Synthesis and biological evaluation of a 13N-labeled opioid peptide

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-05-01 DOI:10.1016/0883-2897(92)90160-Z

Hideo Saji , Daisuke Tsutsumi , Yoshiaki Kiso , Satoshi Iimuma , Tsutomu Mimoto , Kenichi Akaji , Yasuhiro Magata , Hideo Nakamura , Atsuko Kita , Junji Konishi , Akira Yokoyama

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引用次数: 4

Abstract

The ¹³N-labeled opioid tetrapeptide, Tyr-D-Met(O)-Phe-Gly-[¹³N]NH₂ (SD-62), was synthesized by amidation of its activated p-nitrophenol ester with [¹³N]ammonia (total synthesis time: 25 min, radiochemical yield: 48%). When injected intravenously into mice, [¹³N]SD-62 was taken up by the brain and this uptake was blocked by naloxone. In addition, the time course of changes in brain radioactivity paralleled that of the analgesic activity of this compound, suggesting that SD-62 underwent binding to brain opioid receptors. Thus, [¹³N]SD-62 appears to hold some promise for use as a radiopharmaceutical for in vivo studies of opioid peptide behavior, using positron emission tomography.

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13n标记阿片肽的合成及生物学评价

13N标记的阿片四肽，Tyr-D-Met(O)- ph - gly -[13N]NH2 (SD-62)，由其活化的对硝基酚酯与[13N]氨酰胺化合成，总合成时间为25 min，放射化学产率为48%。当静脉注射到小鼠体内时，[13N]SD-62被大脑摄取，这种摄取被纳洛酮阻断。此外，脑放射性变化的时间过程与该化合物的镇痛活性变化相似，表明SD-62与脑阿片受体结合。因此，[13N]SD-62似乎有望作为一种放射性药物，利用正电子发射断层扫描技术在体内研究阿片肽的行为。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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

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