Summary
Two behavioural indices for psychotomimetic activity have been used to elucidate the probable role of methoxy group configuration in the mescaline molecule. The first method using a shuttle box CAR has been reported previously in this series. The second is based on the Sidman Avoidance schedule and utilizes the Bovet-Gatti profiles. Our results indicate that only two analogues of mescaline are active-the 2,3,4,5 and 2,3,4,5,6 compounds. This indicates that the 3,4,5 configuration is necessary and that adding extra methoxy groups increases activity. The great activity of the penta methoxy compound may be due to the fact that this compound substituted in the 2 and 6 positions cannot be metabolized by mescaline oxidase. The significance of these results is discussed.
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Smythies, J.R., Bradley, R.J., Johnston, V.S. et al. Structure-activity relationship studies on mescaline. Psychopharmacologia 10, 379–387 (1967). https://doi.org/10.1007/BF00403978
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DOI: https://doi.org/10.1007/BF00403978