CGP-12177和CGP-26505在β-肾上腺素受体定量成像中的适用性

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-10-01 DOI:10.1016/0883-2897(92)90130-Q

Aren van Waarde , Joan G. Meeder , Paul K. Blanksma , Jaap Bouwer , Gerben M. Visser , Philip H. Elsinga , Anne M.J. Paans , Willem Vaalburg , Kong I. Lie

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引用次数: 26

摘要

[3H]CGP-12177(非选择性β-肾上腺素能受体拮抗剂)和[3H]CGP-26505 (β1-选择性β-肾上腺素能受体拮抗剂)静脉给予大鼠。注射后10 ~ 40 min, CGP-12177的总/非特异性结合率分别为5.4和6.9,CGP-26505的总/非特异性结合率分别为2.0和2.8。标记血浆代谢物出现在20分钟后(CGP-12177)或2分钟内(CGP-26505)。在心脏中未发现代谢物。CGP-12177能与血细胞结合，但CGP-26505不能。CGP-12177可用于实验动物心肺总(β1和β2)肾上腺素受体的PET成像，但CGP-26505不太适合用于β1亚群的体内分析。

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Suitability of CGP-12177 and CGP-26505 for quantitative imaging of β-adrenoceptors

[³H]CGP-12177, a non-selective β-adrenoceptor antagonist, and [³H]CGP-26505, a β₁-selective β-adrenoceptor antagonist, were intravenously administered to rats. 94–97% of the injected radioactivity disappeared from plasma with $t_{12}$ 0.2 and 0.5 min. Total/non-specific binding ratios of 5.4 and 6.9 (CGP-12177) or 2.0 and 2.8 (CGP-26505) were maintained in heart and lung from 10 to 40 min post-injection. Labelled plasma metabolites appeared after >20 min (CGP-12177) or within 2 min (CGP-26505). No metabolites were found in the heart. CGP-12177 binds to blood cells, but CGP-26505 does not. CGP-12177 can be used for PET imaging of total (β₁, and β₂) adrenoceptors in the heart and lung of experimental animals, but CGP-26505 is less suitable for in vivo analysis of the β₁-subpopulation.

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International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology

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