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用于活体人脑多巴胺转运体成像的碘-123标记的2β-甲氧羰基-3β-(4-碘苯基)托烷与2β-甲氧羰基-3β-(4-碘苯基)-N-(3-氟丙基)去甲托烷的比较

Comparison of iodine-123 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane and 2 beta-carbomethoxy-3 beta-(4-iodophenyl)-N-(3-fluoropropyl)nortropane for imaging of the dopamine transporter in the living human brain.

作者信息

Kuikka J T, Bergström K A, Ahonen A, Hiltunen J, Haukka J, Länsimies E, Wang S, Neumeyer J L

机构信息

Department of Clinical Physiology, Kuopio University Hospital, Finland.

出版信息

Eur J Nucl Med. 1995 Apr;22(4):356-60. doi: 10.1007/BF00941854.

DOI:10.1007/BF00941854
PMID:7607268
Abstract

Several cocaine congeners are of potential for imaging the dopamine transporter (DAT). Previous studies have shown that iodine-123 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane ([123I] beta-CIT) is a promising radiotracer for imaging the serotonin (5-HT) and dopamine (DA) transporters in the living human brain with single-photon emission tomography (SPET). [123I] beta-CIT was found to be not very practical for 1-day DAT imaging protocols since peak DAT uptake occurs later than 8 h. Here we report a pilot comparison of [123I] beta-CIT and 2 beta-carbomethoxy-3 beta-(4-iodophenyl)-N-(3-fluoropropyl)nortropane ([123I] beta-CIT-FP), using SPET imaging in four healthy male subjects. Peak uptake of [123I] beta-CIT-FP into the basal ganglia occurred earlier (3-4 h after injection of tracer) than that of [123I] beta-CIT (> 8 h). However, the specific DAT binding of [123I] beta-CIT-FP in the basal ganglia was somewhat less (0.813 +/- 0.047) than that of [123I] beta-CIT (0.922 +/- 0.004). Imaging quality is excellent with both tracers and they are potentially of value for brain imaging in various neuropsychiatric disorders.

摘要

几种可卡因同系物具有用于多巴胺转运体(DAT)成像的潜力。先前的研究表明,碘-123标记的2β-甲氧羰基-3β-(4-碘苯基)托烷([123I]β-CIT)是一种很有前景的放射性示踪剂,可用于通过单光子发射断层扫描(SPET)对活体人脑中的5-羟色胺(5-HT)和多巴胺(DA)转运体进行成像。[123I]β-CIT被发现对于1日DAT成像方案不太实用,因为DAT摄取峰值出现在8小时之后。在此我们报告了在四名健康男性受试者中使用SPET成像对[123I]β-CIT和2β-甲氧羰基-3β-(4-碘苯基)-N-(3-氟丙基)去甲托烷([123I]β-CIT-FP)进行的初步比较。[123I]β-CIT-FP在基底神经节中的摄取峰值出现得比[123I]β-CIT更早(注射示踪剂后3 - 4小时)(> 8小时)。然而,[123I]β-CIT-FP在基底神经节中的特异性DAT结合略低于[123I]β-CIT(0.813±0.047)(0.922±0.004)。两种示踪剂的成像质量都很好,它们在各种神经精神疾病的脑成像中可能具有价值。

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Comparison of iodine-123 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane and 2 beta-carbomethoxy-3 beta-(4-iodophenyl)-N-(3-fluoropropyl)nortropane for imaging of the dopamine transporter in the living human brain.用于活体人脑多巴胺转运体成像的碘-123标记的2β-甲氧羰基-3β-(4-碘苯基)托烷与2β-甲氧羰基-3β-(4-碘苯基)-N-(3-氟丙基)去甲托烷的比较
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本文引用的文献

