Molecular Pharmacology, Vol 10, 419-424, Copyright © 1974 by the American Society for Pharmacology and Experimental Therapeutics

The Lack of Correlation between Hallucinogenesis and Inhibition of Axoplasmic Transport

¹ Department of Biochemistry, University of Illinois, Urbana, Illinois 61801

Several hallucinogenic indoles were examined for an inhibitory effect upon fast axoplasmic transport of proteins in the optic system of the anesthetized rat. No inhibition was produced by milligram levels of lysergide or N,N-dimethyltryptamine, although some derivatives of N,N-dimethyltryptamine produced partial inhibition at this dose. Harmaline and 6-methoxylharmalan, which are poor hallucinogens, are active as inhibitors of transport. The hallucinogenic compound R(-)-1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane and its nonhallucinogenic enantiomer were also tested for antitransport activity in a system in vitro which utilized the rat sciatic nerve. Both enantiomers are effective inhibitors of axoplasmic transport. It is concluded that inhibition of axoplasmic transport is not correlated with hallucinogenesis, even though a good correlation of these parameters has previously been observed in studies of a series of structurally related derivatives of mescaline.