{"title":"13n标记阿片肽的合成及生物学评价","authors":"Hideo Saji , Daisuke Tsutsumi , Yoshiaki Kiso , Satoshi Iimuma , Tsutomu Mimoto , Kenichi Akaji , Yasuhiro Magata , Hideo Nakamura , Atsuko Kita , Junji Konishi , Akira Yokoyama","doi":"10.1016/0883-2897(92)90160-Z","DOIUrl":null,"url":null,"abstract":"<div><p>The <sup>13</sup>N-labeled opioid tetrapeptide, Tyr-<span>D</span>-Met(<em>O</em>)-Phe-Gly-[<sup>13</sup>N]NH<sub>2</sub> (SD-62), was synthesized by amidation of its activated <em>p</em>-nitrophenol ester with [<sup>13</sup>N]ammonia (total synthesis time: 25 min, radiochemical yield: 48%). When injected intravenously into mice, [<sup>13</sup>N]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, [<sup>13</sup>N]SD-62 appears to hold some promise for use as a radiopharmaceutical for <em>in vivo</em> studies of opioid peptide behavior, using positron emission tomography.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 4","pages":"Pages 455-460"},"PeriodicalIF":0.0000,"publicationDate":"1992-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90160-Z","citationCount":"4","resultStr":"{\"title\":\"Synthesis and biological evaluation of a 13N-labeled opioid peptide\",\"authors\":\"Hideo Saji , Daisuke Tsutsumi , Yoshiaki Kiso , Satoshi Iimuma , Tsutomu Mimoto , Kenichi Akaji , Yasuhiro Magata , Hideo Nakamura , Atsuko Kita , Junji Konishi , Akira Yokoyama\",\"doi\":\"10.1016/0883-2897(92)90160-Z\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The <sup>13</sup>N-labeled opioid tetrapeptide, Tyr-<span>D</span>-Met(<em>O</em>)-Phe-Gly-[<sup>13</sup>N]NH<sub>2</sub> (SD-62), was synthesized by amidation of its activated <em>p</em>-nitrophenol ester with [<sup>13</sup>N]ammonia (total synthesis time: 25 min, radiochemical yield: 48%). When injected intravenously into mice, [<sup>13</sup>N]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, [<sup>13</sup>N]SD-62 appears to hold some promise for use as a radiopharmaceutical for <em>in vivo</em> studies of opioid peptide behavior, using positron emission tomography.</p></div>\",\"PeriodicalId\":14328,\"journal\":{\"name\":\"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology\",\"volume\":\"19 4\",\"pages\":\"Pages 455-460\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0883-2897(92)90160-Z\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/088328979290160Z\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/088328979290160Z","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and biological evaluation of a 13N-labeled opioid peptide
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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