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1.
目的 探讨99Tcm-DTPA-脱氧葡萄糖(DG)对乳腺癌荷瘤裸鼠化疗疗效的评价.方法 建立乳腺癌荷瘤裸鼠模型.取裸鼠25只,体质量20~25 g,分为5组,接种乳腺癌MCF-7细胞9 d后进行化疗.对照组:注射0.1 ml生理盐水;联合化疗1组:分别按体质量注射紫杉醇11 mg/kg和阿霉素4.7 mg/kg;联合化疗2组:分别按体质量注射紫杉醇5 mg/kg和阿霉素2.3 mg/kg;顺铂1组:按体质量注射顺铂8 mg/kg;顺铂2组:按体质量注射顺铂4 mg/kg.裸鼠化疗后分别于即刻和第7,14,21及28天注射99Tcm-DTPA-DG 3.7 MBq/只,0.5 h后显像,勾画感兴趣区(ROI),计算肿瘤/健侧对应部位放射性(T/NT)比值,并测量肿瘤体积.第28天完成显像后,处死裸鼠,测量肿瘤/血液及肿瘤/肌肉放射性比值,计算抑瘤率.结果 肿瘤组织吸收99Tcm-DTPA-DG较多,肿瘤/肌肉放射性比值对照组为5.65,高于联合化疗1组(0.98,t=8.735,P<0.01)、联合化疗2组(1.13,t=4.826,P<0.01)和顺铂1组(0.84,t=3.198,P<0.05).肿瘤/血液放射性比值对照组为3.1,高于联合化疗1组(0.83,t=7.652,P<0.01)、联合化疗2组(1.29,t=3.976,P<0.05)和顺铂1组(0.96,t=3.945,P<0.05);顺铂2组因不完全缓解,肿瘤/血液放射性比值为2.66,与对照组差异无统计学意义(t=2.496,P>0.05).99Tcm-DTPA-DG可使肿瘤组织清晰显像,联合化疗1组肿瘤体积400.0 mm3,与对照组(1132.8 mm3)差异有统计学意义(t=3.952,P<0.01);联合化疗2组肿瘤体积633.9 mm3(t=4.592,P<0.05),顺铂1组肿瘤体积699.4 mm3(t=4.837,P<0.05),这2组与对照组差异有统计学意义.除顺铂2组外,余各化疗组与对照组间T/NT比值差异有统计学意义(F=1018.165,P<0.01).结论 化疗效果好的肿瘤,99Tcm-DTPA-DG显像示肿瘤体积较小,瘤体内放射性分布较少;而化疗效果差的肿瘤体积逐渐增大,瘤体内放射性分布较多.99Tcm-DTPA-DG显像可用于指导荷瘤裸鼠的化疗.  相似文献   

2.
目的研究188Re-奥曲肽在荷瘤裸鼠体内的分布,为进一步肿瘤靶向治疗奠定基础.方法16只荷人H460非小细胞肺癌的BALB/c裸鼠分为4组,经尾静脉注射188Re-奥曲肽18.5MBq(0.2ml),于注射后2h,4h,24h,48h每个时间点处死一组裸鼠,取血液、肿瘤组织及主要脏器测量其放射性计数率值,经放射性衰变校正后计算每克组织的百分注射剂量率(%ID/g),观察标记物在动物体内的生物学分布.另2只荷瘤裸鼠同样尾静脉注射相同剂量的188Re-奥曲肽,于注射后相同时间点行SPECT扫描,利用感兴趣区技术对肿瘤/非瘤组织放射性比值(T/NT)进行半定量分析.结果188Re-奥曲肽标记率达(95.3±1.8)%,188Re-奥曲肽在荷瘤裸鼠体内主要分布于肿瘤组织、肝脏、肾脏及肠道,肿瘤部位在4h摄取达到高峰9.8%ID/g,此时SPECT在肿瘤部位有明显的放射性核素浓聚,T/NT在尾静脉药物注射后24h达到高值为7.1.结论188Re-奥曲肽在BALB/c荷瘤裸鼠体内对人非小细胞肺癌具有靶向定位作用,其在肿瘤部位的分布具有较高的T/NT,188Re-奥曲肽有望用于表达生长抑素受体肿瘤的核素靶向治疗.  相似文献   

