5-HT1A受体拮抗剂WAY-100635的合成

2-氨基吡啶和2-氯乙酰氯经酰胺化、与N'-(邻甲氧基苯基)哌嗪缩合、氢化铝锂还原得4-(邻甲氧基苯基)-1-[2-[(2-吡啶基)氨基]乙基]哌嗪,再与环己甲酰氯缩合得到5-HT1A受体拮抗剂WAY-100635,总收率35%.     

微肾镜联合大功率钬激光与大通道经皮肾镜取石术治疗老年复杂肾结石的疗效及安全性比较

目的:探讨微肾镜取石术(MPCNL)联合大功率钬激光与大通道经皮肾镜取石术(PCNL)治疗老年复杂肾结石的疗效及安全性,为老年复杂肾结石PCNL治疗通道的选择提供参考。方法:选择老年复杂肾结石患者92例,随机分为MPCNL组(n=47)和大通道组(n=45),MPCNL组采用MPCNL治疗,大通道组采用大通道PCNL治疗,比较两组手术时间、术中出血量、一次结石取净率、尿液转清时间、术后住院时间、并发症发生情况和肾功能恢复情况。结果:MPCNL手术时间长于大通道组,术中出血量、并发症发生率明显低于大通道组(P<0.05)。两组一次结石取净率差异无统计学意义(P>0.05),MPCNL组术后尿液转清时间、术后住院时间、肾造瘘管留置时间明显短于大通道组(P<0.05)。MPCNL组患者血肌酐水平于术后24 h达高峰,术后30 d恢复至术前水平;大通道组血肌酐水平术后48 h达高峰,术后30 d仍高于术前水平。MPCNL组血肌酐术后24 h、48 h、7 d、30 d均明显低于大通道组(P<0.05)。结论:MPCNL较大通道PCNL术中出血量、并发症明显减少,术后肾功能恢复更快,安全性更高,是老年复杂肾结石患者较适宜的一种术式。     

18F-FECNT的生物分布特性及小动物PET显像研究

Objective 2β-carbomethoxy-3β-(4-corophenyl)-8-(2-18F-fluoroethyl) nortropane (18F-FECNT) is a recently developed dopamine transporter (DAT) imaging agent. The aim of this study was to evaluate its brain biedistribution and to assess its usefulness in quantitation of DAT density in normal and hemiparkinsonian rats. Methods Six groups of mice (5 mice each group) received 18F-FECNT were sacri-ficed at indicated time post injection. Different brain regions (cortex, hippocampus, striatum, cerebellum) were removed, weighed, and countered. DAT blocking effect was investigated in mice pretreated with 2β-Carbomethoxy-3β-(4-fluorpbenyl)tropane (β-CFT) at before 18F-FECNT injection. MicroPET scans were performed in beth normal and unilaterally 6-hydroxydopamine-lesioned rats. Results The brain uptake of 18F-FECNT was 2.22, 1.20, 1.02, 0.78, 0.71, and 0.67 percent injection dose (%ID) at 5, 15, 30, 60, 120, and 180 min post injection. Radioactivity concentration of the striatum, the target region, was the highest in the brain regions and decreased quickly from 5 to 60 min and reached to background at 120 min of post injection. The striatum/cerebellum ratio was 2.56, 3.47, 2.78, 1.63, 0.97, and 0.88 at 5, 15, 30, 60, 120, and 180 min, respectively, post injection. The selective striatum uptake of 18F-FECNT decreased dramatically to the background when the DAT was blocked with β-CFT. The striatum of normal rats in micro-PET exhibited symmetrical (left/right = 1.00±0.05) and the highest uptake of radioactivity (striatum/cere-helium =2.18±0. 16 at 5- 125 min, n =3). As for the hemiparkinsonian rats, nonsymmetrical [unlesioned striatum/cerebellum vs lesioned striatum/cerebellum = 2.01 ± 0.23 (n = 3) vs 1.04 ± 0. 05] and the high-est uptake of radioactivity were also noted. Conclusions The results suggest that 18F-FECNT rapidly pas-ses through blood-brain barrier and locates in stiatal region with high affinity and selectivity to DAT. It is a potential radiotracer to assess the in vivo DAT density in Parkinson's disease.     

