭＲ证实并制成药盒；该药盒经与９９ｍＴｃＯ－４混合，室温放置２０分钟后，可得到放化纯度大于９０％的９９ｍＴｃｔｅｔｒｏｆｏｍｉｎ，标记方法简便，标记产物稳定性好；小鼠分布实验显示较高的心／肝、心／肺比（６０分钟分别为４２６±２００和８９７±３２６）及较快的血清除速率（注射后２分钟全血百分注射剂量小于５％）；药盒各项技术指标符合药典体内诊断试剂的规定。结果表明，所研制的９９ｍＴｃｔｅｔｒｏｆｏｓｍｉｎ及其药盒达到临床试用质量。     

Evaluation of technetium 99m cyclobutylpropylene amine oxime as a potential brain perfusion imaging agent for SPET

Technetium 99md,l-cyclobutylpropylene amine oxime (^99mTc-CBPAO) has been developed as a brain-imaging agent for single photon emission tomography (SPET).^99mTc-CBPAO can be prepared using a simple labelling procedure suitable for routine clinical use. It has a high in vitro stability, as has been demonstrated by high-pressure liquid chromatography (HPLC) analysis. This shows that 3 h after labelling, less than 5% of the primary lipophilic complex which is capable of crossing the blood-brain barrier (BBB) converts to a secondary hydrophilic complex. Brain uptake (% dose/g wet tissue) of^99mTc-CBPAO, determined at 5 and 30 min after injection in two groups of six adult male Sprague-Dawley rats, was found to be 0.74±0.06 and 0.73±0.13 (mean ± SD), respectively. These values are not significantly different from those obtained repeating the experiment with^99mTc-labelled hexamethylpropylene amine oxime (^99mTc-HMPAO) (0.72±0.15 at 5 min and 0.88 ± 0.24 at 30 min after injection). Since the rat brain uptake of^99mTc-CBPAO remained unchanged for a period of time suitable for tomographic study, the comparison of the two tracers was extended to two groups of ten patients. The latter were affected by neurological and psychiatric disorders and were studied with SPET. Human brain uptake (% dose/cc cortical grey matter) of^99mTc-CBPAO and^99mTc-HMPAO were 3.04±0.57 and 4.22±0.46 (mean × 10^–3 ± SD × 10^–3), respectively, with a 32% significant difference. In two other groups of five patients, the first transit time-activity curves of the two tracers were compared. From the analysis of these curves we suggest that^99mTc-CBPAO has a higher binding effect on blood components and/or a higher degradation rate in blood than that of^99mTc-HMPAO. This may account for the reduced human brain uptake. In conclusion, SPET images of^99mTc-CBPAO reflect blood perfusion, and they have a good diagnostic quality. The main advantage of^99mTc-CBPAO is its in vitro stability; however,^99mTc-HMPAO is a superior imaging agent.     

心肌显像剂~(99m)TcN(NOEt)_2的临床前药理研究

对心肌显像剂９９ｍＴｃＮ（ＮＯＥｔ）２（ＮＯＥｔ：Ｎ乙氧基，Ｎ乙基氨荒酸钠盐）进行了临床前药理研究，主要包括兔血药清除动力学，大鼠体内分布，狗显像及毒性等。制备的９９ｍＴｃＮ（ＮＯＥｔ）２放化纯度大于９０％，室温放置６小时稳定。分布半衰期＝２５３分钟，消除半衰期＝３３０分钟，清除率＝３７８ｍｌ／ｈ。药物能很快被大鼠心肌摄取并保留，５、３０、６０和９０分钟时分别为４６９、４２０、３９５和３４３％ＩＤ／ｇ，６０分钟时心／肺比值为１１６。狗显像显示９９ｍＴｃＮ（ＮＯＥｔ）２从肺中清除比心肌快，１０、３０和６０分钟时的心／肺比值分别为１６９、２４０和２５５，３０分钟心肌显像清晰，９０分钟全身显像显示心肌摄取为２８２％ＩＤ，但肝脏摄取高达３０１３％ＩＤ。小鼠对药物的耐受量为人的６１４倍。研究表明，９９ｍＴｃＮ（ＮＯＥｔ）２具有临床研究价值。     