3.
目的研究188Re-奥曲肽在荷瘤裸鼠体内的分布,为进一步肿瘤靶向治疗奠定基础。方法16只荷人H460非小细胞肺癌的BALB/c裸鼠分为4组,经尾静脉注射188Re-奥曲肽 18.5MBq(O.2ml).于注射后2h,4h,24h,48h每个时间点处死一组裸鼠,取血液、肿瘤组织及主要脏器测量其放射性计数率值,经放射性衰变校正后计算每克组织的百分注射剂量率(%ID/g),观察标记物在动物体内的生物学分布。另2只荷瘤裸鼠同样尾静脉注射相同剂量的188Re-奥曲肽,于注射后相同时间点行SPECT扫描,利用感兴趣区技术对肿瘤/非瘤组织放射性比值(T/NT)进行半定量分析。结果188Re-奥曲肽标记率达(95.3±1.8)%,188Re-奥曲肽在荷瘤裸鼠体内主要分布于肿瘤组织、肝脏、肾脏及肠道,肿瘤部位在4h摄取达到高峰9.8%ID/g,此时SPECT在肿瘤部位有明显的放射性核素浓聚,T/NT在尾静脉药物注射后24h达到高值为7.1。结论 188Re-奥曲肽在BALB/c荷瘤裸鼠体内对人非小细胞肺癌具有靶向定位作用,其在肿瘤部位的分布具有较高的T/NT,188Re.奥曲肽有望用于表达生长抑素受体肿瘤的核素靶向治疗。  相似文献   

4.
目的 制备特异性整合素αvβ3探针[^18F]氟化铝-匹仑吉肽(^18F-Al-NOTA-PRGD2),探讨其用于甲状腺乳头状癌(PTC) PET显像的可行性.方法 采用氟化铝新策略制备18F-Al-NOTA-PRGD2.取新鲜切除的人PTC肿瘤组织接种于裸鼠右腋下,制得荷人PTC裸鼠模型.再分别取人PTC标本及毗邻的正常组织、荷瘤裸鼠移植瘤行整合素αvβ3免疫组织化学染色.荷瘤裸鼠(n=5)尾静脉注射1.1 MBq ^18F-Al-NOTA-PRGD2后30、60和120 min分别行microPET显像,通过ROI技术计算肿瘤和主要脏器的放射性摄取值(% ID/g),并通过阻断实验验证其特异性.另取15只荷瘤裸鼠研究其注药后30、60及120 min生物分布,计算放射性摄取值(%ID/g).用两样本t检验进行统计学处理.结果 成功制备^18F-Al-NOTA-PRGD2,标记率>45%.免疫组织化学染色证实人PTC标本和裸鼠移植瘤组织整合素αvβ3染色均呈棕褐色阳性表达,人PTC毗邻正常组织不表达.荷瘤裸鼠注射^18 F-Al-NOTA-PRGD2后行microPET显像示,肿瘤清晰可见,且与周围组织对比度良好.注射后30、60、120 min肿瘤对显像剂的摄取值分别为(2.81±0.35)、(2.45±0.27)和(1.80±0.21) %ID/g.PRGD2阻断后,注射^18F-Al-NOTA-PRGD2后60 min肿瘤对显像剂的摄取值降为(0.51±0.05) %ID/g.荷瘤裸鼠生物分布实验示,注射显像剂后30、60、120 min肿瘤摄取值分别为(3.09±0.25)、(2.75±0.37)和(1.90±0.16) %ID/g,与microPET显像基本一致(t=1.456、1.465和0.847,均P>0.05).^18F-Al-NOTA-PRGD2在血液和肌肉中清除快,注射后60 min肿瘤与血液和肌肉的摄取比值分别为6.15±0.45和7.86±0.56.结论 ^18F-Al-NOTA-PRGD2制备简单,放化纯高,可有效监测PTC中整合素αvβ3表达水平;其PET显像有望为研究PTC整合素αvβ3受体相关机制提供一种新方法.  相似文献   