TURP治疗高危良性前列腺增生症体会

目的探讨高危BPH的有效治疗方法。方法分析我院128例高危BPH患者TURP治疗经过。结果128例经充分术前准备,行TURP,127例治愈,1例术后死于心肌梗死。术后国际前列腺症状评分改善,最大尿流率明显增加。结论选择TURP治疗高危前列腺增生,方法安全,疗效满意。     

18F-FECNT的生物分布特性及小动物PET显像研究

Objective 2β-carbomethoxy-3β-(4-corophenyl)-8-(2-18F-fluoroethyl) nortropane (18F-FECNT) is a recently developed dopamine transporter (DAT) imaging agent. The aim of this study was to evaluate its brain biedistribution and to assess its usefulness in quantitation of DAT density in normal and hemiparkinsonian rats. Methods Six groups of mice (5 mice each group) received 18F-FECNT were sacri-ficed at indicated time post injection. Different brain regions (cortex, hippocampus, striatum, cerebellum) were removed, weighed, and countered. DAT blocking effect was investigated in mice pretreated with 2β-Carbomethoxy-3β-(4-fluorpbenyl)tropane (β-CFT) at before 18F-FECNT injection. MicroPET scans were performed in beth normal and unilaterally 6-hydroxydopamine-lesioned rats. Results The brain uptake of 18F-FECNT was 2.22, 1.20, 1.02, 0.78, 0.71, and 0.67 percent injection dose (%ID) at 5, 15, 30, 60, 120, and 180 min post injection. Radioactivity concentration of the striatum, the target region, was the highest in the brain regions and decreased quickly from 5 to 60 min and reached to background at 120 min of post injection. The striatum/cerebellum ratio was 2.56, 3.47, 2.78, 1.63, 0.97, and 0.88 at 5, 15, 30, 60, 120, and 180 min, respectively, post injection. The selective striatum uptake of 18F-FECNT decreased dramatically to the background when the DAT was blocked with β-CFT. The striatum of normal rats in micro-PET exhibited symmetrical (left/right = 1.00±0.05) and the highest uptake of radioactivity (striatum/cere-helium =2.18±0. 16 at 5- 125 min, n =3). As for the hemiparkinsonian rats, nonsymmetrical [unlesioned striatum/cerebellum vs lesioned striatum/cerebellum = 2.01 ± 0.23 (n = 3) vs 1.04 ± 0. 05] and the high-est uptake of radioactivity were also noted. Conclusions The results suggest that 18F-FECNT rapidly pas-ses through blood-brain barrier and locates in stiatal region with high affinity and selectivity to DAT. It is a potential radiotracer to assess the in vivo DAT density in Parkinson's disease.     

18F-FECNT的生物分布特性及小动物PET显像研究

Objective 2β-carbomethoxy-3β-(4-corophenyl)-8-(2-18F-fluoroethyl) nortropane (18F-FECNT) is a recently developed dopamine transporter (DAT) imaging agent. The aim of this study was to evaluate its brain biedistribution and to assess its usefulness in quantitation of DAT density in normal and hemiparkinsonian rats. Methods Six groups of mice (5 mice each group) received 18F-FECNT were sacri-ficed at indicated time post injection. Different brain regions (cortex, hippocampus, striatum, cerebellum) were removed, weighed, and countered. DAT blocking effect was investigated in mice pretreated with 2β-Carbomethoxy-3β-(4-fluorpbenyl)tropane (β-CFT) at before 18F-FECNT injection. MicroPET scans were performed in beth normal and unilaterally 6-hydroxydopamine-lesioned rats. Results The brain uptake of 18F-FECNT was 2.22, 1.20, 1.02, 0.78, 0.71, and 0.67 percent injection dose (%ID) at 5, 15, 30, 60, 120, and 180 min post injection. Radioactivity concentration of the striatum, the target region, was the highest in the brain regions and decreased quickly from 5 to 60 min and reached to background at 120 min of post injection. The striatum/cerebellum ratio was 2.56, 3.47, 2.78, 1.63, 0.97, and 0.88 at 5, 15, 30, 60, 120, and 180 min, respectively, post injection. The selective striatum uptake of 18F-FECNT decreased dramatically to the background when the DAT was blocked with β-CFT. The striatum of normal rats in micro-PET exhibited symmetrical (left/right = 1.00±0.05) and the highest uptake of radioactivity (striatum/cere-helium =2.18±0. 16 at 5- 125 min, n =3). As for the hemiparkinsonian rats, nonsymmetrical [unlesioned striatum/cerebellum vs lesioned striatum/cerebellum = 2.01 ± 0.23 (n = 3) vs 1.04 ± 0. 05] and the high-est uptake of radioactivity were also noted. Conclusions The results suggest that 18F-FECNT rapidly pas-ses through blood-brain barrier and locates in stiatal region with high affinity and selectivity to DAT. It is a potential radiotracer to assess the in vivo DAT density in Parkinson's disease.     