心肌显像剂[99Tcm(CO)3(MIBI)3]+和99Tcm-MIBI药理实验对比研究

目的对心肌显像剂羰基99Tcm-甲氧基异丁基异腈(MIBI)([99Tcm(CO)3(MIBI)3]+)和99Tcm-MIBI进行动物药理对比研究.方法制备[99Tcm(CO)3(MIBI)3]+注射液,放化纯85%.实验犬3只,每次静脉注射剂量555 MBq,通过动态采集、全身显像和采集血样,获得药代动力学参数、体内生物分布、靶/非靶比值和药效学结果.结果 [99Tcm(CO)3(MIBI)3]+符合一次静脉给药的药代动力学二室模型,快相清除半衰期T(α)1/2=(1.33±0.12) min,慢相清除半衰期T(β)1/2=(102.33±25.58) min,总清除速率(CL)=(401.33±73.51) mL/h.心、肝、肺时间-放射性曲线显示[99Tcm(CO)3(MIBI)3]+肝摄取曲线幅度低于心肌曲线,而99Tcm-MIBI肝曲线明显高于心肌曲线.10、30、60、90和120 min[99Tcm-(CO)3(MIBI)3]+在心、肺、肝百分注射剂量(%ID)与99Tcm-MIBI比较,前者心肌摄取较高,肺本底较低,肝摄取低.[99Tcm(CO)3(MIBI)3]+心/肺和心/肝比值均高于99Tcm-MIBI,差异有显著性,P均<0.01.静脉注射[99Tcm(CO)3(MIBI)3]+后10～120 min均可获得清晰的心肌图像,肝胆排泄较快,肝内放射性较低,左室下壁不受肝影影响,无需脂餐促进肝胆排泄.结论 [99Tcm(CO)3(MIBI)3]+有望成为一种新的心肌灌注显像剂.     

99Tcm-PnAO-硝基咪唑和99Tcm-HL91对乏氧心肌的实验研究

目的 探讨＾９９Ｔｃ＾ｍ－ＰｎＡＯ－硝基咪唑和＾９９Ｔｃ＾ｍ－ＨＬ９１２种乏氧心肌显像剂用于实验性心肌缺血、缺氧的作用。方法 进行小鼠体内分布与离体大鼠心脏模型研究,以９５％Ｏ２和５％ＣＯ２平衡的Ｋｒｅｂｓ－Ｈｅｎｓｅｌｅｉｔ缓冲液进行主动脉逆行灌注为对照组;以Ｎ２取代Ｏ２和ＣＯ２平衡的Ｋｒｅｂｓ－Ｈｅｎｓｅｌｅｉｔ缓冲液进行逆行灌注为乏氧组;以９５％Ｏ２和５％ＣＯ２平衡的Ｋｅｒｂｓ－Ｈｅｎｓｅｌ     

The utilization of technetium-99m CPI as a myocardial perfusion imaging agent in exercise studies

Myocardial perfusion imaging with Tc-99m carbomethoxyisopropylisonitrile (CPI) was compared with Tl-201 imaging in 22 patients who were assessed for coronary artery disease. There was agreement between Tc-99m CPI and Tl-201 imaging for detecting segmental myocardial ischemia and fixed defects in 185/198 (93%) of left ventricular segments. There was also an excellent correlation between the two tracers for the detection of coronary artery disease (18/22 patients). Myocardial clearance of the isonitrile complex was slow, and there was no redistribution into ischemic regions; the normal to ischemic myocardial ratio remained relatively constant over time. Reinjection at rest was used to distinguish transient ischemia from infarction. The isonitrile complex was excreted rapidly via the hepatobiliary system. After 3 hours, background activity was reduced to about 20% of the initial activity. Tc-99m CPI appears comparable to Tl-201 thallous chloride for detecting coronary artery disease. Tc-99m CPI may be useful as a myocardial imaging agent because there is no myocardial redistribution, myocardial clearance is slow, and clearance from background tissues is rapid.     

Influence of calcium channel inhibitors on the myocardial uptake and retention of technetium 99m N-NOET, a new myocardial perfusion imaging agent: A study on isolated perfused rat hearts

BACKGROUND: Technetium 99m N-NOET is a new myocardial perfusion imaging agent currently in phase III clinical trials in Europe. In vitro studies on newborn rat cardiomyocytes have shown that calcium inhibitors, such as verapamil or diltiazem, inhibit its cellular uptake by 40%. To determine whether such a specificity exists ex vivo, we studied the effect of verapamil, diltiazem, and nifedipine on the myocardial uptake and retention of Tc-99m N-NOET in isolated perfused rat hearts. METHODS AND RESULTS: After a 15-minute baseline period, rat hearts were perfused with 0.5 micromol/L verapamil (n = 6), 0.75 micromol/L diltiazem (n = 6), or 0.1 micromol/L nifedipine (n = 6) for 10 minutes before the injection of a bolus (40 microCi/250 microL) of the tracer. Control hearts were perfused with either 1.5 mmol/L calcium (same concentration as in the treated groups; n = 7) or 0.75 mmol/L calcium (same contractility as in the treated groups; n = 6). Myocardial activity of Tc-99m N-NOET was monitored for 30 minutes. The functional parameters of the hearts were recorded throughout the experiments. Calcium inhibitors induced a 40% to 55% decrease in maximal first derivative of left ventricular pressure (dP/dt) (0.0001相似文献   

^99mTc—PYM一步法药盒的研制

研制适宜临床使用的肿瘤阳性显像剂９９ｍＴｃ平阳霉素（ＰＹＭ）一步法药盒，将药盒中含有的各种组分以适宜的配比和方法分装在小瓶中，避光，真空干燥，密封保存。结果：该药盒无菌，无热原，无毒副作用，标记产物的放化纯度大于９０％，稳定性在４小时以上。临床试用于肺癌等９６例患者，表明该药盒的标记方法简便易行，可用于临床上肺癌的诊断。