Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens

@article{Rickli2016ReceptorIP,
  title={Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens},
  author={Anna Rickli and Olivier D. Moning and Marius C. Hoener and Matthias E. Liechti},
  journal={European Neuropsychopharmacology},
  year={2016},
  volume={26},
  pages={1327-1337}
}

Figures and Tables from this paper

Effects of the new psychoactive substances diclofensine, diphenidine, and methoxphenidine on monoaminergic systems

5-HT2 receptor binding, functional activity and selectivity in N-benzyltryptamines

TLDR
Although some N-benzyltryptamines might be abuse-liable, others might represent new leads for the development of therapeutics for weight loss, erectile dysfunction, drug abuse, or schizophrenia.

Investigation of the Structure-Activity Relationships of Psilocybin Analogues.

TLDR
The tryptamine derivatives have psilocybin-like pharmacological properties, supporting their classification as psychedelic drugs.

Pharmacological profiling of novel psychoactive substances

Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines

TLDR
3,4,5-Trimethoxyphenethylamine (mescaline) is a psychedelic alkaloid found in peyote cactus and scalines and 3C-scalines interacted with the 5-HT2A and 5- HT2C receptors and bound with higher affinities when compared to mescaline, with no potent affinity observed at non-serotonergic targets.

Monoamine Transporter and Receptor Interaction Profiles in Vitro Predict Reported Human Doses of Novel Psychoactive Stimulants and Psychedelics

  • D. LuethiM. Liechti
  • Biology, Psychology
    The international journal of neuropsychopharmacology
  • 2018
TLDR
Investigating whether specific in vitro monoamine transporter and receptor interactions can predict effective psychoactive doses in humans found that dopamine and norepinephrine transporter inhibition potency was positively correlated with human doses, whereas serotonin transporter inhibited potency was inversely correlated withhuman doses.
...

References

SHOWING 1-10 OF 93 REFERENCES

Interaction of psychoactive tryptamines with biogenic amine transporters and serotonin receptor subtypes

TLDR
All psychoactive tryptamines are 5-HT2A agonists, but5-HT transporter (SERT) activity may contribute significantly to the pharmacology of certain compounds, and in vitro transporter data confirm structure-activity trends for releasers and uptake inhibitors whereby releasers tend to be structurally smaller compounds.

Differential contributions of serotonin receptors to the behavioral effects of indoleamine hallucinogens in mice

TLDR
It is confirmed that psilocin acts as an agonist at 5-HT1A, 4-hydroxy-N,N-dimethyltryptamine, and 5- HT2C receptors in mice, whereas the behavioral effects of 1-methylpsilocin indicate that this compound is acting at5-HT2A sites but is inactive at the 5-ht1A receptor.

Dimethyltryptamine and other hallucinogenic tryptamines exhibit substrate behavior at the serotonin uptake transporter and the vesicle monoamine transporter

TLDR
High binding-to-uptake ratios support the hypothesis that the tryptamines are transporter substrates, not uptake blockers, at both SERT and VMAT2, and indicate that there are separate substrate and inhibitor binding sites within these transporters.

Hallucinogenic drug interactions at human brain 5-HT2 receptors: implications for treating LSD-induced hallucinogenesis

TLDR
The hypothesis that the hallucinogenic effects of these drugs in humans are mediated in whole or in part via 5-HT2 receptors is supported and treatment with 5- HT2 receptor antagonists may be effective in reversing the halluc inogenic effects caused by the ingestion, of LSD and LSD-like drugs.

Abuse Liability Profile of Three Substituted Tryptamines

TLDR
DIPT and 5-MeO-DET may have abuse liability similar to known hallucinogens and may be hazardous because high doses produced activity and lethality, but were not similar to those of psychostimulants.

The hallucinogenic world of tryptamines: an updated review

TLDR
A comprehensive update on tryptamine hallucinogens, concerning their historical background, prevalence, patterns of use and legal status, chemistry, toxicokinetics, toxicodynamics and their physiological and toxicological effects on animals and humans is provided.

5-Methoxy-N,N-diisopropyltryptamine (Foxy), a selective and high affinity inhibitor of serotonin transporter.

Benzofuran bioisosteres of hallucinogenic tryptamines.

TLDR
It is suggested that benzofurans may be useful in the design of serotonin receptor ligands in rat brain homogenate.

Functional Selectivity of Hallucinogenic Phenethylamine and Phenylisopropylamine Derivatives at Human 5-Hydroxytryptamine (5-HT)2A and 5-HT2C Receptors

TLDR
The results support the concept of functional selectivity and indicate that subtle changes in ligand structure can result in significant differences in the cellular signaling profile.
...