Native inhabitants of north-eastern Mexico around 810–1070 CE (according to carbon dating) are thought to have used a number of "mescal buttons" (peyote plant material) containingmescaline, pellotine, and other related alkaloids. While it is known that thecytisine-containing "mescal beans" were at least ornamental, it is unclear whether "mescal buttons" were ornamental or used for their psychoactive effects.[10]
^Gabermann, V (1978). "Estimation of mescaline and pellotine inLophophora coulter plants (Cactaceae) by means of the oscillographic polarography".Biokhimiia (Moscow, Russia).43 (2):246–51.PMID647075.
^abcJones, Peter (2007). "The American Indian Church and its sacramental use of peyote: A review for professionals in the mental-health arena".Mental Health, Religion & Culture.8 (4):277–290.doi:10.1080/13674670412331304348.S2CID144932041.
^abcShulgin AT (March 1973)."Mescaline: the chemistry and pharmacology of its analogs".Lloydia.36 (1):46–58.PMID4576313.The pharmacological action of peyotline in human subjects is one of calming or sedation, rather than that of a hallucinogen. Jolly (14) has reported the production of an uneventful sleep in patients with a dosage of SO mg. At levels of as much as 240 mg (total dosage) there are no indications of sensory distortions (5). There is a dizziness and a generalized tiredness that undergoes a gentle transition into sleep. This latter quantity of drug is greater than that which would be encountered in a single dosage unit of peyote. It is certainly possible that peyotline could contribute to the pharmacological picture associated with peyote as this sedative action is noted at levels that might well be encountered in the total cactus. At low levels in man (15-30 mg) there has been described a calming effect, without overt hypnosis (14).
^abMangner TJ (1978).Potential Psychotomimetic Antagonists. N,n -diethyl-1-methyl-3-aryl-1, 2, 5, 6-tetrahydropyridine-5-carboxamides (Ph.D. thesis). University of Michigan.doi:10.7302/11268. Archived fromthe original on 30 March 2025.In addition to compounds strictly related to mescaline just described, L. williamsii also contains at least 23 variously substituted tetrahydroisoquinolines,95 of which four have been clinically tested. The two phenolic tetrahydroisoquinolines peyotline (63a) and anhalonidine (63b) were found to produce no sensory distortions, characteristic of the effects of mescaline, at doses of up to 250 mg.98 These compounds appear to induce a calming or sedative effect rather than a psychotomimetic one. Two methylenedioxy tetrahydroisoquinolines, lophophorine (64a) and anhalonine (64b), were also found to lack any psychotomimetic-type effects.98
^Chan CB, Pottie E, Simon IA, Rossebø AG, Herth MM, Harpsøe K, Kristensen JL, Stove CP, Poulie CB (February 2025). "Synthesis, Pharmacological Characterization, and Binding Mode Analysis of 8-Hydroxy-Tetrahydroisoquinolines as 5-HT7 Receptor Inverse Agonists".ACS Chem Neurosci.16 (3):439–451.doi:10.1021/acschemneuro.4c00667.PMID39836645.
^El-Seedi, Hesham R.;De Smet, Peter A. G. M.; Beck, Olof; Possnert, Göran; Bruhn, Jan G. (2005-10-03). "Prehistoric peyote use: Alkaloid analysis and radiocarbon dating of archaeological specimens ofLophophora from Texas".Journal of Ethnopharmacology.101 (1):238–242.doi:10.1016/j.jep.2005.04.022.ISSN0378-8741.PMID15990261.