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Hallucinogens, CNS Stimulants, And Cannabis
Published in S.J. Mulé, Henry Brill, Chemical and Biological Aspects of Drug Dependence, 2019
There are a large number of hallucinogens closely related to dimethyltryptamine chemically. 5-Methoxydimethyltryptamine (Figure 8, R1 = H, R2 = OCH3, R3 = CH3) which accompanies DMT in many of the South American snuffs, is an extremely rapidly acting chemical (effective within seconds), and like DMT, is only active parenterally. The phenolic analog, 5-hydroxy-NAf-dimethyltryptamine is known as bufotenine. Although it is legally classified as an hallucinogenic substance, there is little medical justification for this assignment.24
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
5-MeO-DMT O-demethylation is potentially a bioactivating step because the metabolite bufotenine is a biologically active and toxic agent. Although the psychedelic activity of bufotenine has been documented (McBride 2000; Ott 2001), there are arguments about this because of its poor lipid solubility. Binding studies (McBride 2000; Roth et al. 1997) have shown that bufotenine is a potent ligand for the 5-HT2A receptor with a 10-fold higher affinity compared to 5-MeO-DMT and that bufotenine is approximately three times more potent than 5-MeO-DMT in the brain (Vogel and Evans 1977). It is interesting to note that bufotenine (the metabolite of 5-MeO-DMT) is presently listed as a Schedule I controlled substance in the United States, while 5-MeO-DMT is not.
Catalog of Herbs
Published in James A. Duke, Handbook of Medicinal Herbs, 2018
The active agents are N,N-dimethyltryptamine and related tryptamines.54 Like bufotenine, closely related to serotonin. Active tryptamines apparently reach the brain from the nasal mucosa without a general circulation through the blood stream.
Ayahuasca, a potentially rapid acting antidepressant: focus on safety and tolerability
Published in Expert Opinion on Drug Safety, 2022
Giordano Novak Rossi, Isabella Caroline da Silva Dias, Glen Baker, José Carlos Bouso Saiz, Serdar M. Dursun, Jaime E. C. Hallak, Rafael G. Dos Santos
Regarding the most prevalent AEs and their pharmacological mechanisms, nausea, vomiting, and stomach disturbances are probably related to direct (involving DMT and beta-carbolines binding to receptors) or indirect (involving the inhibition of neurotransmitter metabolism by beta-carbolines) activation of serotoninergic and other monoaminergic receptors located in the gastrointestinal tract. These AEs have been commonly reported with other MAO-inhibiting medications [51] and DMT analogues such as bufotenine (5-OH-DMT) [52] and 5-methoxy-DMT (5-MeO-DMT) [53]. Serotoninergic neurotransmission is also associated with heart rate [54] and blood pressure [55] homeostasis, and alterations in the cardiovascular system by ayahuasca’s alkaloids seems to modulate normal functionality, albeit not in a clinically significant manner for participants with no prior cardiovascular malfunctions. Lastly, it is also known that the serotoninergic system is involved in the etiology of pain and some types of headaches [56], with selective 5-HT1B/D serotonin agonists being approved medications for the treatment of migraines [57]. At the current state of psychedelic substances research, all these AEs are expected and are known to occur with the consumption of ayahuasca and other related substances such as psilocybin and LSD [7,45] (see also our review on the safety of LSD and psilocybin in the context of depression in this Special Issue).
Protein tyrosine phosphatase 1B (PTP1B) inhibitors as potential anti-diabetes agents: patent review (2015-2018)
Published in Expert Opinion on Therapeutic Patents, 2019
Hidayat Hussain, Ivan R Green, Ghulam Abbas, Sergazy M Adekenov, Wahid Hussain, Iftikhar Ali
Heterocycles in general often play a crucial role in medicinal chemistry, photochemistry, agrochemicals, material chemistry, and dyes. Over 24 million organic compounds comprising the heterocyclic scaffold in a 2010 US retail sales report showed that 80% of the drugs comprised of heterocyclic scaffolds [89]. The indole scaffold is present in a wide range of bioactive natural products viz., reserpine, psilocybin, bufotenine, esrine, vinblastine, and vincristine. Moreover, there are a number of marketed drugs comprising the indole scaffold viz., indomethacin (NSAID drug) and pravadoline (analgesic and COX inhibitor) [89]. Additionally, atevirdine (anti-HIV drug) [90], selavirdine (antiretroviral drug), yohimbine (used to treat sexual dysfunction and decrease the risks of type-2 diabetes) [91], pinodolol (antidepressant drug) [92], glufanide (anticancer drug) [93], apaziquone (anticancer) [94], arbidol (antiviral) [95], and panobinostat (anticancer) [96] all contain a heterocyclic scaffold within their structures.