5.
目的 研究131 I标记抗人表皮生长因子受体-2蛋白(HER-2/neu)单克隆抗体Herceptin在正常昆明小鼠和荷人卵巢癌裸鼠体内的生物分布及荷人卵巢癌裸鼠的放射免疫显像特点.方法 (1)Iodogen法131I标记Herceptin,测定其标记率、放化纯、稳定性及免疫活性.(2)流式细胞仪和免疫组织化学法分别检测人卵巢癌SKOV-3、HO-8910细胞株及瘤组织HER-2/neu表达情况.(3)计算131I-Herceptin经昆明小鼠尾静脉注射后5,15,30 min和1,2,4,12,24,48,72 h及荷瘤裸鼠尾静脉注射后4,12,24和48h的每克组织百分注射剂量率(%ID/g)和肿瘤/非肿瘤组织放射性(T/NT)比值.(4)行131I-Herceptin荷卵巢癌裸鼠模型显像,观察注射后1,2,4,8,12,24,48,72,96和120h显像情况并确定最佳显像时间.结果 (1)131I-Herceptin标记率为89.8%,放化纯为98.4%,24 h后仍大于80%,标记物免疫活性较好.(2)SKOV-3细胞株HER-2/neu高表达,表达率92.67% 而HO-8910细胞株表达很低,表达率仅9.59%.(3)131I-Herceptin在昆明小鼠体内主要经肝、脾及肾代谢,血液快相半排期为0.27 h,慢相半排期为51.96h.在荷人SKOV-3移植瘤部位,24 h时放射性摄取值达到18.08%ID/g,显著高于其他脏器组织 T/NT比值随时间延长逐渐增高,72 h时肿瘤/脑放射性比值高达27.27.(4)SKOV-3荷瘤裸鼠在尾静脉注射131I-Herceptin后2 h即可见移植瘤放射性浓聚,48 h后与周围组织对比更为明显,至120 h时仍见移植瘤部位放射性明显浓聚,与对侧感兴趣区比值高达11.44.而HO-8910荷瘤裸鼠各时间点移植瘤几乎未见放射性浓聚.结论 131I-Herceptin对荷人SKOV-3移植瘤具有良好的靶向作用,有望用于高表达HER-2/neu的人卵巢癌患者放射免疫显像及其复发转移灶的靶向治疗.  相似文献   

6.
目的 研究131 I标记抗人表皮生长因子受体-2蛋白(HER-2/neu)单克隆抗体Herceptin在正常昆明小鼠和荷人卵巢癌裸鼠体内的生物分布及荷人卵巢癌裸鼠的放射免疫显像特点.方法 (1)Iodogen法131I标记Herceptin,测定其标记率、放化纯、稳定性及免疫活性.(2)流式细胞仪和免疫组织化学法分别检测人卵巢癌SKOV-3、HO-8910细胞株及瘤组织HER-2/neu表达情况.(3)计算131I-Herceptin经昆明小鼠尾静脉注射后5,15,30 min和1,2,4,12,24,48,72 h及荷瘤裸鼠尾静脉注射后4,12,24和48h的每克组织百分注射剂量率(%ID/g)和肿瘤/非肿瘤组织放射性(T/NT)比值.(4)行131I-Herceptin荷卵巢癌裸鼠模型显像,观察注射后1,2,4,8,12,24,48,72,96和120h显像情况并确定最佳显像时间.结果 (1)131I-Herceptin标记率为89.8%,放化纯为98.4%,24 h后仍大于80%,标记物免疫活性较好.(2)SKOV-3细胞株HER-2/neu高表达,表达率92.67%;而HO-8910细胞株表达很低,表达率仅9.59%.(3)131I-Herceptin在昆明小鼠体内主要经肝、脾及肾代谢,血液快相半排期为0.27 h,慢相半排期为51.96h.在荷人SKOV-3移植瘤部位,24 h时放射性摄取值达到18.08%ID/g,显著高于其他脏器组织;T/NT比值随时间延长逐渐增高,72 h时肿瘤/脑放射性比值高达27.27.(4)SKOV-3荷瘤裸鼠在尾静脉注射131I-Herceptin后2 h即可见移植瘤放射性浓聚,48 h后与周围组织对比更为明显,至120 h时仍见移植瘤部位放射性明显浓聚,与对侧感兴趣区比值高达11.44.而HO-8910荷瘤裸鼠各时间点移植瘤几乎未见放射性浓聚.结论 131I-Herceptin对荷人SKOV-3移植瘤具有良好的靶向作用,有望用于高表达HER-2/neu的人卵巢癌患者放射免疫显像及其复发转移灶的靶向治疗.  相似文献   

