Agonist Properties of N,N-Dimethyltryptamine at Serotonin 5-HT2A and 5-HT2C Receptors

  title={Agonist Properties of N,N-Dimethyltryptamine at Serotonin 5-HT2A and 5-HT2C Receptors},
  author={Randy L. Smith and Herv{\'e} Canton and Robert John Barrett and Elaine sanders-Bush},
  journal={Pharmacology Biochemistry and Behavior},

Figures and Tables from this paper

The role of 5-HT2A, 5-HT2C and mGlu2 receptors in the behavioral effects of tryptamine hallucinogens N,N-dimethyltryptamine and N,N-diisopropyltryptamine in rats and mice
The 5-HT2AR likely plays a major role in mediating the effects of two tryptamine hallucinogenic drugs and likely modulate the discriminative stimulus effects of both compounds.
5-HT2A and 5-HT2C receptors exert opposing effects on locomotor activity in mice
Data indicate that the decrease in locomotor activity induced by 10 mg/kg DOI is mediated by 5-HT2C receptors, an interpretation that is supported by the finding that the selective 5- HT2C agonist WAY 161,503 produces reductions in the locomotory activity that are potentiated in 5HT2A KO mice.
Neurotoxic Effects of 5-MeO-DIPT: A Psychoactive Tryptamine Derivative in Rats
The induction of head-twitch response and potentiation of forepaw treading induced by 8-OH-DPAT indicate that hallucinogenic activity seems to be mediated through the stimulation of 5-HT2A and5-HT1A receptors by 5-MeO-DIPT.
Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens
A possibly sigma-1 receptor mediated role of dimethyltryptamine in tissue protection, regeneration, and immunity
N,N-dimethyltryptamine (DMT) is classified as a naturally occurring serotonergic hallucinogen of plant origin. It has also been found in animal tissues and regarded as an endogenous trace amine
The hallucinogenic world of tryptamines: an updated review
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.
Chapter 15 – Tryptamines
Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats
The present results suggest that antagonists of the 5-HT5A receptor may inhibit subjective effects of LSD in rats.
In vitro assays for the functional characterization of (psychedelic) substances at the serotonin receptor 5‐HT2AR
This review elaborates on the in vitro molecular techniques that have been used the most abundantly for the characterization of (psychedelic) 5‐HT2AR agonists and focuses on the mechanism behind the techniques, and the specific advantages and challenges that are associated with these.
Mapping the binding site of the 5-HT2A receptor using mutagenesis and ligand libraries: Insights into the molecular actions of psychedelics
To map how each structural class of psychedelics binds and activates the serotonin 5-HT2A, receptor using a combination of mutagenesis and a library of ligands, results indicate that serine 5.43 (S239) and asparagine 6.55 (N343) form a hydrogen bond with the 5-position of tryptamines and phenylalkylamines, whereas the affinity of LSD is more mediated by S242.


Lysergic acid diethylamide and 2,5-dimethoxy-4-methylamphetamine are partial agonists at serotonin receptors linked to phosphoinositide hydrolysis.
LSD partially antagonized the effect of 5-HT in the choroid plexus, consistent with a partial agonist effect at the 5- HT-1c receptor in this tissue.
Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists.
5-HT2C receptor neutral antagonists exhibited functional and receptor binding properties consistent with those of classical receptor antagonists, however, 5-HT 2C receptor inverse agonists displayed functional and receptors binding properties that were opposite those of agonists.
Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies.
The data indicate that MDL 100,907 has a clozapine-like profile of potential antipsychotic activity with low extrapyramidal sid-effect liability.
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
It would appear that the DOM stimulus is primarily a 5-HT2-mediated, and not 5- HT1C- mediated, phenomenon, and compound 26 may find application in other pharmacologic investigations where spiperone may not be a suitable antagonist.
Pharmacological activity of the isomers of LY53857, potent and selective 5-HT2 receptor antagonists.
The present study investigated the activities of the diastereomers of LY53857 and found that a similar profile of selectivity was demonstrated for each of the isomers studied, with the meso mixture of isomers being slightly less potent than the SS- and RR-isomers after p.o.v. administration of serotonin.
Human psychopharmacology of N,N-dimethyltryptamine
  • R. Strassman
  • Psychology, Biology
    Behavioural Brain Research
  • 1995
Neurochemical and behavioral evidence that quipazine-ketanserin discrimination is mediated by serotonin2A receptor.
The combined results from the substitution, antagonism and ex vivo receptor autoradiographic studies suggest that the discriminative stimuli of quipazine and ketanserin are mediated at least in part by the 5-HT2A receptor.
Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects.
Dimethyltryptamine can be administered safely to experienced hallucinogen users and dose-response data generated for several measures hypothesized under serotonergic modulatory control may prove useful in psychopharmacological investigations of drug-induced and endogenous alterations in brain function.