大鼠脑内放射性配体特异性结合的体内测量的长期可重复性。

Long-term reproducibility of in vivo measures of specific binding of radioligands in rat brain.

作者信息

Kilbourn Michael R

机构信息

Division of Nuclear Medicine, Department of Radiology, University of Michigan Medical School, Ann Arbor, MI 48109, USA.

出版信息

Nucl Med Biol. 2004 Jul;31(5):591-5. doi: 10.1016/j.nucmedbio.2004.02.003.

DOI:10.1016/j.nucmedbio.2004.02.003

PMID:15219277

Abstract

The long-term reproducibility of measures of in vivo specific binding of radiolabeled forms of (+)-alpha-dihydrotetrabenazine (DTBZ) and d-threo-methylphenidate (MPH) in rat brain was examined. All studies were done using a consistent bolus plus infusion protocol and calculation of equilibrium distribution volume ratios (DVR). Over a period of eight years striatal DVR values for DTBZ binding to the vesicular monoamine transporter 2 (VMAT2) in young adult (8-10 wks old) rats showed very good reproducibility (3.62+/-0.33, N=35). Equivalent values were obtained using either tritiated or carbon-11 labeled DTBZ, and were irrespective of sex of animals. Older animals (78 wks old) showed losses (-45%) of specific binding. Striatal binding of MPH to the dopamine transporter (DAT) showed a similar reproducibility over a five year period (DVR=2.17+/-0.39, N=52), again irrespective of radionuclide or sex. These studies demonstrate that use of a consistent in vivo technique can provide reliable measures of specific binding of radioligands to high affinity sites in the rat brain.

摘要

研究了放射性标记的（+）-α-二氢丁苯那嗪（DTBZ）和d-苏式-甲基苯丙胺（MPH）在大鼠脑内体内特异性结合测量的长期可重复性。所有研究均采用一致的推注加输注方案以及平衡分布容积比（DVR）计算。在八年的时间里，年轻成年（8 - 10周龄）大鼠中DTBZ与囊泡单胺转运体2（VMAT2）结合的纹状体DVR值显示出非常好的可重复性（3.62±0.33，N = 35）。使用氚标记或碳-11标记的DTBZ均可获得等效值，且与动物性别无关。老年动物（78周龄）显示特异性结合丧失（-45%）。MPH与多巴胺转运体（DAT）的纹状体结合在五年期间显示出类似的可重复性（DVR = 2.17±0.39，N = 52），同样与放射性核素或性别无关。这些研究表明，使用一致的体内技术可以提供放射性配体与大鼠脑内高亲和力位点特异性结合的可靠测量。