7.
目的 研究131 I标记抗人表皮生长因子受体-2蛋白(HER-2/neu)单克隆抗体Herceptin在正常昆明小鼠和荷人卵巢癌裸鼠体内的生物分布及荷人卵巢癌裸鼠的放射免疫显像特点.方法 (1)Iodogen法131I标记Herceptin,测定其标记率、放化纯、稳定性及免疫活性.(2)流式细胞仪和免疫组织化学法分别检测人卵巢癌SKOV-3、HO-8910细胞株及瘤组织HER-2/neu表达情况.(3)计算131I-Herceptin经昆明小鼠尾静脉注射后5,15,30 min和1,2,4,12,24,48,72 h及荷瘤裸鼠尾静脉注射后4,12,24和48h的每克组织百分注射剂量率(%ID/g)和肿瘤/非肿瘤组织放射性(T/NT)比值.(4)行131I-Herceptin荷卵巢癌裸鼠模型显像,观察注射后1,2,4,8,12,24,48,72,96和120h显像情况并确定最佳显像时间.结果 (1)131I-Herceptin标记率为89.8%,放化纯为98.4%,24 h后仍大于80%,标记物免疫活性较好.(2)SKOV-3细胞株HER-2/neu高表达,表达率92.67%;而HO-8910细胞株表达很低,表达率仅9.59%.(3)131I-Herceptin在昆明小鼠体内主要经肝、脾及肾代谢,血液快相半排期为0.27 h,慢相半排期为51.96h.在荷人SKOV-3移植瘤部位,24 h时放射性摄取值达到18.08%ID/g,显著高于其他脏器组织;T/NT比值随时间延长逐渐增高,72 h时肿瘤/脑放射性比值高达27.27.(4)SKOV-3荷瘤裸鼠在尾静脉注射131I-Herceptin后2 h即可见移植瘤放射性浓聚,48 h后与周围组织对比更为明显,至120 h时仍见移植瘤部位放射性明显浓聚,与对侧感兴趣区比值高达11.44.而HO-8910荷瘤裸鼠各时间点移植瘤几乎未见放射性浓聚.结论 131I-Herceptin对荷人SKOV-3移植瘤具有良好的靶向作用,有望用于高表达HER-2/neu的人卵巢癌患者放射免疫显像及其复发转移灶的靶向治疗.  相似文献   

8.
目的 观察放射性榄香烯三羰基铼(ETRC)对荷小细胞肺癌裸鼠模型的肿瘤生长抑制作用,并分析其在裸鼠体内的分布、靶向性.方法 以中草药有效成分β-榄香烯为起始原料,人工合成ETRC;制备荷H128小细胞肺癌BALB/c裸鼠模型,12只荷瘤裸鼠尾静脉注射ETRC,分别在不同时间测量肿瘤组织及各器官的放射性,计算每克组织百分注射剂量率(%ID/g).将20只荷瘤裸鼠随机分为4组:①对照组;②榄香烯治疗组;③~(188)Re治疗组;④ETRC治疗组.尾静脉注射相应试剂后24d比较肿瘤的体积和质量.结果 给药后6h肿瘤组织的放射性最强,为(6.35±0.33)%ID/g,此时肿瘤/血液放射性比值为2.59,肿瘤/肝放射性比值为4.07,肿瘤/脾放射性比值为3.87.给药后24d,肿瘤体积和质量分别为①组:(2.945±0.567)cm~3,(5.438±1.232)g;②组:(1.860±0.263)cm~3,(4.876±0.621)g;③组:(1.861±0.896)cm~3,(4.691±1.595)g;④组:(0.601±0.152)cm~3,(1.602±0.194)g.ETRC治疗组显著好于其他各组.结论 ETRC能有效抑制裸鼠小细胞肺癌的生长,对小细胞肺癌治疗有潜在的应用前景.  相似文献   

9.
目的 进行99Tcm-精氨酸-谷氨酸-丝氨酸(RES)的亲肿瘤实验研究.方法 采用标准Fmoc固相合成法合成RES,在不同的试剂和温度(100 ℃或室温)条件下,以氯化亚锡为还原剂进行RES的99Tcm标记,优化标记条件.进行荷A549肺癌裸鼠99Tcm-RES显像并测定%ID/g,研究99TcmRES在荷瘤裸鼠体内的分布.比较兔炎性反应和肿瘤模型显像结果.结果 (1)酒石酸钠及氢氧化钠为缓冲剂,氯化亚锡为还原剂,100 ℃水浴10 min,RES放化纯最高达到85%;99Tcm-RES性能稳定,室温下放置6 h,放化纯仍达75%.(2)注射后0.5 h,99Tcm-RES多分布于心、肝、肾等血供丰富脏器,2 h血液的放射性(0.36%ID/g)降幅明显,仅相当于0.5 h(2.35%ID/g)的1/7;心、肝、肺的放射性降幅稍慢,但明显快于肿瘤;注射后0.5 h肿瘤放射性摄取为2.32%ID/g,6 h为1.54%ID/g,6 h后仍有超过60%的放射性滞留.99Tcm-RES注射后6 h肿瘤/血、肿瘤/心、肿瘤/肝、肿瘤/肺、肿瘤/脾和肿瘤/骨骼肌放射性比值分别为5.31,1.88,1.57,3.58,4.16和5.92.(3)荷瘤鼠显像发现肿瘤部位明显浓聚99Tcm-RES,而201Tl、99Tcm-MIBI在肿瘤部位未见明显浓聚.(4)兔炎性反应和肿瘤模型显像示肿瘤部位放射性明显浓聚,而炎性反应部位放射性无明显浓聚,注药后6 h肿瘤/炎性反应部位放射性比值为3.12.结论 用放射性组合化学文库筛选出的小分子RES是一种与肿瘤高亲和力的多肽,有望成为一种肿瘤显像剂.  相似文献   