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Single photon emission computed tomographic imaging demonstrates loss of striatal dopamine transporters in Parkinson disease.单光子发射计算机断层扫描成像显示帕金森病患者纹状体多巴胺转运体缺失。
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Initial experience with single-photon emission tomography using iodine-123-labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl) tropane in human brain.使用碘-123标记的2β-甲氧基羰基-3β-(4-碘苯基)托烷进行人脑单光子发射断层扫描的初步经验。
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N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters.
用于成像单胺转运体(多巴胺、5-羟色胺和去甲肾上腺素)的氟-18放射性标记正电子发射断层显像剂
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Quantification of [123I]FP-CIT SPECT brain images: an accurate technique for measurement of the specific binding ratio.[123I]FP-CIT单光子发射计算机断层扫描(SPECT)脑图像的定量分析:一种测量特异性结合率的精确技术。
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IBZM tool: a fully automated expert system for the evaluation of IBZM SPECT studies.IBZM工具:用于评估IBZM单光子发射计算机断层扫描研究的全自动专家系统。
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Iodine-123 labelled radiopharmaceuticals and single-photon emission tomography: a natural liaison.碘-123标记的放射性药物与单光子发射断层扫描:一种天然的结合。
Eur J Nucl Med. 1997 Mar;24(3):331-44. doi: 10.1007/BF01728774.
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Relationship between clinical features of Parkinson's disease and presynaptic dopamine transporter binding assessed with [123I]IPT and single-photon emission tomography.帕金森病临床特征与通过[123I]IPT和单光子发射断层扫描评估的突触前多巴胺转运体结合之间的关系
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[123I]FP-CIT SPECT shows a pronounced decline of striatal dopamine transporter labelling in early and advanced Parkinson's disease.[123I]FP - CIT单光子发射计算机断层扫描显示,在早期和晚期帕金森病中,纹状体多巴胺转运体标记明显减少。
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Eur J Nucl Med. 1997 Jan;24(1):68-71. doi: 10.1007/BF01728311.
10
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Eur J Nucl Med. 1995 Jul;22(7):682-6. doi: 10.1007/BF01254571.
(1R)-2β-甲氧羰基-3β-(4-碘苯基)-托烷(β-CIT)的N-ω-氟烷基类似物:用于多巴胺转运体正电子发射断层扫描和单光子发射计算机断层扫描成像的放射性示踪剂。
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PET study of [11C]beta-CIT binding to monoamine transporters in the monkey and human brain.[11C]β-CIT与猴脑和人脑单胺转运体结合的正电子发射断层扫描(PET)研究。
Synapse. 1994 Feb;16(2):93-103. doi: 10.1002/syn.890160203.
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SPECT imaging of dopamine and serotonin transporters with [123I]beta-CIT. Binding kinetics in the human brain.用[123I]β-CIT对多巴胺和5-羟色胺转运体进行单光子发射计算机断层扫描成像。人脑内的结合动力学。
J Neural Transm Gen Sect. 1993;94(2):137-46. doi: 10.1007/BF01245007.
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The dosimetry of iodine-123 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane.碘-123标记的2β-甲氧基羰基-3β-(4-碘苯基)托烷的剂量测定法
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Single-photon emission tomography imaging of dopamine terminal innervation: a potential clinical tool in Parkinson's disease.多巴胺终末神经支配的单光子发射断层扫描成像:帕金森病的一种潜在临床工具。
Eur J Nucl Med. 1994 Jan;21(1):1-5. doi: 10.1007/BF00182298.
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Graphical, kinetic, and equilibrium analyses of in vivo [123I] beta-CIT binding to dopamine transporters in healthy human subjects.健康人类受试者体内[123I]β-CIT与多巴胺转运体结合的图像、动力学和平衡分析。
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Lipophilic metabolite of [123I]beta-CIT in human plasma may obstruct quantitation of the dopamine transporter.人血浆中[123I]β-CIT的亲脂性代谢物可能会妨碍多巴胺转运体的定量分析。
Synapse. 1995 Apr;19(4):297-300. doi: 10.1002/syn.890190407.
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Regional brain uptake and pharmacokinetics of [123I]N-omega-fluoroalkyl-2 beta-carboxy-3 beta-(4-iodophenyl)nortropane esters in baboons.狒狒体内[123I]N-ω-氟烷基-2β-羧基-3β-(4-碘苯基)降托烷酯的脑区摄取及药代动力学
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