^18F-FECNT的生物分布特性及小动物PET显像研究

目的探讨多巴胺转运蛋白（DAT）显像剂^18F-N-（2-氟乙基）-2β-甲酯基-3β-（4-氯苯基）去甲基托烷（FECNT）的体内生物分布特性,并进行小动物PET显像研究,以评价其临床应用潜力。方法自制^18F-FECNT注射液,进行正常小鼠脑内分布、DAT阻断实验、正常和单侧帕金森病（PD）模型大鼠小动物PET脑显像。结果正常ICR小鼠在给药后5,15,30,60,120,180min的进脑量分别达2．22,1．20,1．02,0．78,0．71,0．67百分注射剂量率（％ID）。给药后5～60min内,药物在纹状体（ST）部位浓聚,纹状体／小脑（ST／CB）比值在5,15,30,60min时分别为2．56,3．47,2．78,1．63。120min后ST的放射性浓度下降至与其他脑组织相近。脑内DAT经β-CFF阻断的小鼠,其ST未见放射性浓聚。正常大鼠小动物PFT显像图中ST显影清晰（ST／CB=2．18±0．16,n=3）,双侧对称;PD模型大鼠未损毁侧ST放射性浓聚（ST未损毁侧／CB=2．01±0．23,n=3）,而损毁侧ST放射性摄取不明显,与小脑相当（ST损毁侧／CB=1．04±0．05）。结论^18F-FECNT能透过无损的血脑屏障浓聚于ST,对DAT具有高亲和性与特异性,是一种有临床应用潜力的DAT显像剂。     

18F-FECNT的生物分布特性及小动物PET显像研究

Objective 2β-carbomethoxy-3β-(4-corophenyl)-8-(2-18F-fluoroethyl) nortropane (18F-FECNT) is a recently developed dopamine transporter (DAT) imaging agent. The aim of this study was to evaluate its brain biedistribution and to assess its usefulness in quantitation of DAT density in normal and hemiparkinsonian rats. Methods Six groups of mice (5 mice each group) received 18F-FECNT were sacri-ficed at indicated time post injection. Different brain regions (cortex, hippocampus, striatum, cerebellum) were removed, weighed, and countered. DAT blocking effect was investigated in mice pretreated with 2β-Carbomethoxy-3β-(4-fluorpbenyl)tropane (β-CFT) at before 18F-FECNT injection. MicroPET scans were performed in beth normal and unilaterally 6-hydroxydopamine-lesioned rats. Results The brain uptake of 18F-FECNT was 2.22, 1.20, 1.02, 0.78, 0.71, and 0.67 percent injection dose (%ID) at 5, 15, 30, 60, 120, and 180 min post injection. Radioactivity concentration of the striatum, the target region, was the highest in the brain regions and decreased quickly from 5 to 60 min and reached to background at 120 min of post injection. The striatum/cerebellum ratio was 2.56, 3.47, 2.78, 1.63, 0.97, and 0.88 at 5, 15, 30, 60, 120, and 180 min, respectively, post injection. The selective striatum uptake of 18F-FECNT decreased dramatically to the background when the DAT was blocked with β-CFT. The striatum of normal rats in micro-PET exhibited symmetrical (left/right = 1.00±0.05) and the highest uptake of radioactivity (striatum/cere-helium =2.18±0. 16 at 5- 125 min, n =3). As for the hemiparkinsonian rats, nonsymmetrical [unlesioned striatum/cerebellum vs lesioned striatum/cerebellum = 2.01 ± 0.23 (n = 3) vs 1.04 ± 0. 05] and the high-est uptake of radioactivity were also noted. Conclusions The results suggest that 18F-FECNT rapidly pas-ses through blood-brain barrier and locates in stiatal region with high affinity and selectivity to DAT. It is a potential radiotracer to assess the in vivo DAT density in Parkinson's disease.     