10.
目的 观察131I-2F7抗体对荷小细胞肺癌裸鼠模型的肿瘤生长抑制作用,并分析其在裸鼠体内的分布、靶向性和药代动力学.方法 用氯胺T法制备131I-2F7抗体,制备荷H128小细胞肺癌BALB/c裸鼠模型,15只荷瘤裸鼠尾静脉注射131I-2F7抗体7.4 MBq,分别在不同时间测量肿瘤组织及各器官的放射性,计算每克组织百分注射剂量率(%ID/g).将20只荷瘤裸鼠随机分成4组①生理盐水对照组,②单纯2F7抗体治疗组,③单纯131I治疗组和④131I-2F7抗体治疗组.尾静脉注射相应试剂后观察24 d,比较肿瘤的体积、质量,计算抑瘤率.结果 给药36 h肿瘤组织的放射性最强,为(6.45±0.33)%ID/g,此时肿瘤/血液放射性比值为2.63,肿瘤/肝放射性比值为4.13.给药24 d后,肿瘤体积和质量分别为①组(3.431±0.667)cm3,(6.441±1.234)g;②组(2.964±0.263)cm3,(5.876±0.620)g;③组(2.674±0.897)cm3,(5.689±1.605)g;④组(0.746±0.153)cm3,(1.602±0.194)g.131I-2F7抗体治疗组与其他各组间差异有显著性(P<0.05).结论 131I-2F7抗体能有效抑制裸鼠小细胞肺癌的生长,对小细胞肺癌治疗有潜在的应用前景.  相似文献   

11.
Two groups of young healthy men--natives of lowlands who for one year lived and worked in chronic hypoxia (Group 1 at an altitude of 1680 m with PO2 = 120 mm Hg and Group 2 at an altitude of 3650 with PO2 = 90 mm Hg) were examined. It was found that after this prolonged exposure the subjects showed a higher sensitivity of the respiration system to hypoxia, an enhanced lung ventilation and circulation, a lower gas exchange and physical work capacity. The concentration of lactic acid at rest in the Group 2 subjects was 47% higher than in the Group 1 subjects. The lactate/pyruvate ratio in the Group 2 subjects increased by 46% thus indicating an enhanced rate of anaerobic processes. A higher deficiency of buffer bases, a lower concentration of bicarbonates in blood at rest and during exercise tests of the Group 2 subjects pointed to metabolic acidosis. The subjects with a higher rate of anaerobic metabolism in a low PO2 environment displayed a diminished sensitivity of the hypoxic stimulation of respiration, an increased tolerance to the very low PAO2 and a reduced work capacity in chronic hypoxia.  相似文献   

12.
The purpose of this study was to determine, with a rodent tumor model, if microelectrode measurements of unmodulated tumor oxygenation predict for the avidity of hypoxic markers to tumor tissue. METHODS: The rapidly growing, anaplastic variant of the Dunning rat prostate carcinoma cell line (R3327-AT) was implanted subcutaneously on the upper backs of Fischer X Copenhagen rats. Approximately 100 measurements of PO2 were obtained from tumors of 5-10 g in animals that were restrained and then subjected to different anesthetic procedures. Values of median PO2 (in mm Hg) and percentage of measurements <5 mm Hg obtained from individual tumors were used to define tumor oxygenation status. The radiodiagnostic hypoxic markers beta-D-iodinated azomycin galactopyranoside (IAZGP) and [99mTc]HL-91 were simultaneously administered to 26 animals whose tumor oxygen levels had been measured. Six hours after marker administration, the animals were killed; tumor, blood, and muscle tissues were sampled; and percentage injected dose per gram (%ID/g*), tumor/blood ratio (T/B), and tumor/muscle ratio (T/M) parameters were determined. Parameters of marker avidity to individual tumors were linearly correlated with microelectrode measurements of tumor oxygenation to determine the significance of inverse associations. RESULTS: The median PO2 of 41 tumors varied from 2.0 to 20.9 mm Hg, with an average value of 7.5 +/- 1.4 mm Hg. Six tumors had unusually high values; that is, >10 mm Hg, and when these were excluded from the analysis, the average median PO2 of the remaining 35 was 4.3 +/- 0.7 mm Hg. When electrode measurements of tumor oxygenation were obtained under conditions of halothane anesthesia with the animals breathing O2, carbogen, or air, median PO2 values increased significantly (P = 0.001). When animals were deeply anesthetized by intraperitoneal injection of ketamine-xylazine, median PO2 values were not significantly different (P = 0.13) from those obtained while the animals were restrained and breathing air. There was no inverse correlation of significance between the electrode measurements of median PO2 and the avidity of beta-D-IAZGP nor [99mTc]HL-91 in this tumor model. The range of median PO2 values in these tumors was at least 3 mm Hg, and the range of hypoxic marker avidity was less than twofold. CONCLUSION: These data demonstrate that microelectrode measurements of rat tumor oxygenation did not correlate with the avidity of the two hypoxic markers, at least in this tumor model. The larger dynamic range of tumor oxygen measurements obtained with microelectrodes might be biased to low values by their necrotic fractions, the zones within solid tumors that contain dead cells and debris that will not be labeled by bioreducible hypoxic markers. Hypoxic marker avidity to individual tumors will have to be validated by other assays that can predict for their radiosensitivity.  相似文献   

