The β-fumarate methyl ester of naltrexone, β-FNA has been reported to be a selective non-equilibrium opiate mu receptor antagonist and reversible kappa receptor agonist in vitro and in vivo. These properties would make β-FNA very useful as a pharmacologic probe. However, the pharmacology of this interesting compound has not yet been characterized extensively. In this work, we have studied β-FNA by observing its overt behavioral effects in drug-naive and morphine-dependent rhesus monkeys. It was compared to the chemically related narcotic antagonist naltrexone. β-FAN appears to reach sites in the central nervous system after systemic administration in small amounts compared to naltrexone; we find β-FNA to be an insurmountable mu receptor-selective antagonist in the rhesus monkey.
|Original language||English (US)|
|Number of pages||7|
|Journal||NIDA Research Monograph Series|
|State||Published - 1985|
ASJC Scopus subject areas
- Medicine (miscellaneous)