S‐[18F]Acetylcyclofoxy: a useful probe for the visualization of opiate receptors in living animals
- 5 November 1984
- journal article
- Published by Wiley in FEBS Letters
- Vol. 177 (2) , 281-286
- https://doi.org/10.1016/0014-5793(84)81300-9
Abstract
A fluoro-analogue of the potent narcotic antagonist, naltrexone, was synthesized and shown to bind with high affinity to opiate receptors in vitro. 3-[18F]acetylcyclofoxy was prepared via a one-step Inflate displacement reaction with the positron emitting 18F ion from tetraethylammonium [18F]fluoride. 3-[18F]acetylcyclofoxy accumulation in opiate receptor rich brain regions of both rat and baboon is shown to be completely displaced by the active enantiomer ofnaloxone ((−)-naloxone) while the identical dose of the pharmacologically inert(+)-naloxone has no detectable effect. Moreover, both rat and baboon brain showed the well documented, typical opiate receptor distribution so that basal ganglia and thalamus are clearly visible in the living baboon brain up to 95 min after intravenous injection of 3-[18F]acetylcyclofoxy. We expect that 3-[18F]acetylcyclofoxy will be a useful probe for visualizing opiate receptors in living humans.Opiate receptorPET3-[18F]AcetylcyclofoxyStereospecificityNaloxonKeywords
This publication has 21 references indexed in Scilit:
- A new method for receptor autoradiography: [3H]Opioid receptors in rat brainBrain Research, 1979
- Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxoneJournal of Medicinal Chemistry, 1978
- Stereospecific and Nonstereospecific Effects of (+)- and (—)-Morphine: Evidence for a New Class of Receptors?Science, 1977
- Correlation of opiate receptor affinity with analgetic effects of meperidine homologsJournal of Medicinal Chemistry, 1976
- Identification of opiate receptor binding in intact animalsLife Sciences, 1975
- Homologous N-alkylnorketobemidones. Correlation of receptor binding with analgesic potencyJournal of Medicinal Chemistry, 1975
- Regional Distribution of Opiate Receptor Binding in Monkey and Human BrainNature, 1973
- Stereospecific Interaction Between Narcotic Analgesics and a Synaptic Plasma Membrane Fraction of Rat Cerebral CortexActa Pharmacologica et Toxicologica, 1973
- Opiate Receptor: Demonstration in Nervous TissueScience, 1973
- Stereospecific and Nonspecific Interactions of the Morphine Congener Levorphanol in Subcellular Fractions of Mouse BrainProceedings of the National Academy of Sciences, 1971