13.
18F-labeled fluoroerythronitroimidazole (FETNIM) has been suggested as a marker of tumor hypoxia for use with PET. Our goal was to evaluate the pharmacokinetic properties of [18F]FETNIM in rats and analyze metabolites in human, dog, and rat plasma and urine. Metabolites in liver and tumor homogenates from tumor-bearing rats, as well as the biodistribution of the tracer, were also studied. METHODS: Radio-thin-layer chromatography and digital autoradiography were used to distinguish metabolites from the parent drug in urine and plasma from 8 patients, 3 dogs, and 18 rats, as well as in liver and tumor homogenates from Sprague-Dawley rats bearing 7,12-dimethylbenzanthracene-induced rat mammary carcinoma. Biodistribution of [18F]FETNIM was also studied in rats at 15, 30, 60, 120, and 240 min after tracer injection. RESULTS: Most of the radioactivity in plasma and urine was the unchanged tracer, whereas rat liver homogenates contained almost only metabolites of [18F]FETNIM. None of the species studied showed binding of tracer to plasma proteins. A large variation-3%-70%-in the radioactivity represented by unchanged [18F]FETNIM was found in rat tumor. A negative correlation was found between the percentage of radioactivity represented by unchanged [18F]FETNIM in tumor tissue and tumor uptake (percentage injected dose per gram of tissue) at later times. The highest radioactivity was seen in urine and kidney; the lowest uptake was in fat, cerebellum, and bone matrix. In contrast to matrix, bone marrow had high uptake of 18F. The tumor-to-blood ratio reached a maximum of 1.80 +/- 0.64 at 2 h. CONCLUSION: We conclude that [18F]FETNIM shows low peripheral metabolism, little defluorination, and possible metabolic trapping in hypoxic tumor tissue. These suggest a potential use for this tracer in PET studies on hypoxia of cancer patients.  相似文献   

14.
目的研究^99Tc^m-survivin mRNA反义肽核酸(PNA)显像在肿瘤特异性诊断中的价值。方法用^99Tc^m标记人工合成的12碱基单链survivin mRNA反义PNA。20只荷瘤(A549)裸鼠按随机数字表法分为4组,每组5只。每只裸鼠经尾静脉注入^99Tc^m-survivin mRNA反义PNA,3组进行体内分布研究,其余进行显像研究。用同样方法对20只炎性反应(金黄色葡萄球菌)小鼠进行分组、体内分布和显像研究。采用SPSS13.0软件进行统计学分析,组间计量资料比较采用t检验。结果^99Tc^m-survivin mRNA反义PNA在肝内分布最高,其次是肾,注射后4h肿瘤组靶/非靶(T/NT)比值明显高于炎性反应组,分别为3.69±1.13,2.03±0.47,差异有统计学意义(t=3.01,P=0.02)。肿瘤组在注射药物后0.5h即可见肿瘤清晰显影,至4h时显影仍较清晰,而炎性反应部位始终未见明显显影。结论^99Tc^m-survivin mRNA反义PNA基因显像可通过其在肿瘤组织中的特异性浓聚区分肿瘤与炎性反应,为肿瘤的特异性诊断提供了一种可能的新方法。  相似文献   

