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It is a small, spineless cactus that grows in clusters, produces edible fruits, and contains psychoactive alkaloids—primarily mescaline—at concentrations of about 0.4% when fresh and up to 6% when dried.
Abstract
Peyote (Lophophora williamsii) is a cactus that contains various biologically active alkaloids—such as pellotine, anhalonidine, hordenine and mescaline. Here, mescaline induces the psychoactive effects of peyote through the activation of the serotonin 5-HT2A receptor and the subsequent release of calcium (Ca2+) from the endoplasmic reticulum (ER). Moreover, an evaluation of the therapeutic benefits of mescaline is also currently the subject of research. It is important to consider that the outcome of taking a psychedelic drug strongly depends on the mindset of the recipient and the context (set and setting principle), including ceremonies and culture. This overview serves to summarise the current state of the knowledge of the metabolism, mechanism of action and clinical application studies of peyote and mescaline. Furthermore, the benefits of the potential of peyote and mescaline are presented in a new light, setting an example for combining a form of treatment embedded in nature and ritually enriched with our current highly innovative Western medicine.
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The history of peyote research begins with botanical studies from the 1840s and the listing of peyote in the Mexican pharmacopoeia [14]. Subsequently, in 1887, John Raleigh Briggs published the first study on the effects of mescal buttons [14]. Since then, research into the constituents (e.g., the main alkaloids: mescaline, pellotine, anhalonidine and hordenine), the biological effects and the biosynthesis of the active alkaloids progressed rapidly. The German pharmacologist Louis Lewin (1850–1929) and the chemist and physician Arthur Heffter (1860–1925), as well as the Merck Laboratory in Darmstadt, Germany, provided the decisive insights into alkaloid isolation from peyote in 1897 [14]. Heffter was finally able to show that mescaline, with a half-life of 6 h, was exclusively responsible for the intoxication symptoms associated with peyote consumption [14]. In the 1990s, the mechanism of action of mescaline finally became known. As with other psychedelic agents, the effect of mescaline is based on the binding and activation of the serotonin 5-HT2A receptor [15,16,17,18].
DID YOU KNOW ?
Peyote (Lophophora williamsii) is a cactus that contains various biologically active alkaloids—such as pellotine, anhalonidine, hordenine and mescaline. Here, mescaline induces the psychoactive effects of peyote through the activation of the serotonin 5-HT2A receptor and the subsequent release of calcium (Ca2+) from the endoplasmic reticulum (ER). Moreover, an evaluation of the therapeutic benefits of mescaline is also currently the subject of research. It is important to consider that the outcome of taking a psychedelic drug strongly depends on the mindset of the recipient and the context (set and setting principle), including ceremonies and culture. This overview serves to summarise the current state of the knowledge of the metabolism, mechanism of action and clinical application studies of peyote and mescaline. Furthermore, the benefits of the potential of peyote and mescaline are presented in a new light, setting an example for combining a form of treatment embedded in nature and ritually enriched with our current highly innovative Western medicine.
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