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中枢神经系统D-2多巴胺受体的体内单光子发射计算机断层扫描成像:用碘-123-碘苄胍对人体的初步研究。

In vivo SPECT imaging of CNS D-2 dopamine receptors: initial studies with iodine-123-IBZM in humans.

作者信息

Kung H F, Alavi A, Chang W, Kung M P, Keyes J W, Velchik M G, Billings J, Pan S, Noto R

机构信息

Department of Radiology, University of Pennsylvania, Philadelphia.

出版信息

J Nucl Med. 1990 May;31(5):573-9.

PMID:2140408
Abstract

Iodobenzamide (IBZM) is a D-2 dopamine receptor antagonist. In this paper the results of Phase I clinical studies of iodine-123-(123I)IBZM in humans are reported. Preliminary imaging studies, both planar and single-photon emission tomography (SPECT), of no-carrier added [123I]IBZM in humans show specific localization in the basal ganglia of the brain. At 2 hr after an i.v. injection, the brain uptake was 3.72% of the dose, and at 20 hr later the uptake diminished to 0.7%. Radiation dosimetry calculation indicated that the radiation dose to the brain was minimum, 0.039 rad/mCi, while the large intestine wall received the highest dose, 0.28 mrad/mCi. The radiation dosimetry and pharmacology data suggest that this agent is safe for human use.

摘要

碘苯甲酰胺(IBZM)是一种D-2多巴胺受体拮抗剂。本文报道了碘-123-(123I)IBZM在人体的I期临床研究结果。对人体中无载体添加的[123I]IBZM进行的初步成像研究,包括平面成像和单光子发射断层扫描(SPECT),显示其在大脑基底神经节中有特异性定位。静脉注射后2小时,脑部摄取量为给药剂量的3.72%,20小时后摄取量降至0.7%。辐射剂量学计算表明,脑部的辐射剂量最低,为0.039拉德/毫居里,而大肠壁接受的剂量最高,为0.28毫拉德/毫居里。辐射剂量学和药理学数据表明,该药物对人体使用是安全的。

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In vivo SPECT imaging of CNS D-2 dopamine receptors: initial studies with iodine-123-IBZM in humans.中枢神经系统D-2多巴胺受体的体内单光子发射计算机断层扫描成像:用碘-123-碘苄胍对人体的初步研究。
J Nucl Med. 1990 May;31(5):573-9.
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J Nucl Med. 1989 Jan;30(1):88-92.
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[In vivo characteristics of IBZM in rat brains: an agent for quantitative SPECT imaging of dopamine D2 receptors. Preparation of 125I-IBZM and its biodistribution and kinetic properties].
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