15.
The purpose of this study was to evaluate the effect of tumor size on the uptake of 18F-fluorodeoxyglucose (FDG) and fluoroerythronitroimidazole (FETNIM) in a murine sarcoma model. ICR mice were xenografted with sarcoma 180 cell line and tumors were allowed to grow to a weight of 0.26-5.82 grams. 18F-FDG and 18F-FETNIM were injected intravenously in separate groups of mice, and after 1 hr, the tumors were excised and radiotracer uptake was measured. In another group of mice tumors were autoradiographically analyzed and subjected to H & E staining. In both the FDG and FETNIM group, per-gram radiotracer uptake by a tumor was inversely proportional to tumor weight. 18F-FETNIM correlated more (r = -0.593, p < 0.05) than 18F-FDG (r = -0.447, p < 0.05). Autoradiographic studies revealed that FDG accumulated in viable tumor areas, whereas FETNIM accumulated in both viable and partially necrotic areas. In the case of 18F-FETNIM, a direct correlation between tumor weight and the no-uptake-area to total-tumor-area was demonstrated. We concluded that increased tumor size is associated with decreased uptake of 18F-FDG and FETNIM, though this depends on the type of radiotracers and distribution of necrosis.  相似文献   

16.
18F-Fluoroerythronitromidazole (FETNIM) is a new promising PET tracer for imaging tumor hypoxia. Accurate radiation dosimetry is important for estimating absorbed radiation doses to patients and for calculating the allowable injected dose. METHODS: Radiation absorbed doses were estimated from PET scans obtained on cancer patients on the basis of the MIRD procedure. Dynamic acquisition data was obtained from the thorax, abdomen, and head and neck regions. The tracer was injected intravenously and mean injected activity was 366 MBq (range, 288-385 MBq). Arterial blood was continuously assayed over dynamic PET imaging. The bladder wall dose was evaluated from the voided urine activity measurements. RESULTS: The effective dose to a 70-kg adult was 0.015 or 0.019 mSv/MBq, calculated on 2- or 4-h voiding intervals, respectively. The critical organ proved to be the urinary bladder wall, with a highest absorbed dose of 0.062 or 0.127 mGy/MBq depending on the voiding schedule as described above. Absorbed doses in all other organs were at least 5-fold smaller than the bladder wall doses. CONCLUSION: With an injected activity of 370 MBq (18)F-FETNIM, the radiation doses are generally comparable with those of other related radionuclide imaging procedures. Specifically, in comparison with (18)F-fluoromisonidazole, the absorbed doses of (18)F-FETNIM are equal. However, special attention should be given to adequate hydration and voiding to limit the relatively high exposure of the critical organ, bladder wall, to (18)F-FETNIM.  相似文献   

17.
目的 探讨小分子多肽血栓显像剂99Tcm-邻苯二甲酸二甲酯(DMP) 444在PE和下肢深静脉血栓(DVT)动物模型中的显像效果.方法 选5条杂种犬,制备左下肺动脉血栓和右股静脉血栓动物模型.注射显像剂后即刻(30 s)、2、3、4、5、10、15、30、60、90和120 min分别取静脉血1ml,测质量及放射性计数.以注射后即刻的血液放射性计数为100%,计算各时间点的99Tcm-DMP444血液清除率.注射后15、30、60、90和120 min,分别进行胸部及双后肢平面显像.应用ROI方法,分别计算肺血栓/肺本底(P/L)、股静脉血栓/对侧股静脉血(D/B)和股静脉血栓/肌肉本底(D/M)的放射性比值.显像结束后,取出血栓分别测定肺动脉血栓和股静脉血栓摄取99Tcm-DMP444的%ID/g.不同时间点均数之间的差异采用单向重复测量方差分析.结果 99Tcm-DMP444注射后120 min的血液清除率为(65.4±3.9)%.左下肺动脉及右股静脉血栓部位放射性摄取随时间逐步增强,注射后15至120 min,P/L,D/B和D/M比值分别从2.41±0.28、1.67±0.33、2.20±0.14增加至3.96±0.64、2.56±0.57、3.90±0.95,差异均有统计学意义(F=14.57、7.68和9.37,P均<0.05).PE和后肢DVT的%ID/g分别为0.085±0.023和0.054±0.018.结论 99Tcm-DMP444能无创性地早期检测急性PE和下肢DVT,是较为理想的小分子多肽血栓显像剂.  相似文献   

