Rothman R B, McLean S
Laboratory of Preclinical Pharmacology, National Institute of Mental Health, Bethesda, MD 20892.
Biol Psychiatry. 1988 Mar 1;23(5):435-58. doi: 10.1016/0006-3223(88)90016-9.
17-Cyclopropylmethyl-3,14-dihydroxy-4,5-alpha-epoxy-6-beta-fluoromorp hinan (cycloFOXY) is a fluorinated derivative of naltrexone suitable for labeling opiate receptors using positron emission transaxial tomography. Using the quantitative ligand binding method "binding surface analysis," in vitro autoradiography, and site-directed alkylating agents, [3H]cycloFOXY is shown to label mu and kappa opiate binding sites in vitro. Similar results were obtained using [3H]naloxone. Additional experiments demonstrate that [3H]cycloFOXY administered in vivo also labels mu and kappa binding sites. The relevance of these findings are discussed from clinical and basic science perspectives.
17-环丙基甲基-3,14-二羟基-4,5-α-环氧-6-β-氟吗啡喃（环丙氟氧吗啡）是纳曲酮的一种氟化衍生物，适用于使用正电子发射断层扫描标记阿片受体。采用定量配体结合方法“结合表面分析”、体外放射自显影和定点烷基化剂，[3H]环丙氟氧吗啡在体外显示可标记μ和κ阿片结合位点。使用[3H]纳洛酮也获得了类似结果。额外实验表明，体内给予的[3H]环丙氟氧吗啡也能标记μ和κ结合位点。从临床和基础科学角度讨论了这些发现的相关性。
