Molecular Pharmacology, Vol 9, 41-50, Copyright © 1973 by the American Society for Pharmacology and Experimental Therapeutics

Inhibition of Axoplasmic Transport by Mescaline and Other Trimethoxyphenylalkylamines

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

Following an intraocular injection of [³H]L-proline, fast axoplasmic transport can be demonstrated in the rat optic system by a flow of ³H-labeled protein which moves from the ganglion cells of the retina at a rate of approximately 16 mm/hr. The injection of mescaline or one of several trimethoxyphenylalkylamines inhibits the transport of labeled proteins through the optic nerve. By using one eyeball containing the drug as the experimental eye and the contralateral eye as a control, the degree of inhibition may be determined quantitatively, allowing evaluation of dose-response curves. Dose-response curves for the inhibition of axoplasmic transport by mescaline, 1-(3,4,5-trimethoxyphenyl)-2-aminopropane, and 1-(2,4,5-trimethoxyphenyl)-2-aminopropane have been obtained. Further experiments with mescaline indicate that (a) the inhibition of fast axoplasmic transport produced by mescaline in the rat optic system is reversible, (b) mescaline inhibits transport when applied directly to the cat sciatic nerve, and (c) mixtures of component pieces of the molecular skeleton of mescaline, trimethoxybenzene and ethylamine, have little activity as inhibitors of fast axoplasmic transport in either the rat optic or cat sciatic nerves. Several of the agents found effective as inhibitors of axoplasmic transport are known hallucinogens. The hallucinogenic potencies of these drugs rank in the same order as their effectiveness as antitransport agents.