Srinivasan Rajagopal , Mirko Diksic , Barbara Francis , Christopher J. Swain , H.Donald Burns
{"title":"Synthesis of a 11C-labeled novel, quinuclidine based ligand for the 5-HT3 receptor","authors":"Srinivasan Rajagopal , Mirko Diksic , Barbara Francis , Christopher J. Swain , H.Donald Burns","doi":"10.1016/0883-2889(92)90010-C","DOIUrl":null,"url":null,"abstract":"<div><p>L-683,877, a high affinity, 5-HT<sub>3</sub> selective receptor ligand has been labeled with <sup>11</sup>C for use in PET studies to measure regional brain kinetics of L-683,877 and to determine if [<sup>11</sup>C]L-683,877 can be used for serotonin 5-HT<sub>3</sub> receptor imaging. [<sup>11</sup>C]L-683,877 was prepared by reacting [<sup>11</sup>C]methyl iodide with the desmethyl, borane-protected precursor, L-686,472, in DMF in the presence of tetrabutyl ammonium hydroxide. The average specific activity of [<sup>11</sup>C]L-683,877 was 2700 Ci/mmol and the average radiochemical yield (decay uncorrected) was 20% at the end of synthesis (22 min from EOB).</p></div>","PeriodicalId":14288,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2889(92)90010-C","citationCount":"8","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/088328899290010C","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 8
Abstract
L-683,877, a high affinity, 5-HT3 selective receptor ligand has been labeled with 11C for use in PET studies to measure regional brain kinetics of L-683,877 and to determine if [11C]L-683,877 can be used for serotonin 5-HT3 receptor imaging. [11C]L-683,877 was prepared by reacting [11C]methyl iodide with the desmethyl, borane-protected precursor, L-686,472, in DMF in the presence of tetrabutyl ammonium hydroxide. The average specific activity of [11C]L-683,877 was 2700 Ci/mmol and the average radiochemical yield (decay uncorrected) was 20% at the end of synthesis (22 min from EOB).