18.
目的 评价非气性腹腔内加压作为肝脏损伤后院前救治手段的有效性和安全性.方法 将Wistar大鼠29只按随机数字表法分配进入IAP0、IAP5、IAP10、IAP15组(每组鼠数分别为8,8,8,5只),建立抗凝大鼠严重肝损伤动物模型后,采用非可扩张性充气式气囊相应地行0,5,10,15 mm Hg(1 mm Hg =0.133 kPa)等不同程度的腹腔内加压.实验过程中,如平均动脉压(MAP)< 95 mm Hg时,颈静脉内补充乳酸钠林格液(3.3 ml· min-1·kg-1)直至MAP达到100 mm Hg.持续30 min后,以饱和氯化钾处死动物,记录各组动物死亡率、失血量、补液量、肝脏湿重以及MAP等指标.结果 IAP0、IAP5、IAP10组动物无死亡,IAP15组4/5的大鼠于加压后10~15 min内死亡.IAP0、IAP5、IAP10、IAP15组大鼠腹腔内失血量依次减少[(54.20±11.30) ml/kg、(43.98±9.20) ml/kg、(32.49±7.40) ml/kg、(25.77±14.16) ml/kg,P<0.01].IAP10组补液量高于IAP0、IAP5、IAP15组补液量[(31.06±3.14)ml、(24.94±6.67) ml、(23.06±7.98)ml、( 16.50±7.27) ml,P<0.05].IAP5、IAP10、IAP15组中肝脏湿重明显大于IAP0组肝脏湿重[(11.18±1.45)g、( 12.13±0.96)g、(11.41±1.20)g、(10.03±0.58)g,P<0.05].IAP5、IAP10两组MAP差异无统计学意义[(64.81±19.65) mm Hg、( 65.80±15.36 )mm Hg,P>0.05)],却明显高于IAP0及IAP15组MAP[ (41.22±10.00) mm Hg、(44.50±28.60) mm Hg,P<0.05)].结论 非气性腹腔内加压对于严重的大鼠肝脏损伤具有止血作用,但需注意避免腹腔内压力过高所致的副作用.  相似文献   

19.
18F-FRP170, 1-(2-fluoro-1-[hydroxymethyl]ethoxy)methyl-2-nitroimidazole, is a new hypoxia imaging agent for positron emission tomography. This compound was synthesized by 18F-labeling of RP170, which was developed as a new hydrophilic 2-nitroimidazole analog. In the present study, we analyzed dynamic whole-body imaging in healthy volunteers and dynamic tumor imaging in three patients with lung cancer. METHODS: Four healthy male volunteers and three lung cancer patients were enrolled in this study. Volunteers underwent dynamic whole-body scans just after injection of 18F-FRP170 for about 90 min, while the lung cancer patients underwent dynamic tumor imaging for about 60 or 120 min. Data are expressed as standardized uptake values (SUV). Regions of interest were placed over images of each organ or tumor to generate time-SUV curves. RESULTS: The series of dynamic whole-body scans showed rapid elimination of 18F-FRP170 from the kidneys following elimination from the liver. Very low physiological uptake was observed above the diaphragm. 18F-FRP170 uptake in the lung cancer lesion could be visualized clearly from early after injection. The changes of tumor SUV, tumor/blood ratio, or tumor/muscle ratio about 30 min after injection or later were small. CONCLUSIONS: Dynamic imaging using 18F-FRP170 demonstrated rapid elimination from the kidney, suggesting the high hydrophilicity of this imaging agent. The background activity above the diaphragm was very low, and patients with lung cancer showed clear tumor uptake of 18F-FRP170 early after injection.  相似文献   

20.
[A(14)-*I]iodoinsulin was prepared for studies to assess the suitability of labeled iodoinsulin for positron emission tomography (PET). Iodine-125 was used to establish the methods and for preliminary studies in rats. Further studies and PET scanning in rats were carried out using iodine-124. Tissue and plasma radioactivity was measured as the uptake index (UI = [cpm x (g tissue)(-1)]/[cpm injected x (g body weight)(-1)]) at 1 to 40 min after intravenous injection of either [A(14)-(125)I]iodoinsulin or [A(14)-(124)I]iodoinsulin. For both radiotracers, initial clearance of radioactivity from plasma was rapid (T(1/2) approximately 1 min), reaching a plateau (UI = 2.8) at approximately 5 min which was maintained for 35 min. Tissue biodistributions of the two radiotracers were comparable; at 10 min after injection, UI for myocardium was 2.4, liver, 4.0, pancreas, 5.4, brain, 0.17, kidney, 22, lung, 2.3, muscle, 0.54 and fat, 0.28. Predosing rats with unlabelled insulin reduced the UI for myocardium (0.95), liver (1.8), pancreas (1.2) and brain (0.08), increased that for kidney (61) but had no effect on that for lung (2.5), muscle (0.50) or fat (0.34). Analysis of radioactivity in plasma demonstrated a decrease of [(125)I]iodoinsulin associated with the appearance of labeled metabolites; the percentage of plasma radioactivity due to [(125)I]iodoinsulin was 40% at 5 min and 10% at 10 min. The heart, liver and kidneys were visualized using [(124)I]iodoinsulin with PET.  相似文献   

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