C. Foulon , D. Guilloteau , J.L. Baulieu , M.J. Ribeiro-Barras , G. Desplanches , Y. Frangin , J.C. Besnard
{"title":"雌激素受体的17α-[123I]碘乙烯基-11β-甲氧基雌二醇(MIVE2)成像-第一部分:放射性示踪剂的制备和表征","authors":"C. Foulon , D. Guilloteau , J.L. Baulieu , M.J. Ribeiro-Barras , G. Desplanches , Y. Frangin , J.C. Besnard","doi":"10.1016/0883-2897(92)90108-B","DOIUrl":null,"url":null,"abstract":"<div><p>It is important to know the estrogen receptor rate in breast carcinoma management. Thus, an <em>in vivo</em> and atraumatic method would be very useful. Different ligands have been proposed for this. We present here the specific synthesis of 20E- and 20Z-17α-iodovinyl-11β-methoxyestradiols and their biological characterization as estrogen receptor ligands. The two isomers were analysed by current chemical methods (NMR) and purified by HPLC. We carried out an <em>in vivo</em> study with 21-day-old Swiss mice to compare properties of the two ligands. The 20E-MIVE<sub>2</sub> showed the best affinity for estrogen receptors, the uterus-to-blood ratio was 15-fold higher for the <em>trans</em> derivative. We enhanced the <em>in vivo</em> and <em>in vitro</em> properties of the 20E-MIVE<sub>2</sub>: the affinity constant was determined by Scatchard analysis, <em>K</em><sub><em>d</em></sub> = 16 × 10<sup>−10</sup>M, and biodistributions were performed with unlabelled estradiol pre-injection. We concluded that 20E-MIVE<sub>2</sub> can be used for a feasibility study in patients with breast carcinoma.</p></div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 3","pages":"Pages 257-261"},"PeriodicalIF":0.0000,"publicationDate":"1992-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90108-B","citationCount":"16","resultStr":"{\"title\":\"Estrogen receptor imaging with 17α-[123I]iodovinyl-11β-methoxyestradiol (MIVE2)—part I. Radiotracer preparation and characterization\",\"authors\":\"C. Foulon , D. Guilloteau , J.L. Baulieu , M.J. Ribeiro-Barras , G. Desplanches , Y. Frangin , J.C. Besnard\",\"doi\":\"10.1016/0883-2897(92)90108-B\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>It is important to know the estrogen receptor rate in breast carcinoma management. Thus, an <em>in vivo</em> and atraumatic method would be very useful. Different ligands have been proposed for this. We present here the specific synthesis of 20E- and 20Z-17α-iodovinyl-11β-methoxyestradiols and their biological characterization as estrogen receptor ligands. The two isomers were analysed by current chemical methods (NMR) and purified by HPLC. We carried out an <em>in vivo</em> study with 21-day-old Swiss mice to compare properties of the two ligands. The 20E-MIVE<sub>2</sub> showed the best affinity for estrogen receptors, the uterus-to-blood ratio was 15-fold higher for the <em>trans</em> derivative. We enhanced the <em>in vivo</em> and <em>in vitro</em> properties of the 20E-MIVE<sub>2</sub>: the affinity constant was determined by Scatchard analysis, <em>K</em><sub><em>d</em></sub> = 16 × 10<sup>−10</sup>M, and biodistributions were performed with unlabelled estradiol pre-injection. We concluded that 20E-MIVE<sub>2</sub> can be used for a feasibility study in patients with breast carcinoma.</p></div>\",\"PeriodicalId\":14328,\"journal\":{\"name\":\"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology\",\"volume\":\"19 3\",\"pages\":\"Pages 257-261\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0883-2897(92)90108-B\",\"citationCount\":\"16\",\"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/088328979290108B\",\"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/088328979290108B","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Estrogen receptor imaging with 17α-[123I]iodovinyl-11β-methoxyestradiol (MIVE2)—part I. Radiotracer preparation and characterization
It is important to know the estrogen receptor rate in breast carcinoma management. Thus, an in vivo and atraumatic method would be very useful. Different ligands have been proposed for this. We present here the specific synthesis of 20E- and 20Z-17α-iodovinyl-11β-methoxyestradiols and their biological characterization as estrogen receptor ligands. The two isomers were analysed by current chemical methods (NMR) and purified by HPLC. We carried out an in vivo study with 21-day-old Swiss mice to compare properties of the two ligands. The 20E-MIVE2 showed the best affinity for estrogen receptors, the uterus-to-blood ratio was 15-fold higher for the trans derivative. We enhanced the in vivo and in vitro properties of the 20E-MIVE2: the affinity constant was determined by Scatchard analysis, Kd = 16 × 10−10M, and biodistributions were performed with unlabelled estradiol pre-injection. We concluded that 20E-MIVE2 can be used for a feasibility study in patients with breast carcinoma.
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