Macromerine, normacromerine and bisnormacromerine: Non-psychoactive methylated derivatives of norepinephrine.

Macromerine, normacromerine and bisnormacromerine, O and/or N methylated derivatives of norepinephrine, produce no effect on the conditioned avoidance response (CAR) in rats after IP injection of up to 100 mg/kg of the corresponding hydrochloride. The fate of these compounds was studied by a newly developed assay method utilizing an extraction procedure and the native fluorescence of the compounds. The compounds are rapidly absorbed from the peritoneal cavity, show a half-life of 30 to 60 min in plasma and liver, but remain rather unchanged in the brain during the first hour. Brain levels were found to be between 5 and 30 Μg/g. Since these brain levels are higher than those found for hallucinogenic compounds which do interfere with the CAR we conclude that these compounds are not or less psychoactive than known hallucinogenic substances. [ABSTRACT FROM AUTHOR]