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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.
Salamanders and caecilians, neglected from the chemical point of view
Published in Toxin Reviews, 2022
Isadora Alves de Vasconcelos, Jéssica Oliveira de Souza, Jessica Schneider de Castro, Carlos José Correia de Santana, Ana Carolina Martins Magalhães, Mariana de Souza Castro, Osmindo Rodrigues Pires Júnior
The first register of indolalkylamines in caecilian was described in the family Siphonopidae, more specifically in the skin secretion of S. annulatus, where serotonin and bufotenin were found (Schwartz et al.2007).
Neural Plasticity in the Ventral Tegmental Area, Aversive Motivation during Drug Withdrawal and Hallucinogenic Therapy
Published in Journal of Psychoactive Drugs, 2023
Hector Vargas-Perez, Taryn Elizabeth Grieder, Derek van der Kooy
The so-called classical hallucinogens (5-HT2a agonists) such as Psilocybin, Dimethyltryptamine (DMT), Bufotenin, LSD-25 and Mescaline have an ancient history of medical use (Carhart-Harris and Goodwin 2017; Johnson et al. 2019). In recent years, there has been increasing interest of people seeking to use these substances to treat mood-related disorders (dos Santos et al., 2016; Johnson & Griffiths, 2017; Johnson et al. 2019, 2019; Mithoefer, Grob, and Brewerton 2016; Muttoni, 2019; Nichols, Johnson, and Nichols 2017; dos Santos et al., 2019; Vargas-Perez and Doblin 2013). Experimental studies and preclinical evidence suggest that classical hallucinogens, administered in a supportive environment with preparatory and integrative mental care, can be used safely to treat a range of psychiatric conditions related to aversive motivation, such as end-of-life anxiety, drug addiction, obsessive-compulsive disorder and depression (DiVito and Leger 2020; Dos Santos Rg et al. 2016; Johnson, Garcia-Romeu, and Griffiths 2017; Johnson et al. 2019; Mithoefer, Grob, and Brewerton 2016; Muttoni, Ardissino, and John 2019; Nichols, Johnson, and Nichols 2017; RG et al. 2019; Vargas-Perez and Doblin 2013). Moreover, recent experimental evidence suggest that classical hallucinogens could be acting as a pharmacological agent with high specificity to effectively treat aversive motivation, promoting neural plasticity in the frontal cortex and hippocampus, and reducing BDNF-related increased plasticity in the mesolimbic system. For example, intraperitoneal administration of psilocybin increase neural plasticity in the hippocampus (Catlow et al. 2013) and frontal cortical pyramidal neurons (Raval et al. 2021; Shao et al. 2021), and enhances the extinction of aversive motivation related to fear conditioning in rodents. These results are aligned with the finding that psychedelic compounds such as LSD and DMT, among other, are able to increase dendritic arbor complexity, promote dendritic spine growth, and stimulate synapse formation on pyramidal neurons, both in vitro and in vivo. In the ventral tegmental area, the administration of psilacetin, a pro-drug of psilocin (Nichols et al., 1999) reverses the plastic changes in the mesolimbic system induced by BDNF-related aversive drug withdrawal symptoms (Vargas-Perez et al. 2017). It also has been observed that repeated self administrations of LSD attenuates the depressant effects of the kappa opioid receptor agonist U69,593 on intra cranial self-stimulation in the medial forebrain bundle in rodents (Sakloth, 2019).