6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo.
6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo.
复制标题
6-O-(2-[18F]氟乙基)-6-O-去甲基-二丙诺啡 ([18F]FE-DPN) 在体内优先与 Mu 阿片受体结合。
DOI：
10.1007/s11307-022-01767-5
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发表时间：
2023
影响因子：
3.1
通讯作者：
Michaelides,Michael
中科院分区：
文献类型：
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作者：
Levinstein,MarjorieR;Ventriglia,EmilyaN;Gomez,JuanL;Budinich,ReeceC;Marton,János;Henriksen,Gjermund;Holt,DanielP;Dannals,RobertF;Pomper,MartinG;ZarateJr,CarlosA;Bonaventura,Jordi;Michaelides,Michael
目的6-O-（2-[18F]氟乙基）-6-O-去甲基-二丙诺啡[18 F]FE-DPN是一种非选择性阿片受体放射性示踪剂，本文报道了由新型前体6-O-[18 F]FE-DPN合成的[18 F]FE-DPN的首次表征。（2-甲苯磺酰氧基乙氧基）-6-O-去甲基-3-O-三苯甲基-二丙诺啡（TE-TDDPN），使用一锅法，两步亲核放射合成成像阿片受体在大鼠和小鼠使用正电子发射断层扫描。结果我们还表明，[18 F]FE-DPN和[3 H] DPN在小鼠脑中的摄取可忽略不计，与以前的研究结果一起，我们的结果表明，[18 F]FE-DPN和[3 H]DPN优先结合在啮齿动物体内莫尔。
Purpose6-O-(2-[18F]Fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) is regarded as a non-selective opioid receptor radiotracer.ProcedureHere, we report the first characterization of [18F]FE-DPN synthesized from the novel precursor, 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3-O-trityl-diprenorphine (TE-TDDPN), using a one-pot, two-step nucleophilic radiosynthesis to image opioid receptors in rats and mice using positron emission tomography.ResultsWe also show that [18F]FE-DPN and [3H]DPN exhibit negligible brain uptake in mu opioid receptor (MOR) knockout mice.ConclusionsTaken together with prior findings, our results suggest that [18F]FE-DPN and [3H]DPN preferentially bind to MOR in rodentsin vivo.