18F-FECNT的生物分布特性及小动物PET显像研究

Objective 2β-carbomethoxy-3β-(4-corophenyl)-8-(2-18F-fluoroethyl) nortropane (18F-FECNT) is a recently developed dopamine transporter (DAT) imaging agent. The aim of this study was to evaluate its brain biedistribution and to assess its usefulness in quantitation of DAT density in normal and hemiparkinsonian rats. Methods Six groups of mice (5 mice each group) received 18F-FECNT were sacri-ficed at indicated time post injection. Different brain regions (cortex, hippocampus, striatum, cerebellum) were removed, weighed, and countered. DAT blocking effect was investigated in mice pretreated with 2β-Carbomethoxy-3β-(4-fluorpbenyl)tropane (β-CFT) at before 18F-FECNT injection. MicroPET scans were performed in beth normal and unilaterally 6-hydroxydopamine-lesioned rats. Results The brain uptake of 18F-FECNT was 2.22, 1.20, 1.02, 0.78, 0.71, and 0.67 percent injection dose (%ID) at 5, 15, 30, 60, 120, and 180 min post injection. Radioactivity concentration of the striatum, the target region, was the highest in the brain regions and decreased quickly from 5 to 60 min and reached to background at 120 min of post injection. The striatum/cerebellum ratio was 2.56, 3.47, 2.78, 1.63, 0.97, and 0.88 at 5, 15, 30, 60, 120, and 180 min, respectively, post injection. The selective striatum uptake of 18F-FECNT decreased dramatically to the background when the DAT was blocked with β-CFT. The striatum of normal rats in micro-PET exhibited symmetrical (left/right = 1.00±0.05) and the highest uptake of radioactivity (striatum/cere-helium =2.18±0. 16 at 5- 125 min, n =3). As for the hemiparkinsonian rats, nonsymmetrical [unlesioned striatum/cerebellum vs lesioned striatum/cerebellum = 2.01 ± 0.23 (n = 3) vs 1.04 ± 0. 05] and the high-est uptake of radioactivity were also noted. Conclusions The results suggest that 18F-FECNT rapidly pas-ses through blood-brain barrier and locates in stiatal region with high affinity and selectivity to DAT. It is a potential radiotracer to assess the in vivo DAT density in Parkinson's disease.     

18F-FECNT的生物分布特性及小动物PET显像研究

Objective 2β-carbomethoxy-3β-(4-corophenyl)-8-(2-18F-fluoroethyl) nortropane (18F-FECNT) is a recently developed dopamine transporter (DAT) imaging agent. The aim of this study was to evaluate its brain biedistribution and to assess its usefulness in quantitation of DAT density in normal and hemiparkinsonian rats. Methods Six groups of mice (5 mice each group) received 18F-FECNT were sacri-ficed at indicated time post injection. Different brain regions (cortex, hippocampus, striatum, cerebellum) were removed, weighed, and countered. DAT blocking effect was investigated in mice pretreated with 2β-Carbomethoxy-3β-(4-fluorpbenyl)tropane (β-CFT) at before 18F-FECNT injection. MicroPET scans were performed in beth normal and unilaterally 6-hydroxydopamine-lesioned rats. Results The brain uptake of 18F-FECNT was 2.22, 1.20, 1.02, 0.78, 0.71, and 0.67 percent injection dose (%ID) at 5, 15, 30, 60, 120, and 180 min post injection. Radioactivity concentration of the striatum, the target region, was the highest in the brain regions and decreased quickly from 5 to 60 min and reached to background at 120 min of post injection. The striatum/cerebellum ratio was 2.56, 3.47, 2.78, 1.63, 0.97, and 0.88 at 5, 15, 30, 60, 120, and 180 min, respectively, post injection. The selective striatum uptake of 18F-FECNT decreased dramatically to the background when the DAT was blocked with β-CFT. The striatum of normal rats in micro-PET exhibited symmetrical (left/right = 1.00±0.05) and the highest uptake of radioactivity (striatum/cere-helium =2.18±0. 16 at 5- 125 min, n =3). As for the hemiparkinsonian rats, nonsymmetrical [unlesioned striatum/cerebellum vs lesioned striatum/cerebellum = 2.01 ± 0.23 (n = 3) vs 1.04 ± 0. 05] and the high-est uptake of radioactivity were also noted. Conclusions The results suggest that 18F-FECNT rapidly pas-ses through blood-brain barrier and locates in stiatal region with high affinity and selectivity to DAT. It is a potential radiotracer to assess the in vivo DAT density in Parkinson's disease.