Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens

@article{Halberstadt2011MultipleRC,
  title={Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens},
  author={Adam L Halberstadt and Mark A Geyer},
  journal={Neuropharmacology},
  year={2011},
  volume={61},
  pages={364-381}
}
Serotonergic hallucinogens produce profound changes in perception, mood, and cognition. These drugs include phenylalkylamines such as mescaline and 2,5-dimethoxy-4-methylamphetamine (DOM), and indoleamines such as (+)-lysergic acid diethylamide (LSD) and psilocybin. Despite their differences in chemical structure, the two classes of hallucinogens produce remarkably similar subjective effects in humans, and induce cross-tolerance. The phenylalkylamine hallucinogens are selective 5-HT(2) receptor… Expand
Role of the 5-HT2A receptor in the locomotor hyperactivity produced by phenylalkylamine hallucinogens in mice
TLDR
It is confirmed that phenylalkylamine hallucinogens increase locomotor activity in mice and demonstrated that this effect is mediated by 5-HT₂A receptor activation, and provided additional support for the link between 5- HT₁A activation and hallucinogenesis. Expand
Recent advances in the neuropsychopharmacology of serotonergic hallucinogens
TLDR
The 5-HT2A receptor is responsible for mediating the effects of hallucinogens in human subjects, as well as in animal behavioral paradigms such as drug discrimination, head twitch response, prepulse inhibition of startle, exploratory behavior, and interval timing. Expand
ecent advances in the neuropsychopharmacology of serotonergic allucinogens
Serotonergic hallucinogens, such as (+)-lysergic acid diethylamide, psilocybin, and mescaline, are somewhat enigmatic substances. Although these drugs are derived from multiple chemical families,Expand
Serotonergic hallucinogens as translational models relevant to schizophrenia.
TLDR
Despite the difficulty of modelling hallucinogen effects in nonverbal species, animal models of schizophrenia based on hallucinogens have yielded important insights into the linkage between 5-HT and schizophrenia and have helped to identify receptor targets and interactions that could be exploited in the development of new therapeutic agents. Expand
Pharmacology and Toxicology of N-Benzylphenethylamine ("NBOMe") Hallucinogens.
TLDR
Based on a review of 51 cases of NBOMe toxicity reported in the literature, it appears that rhabdomyolysis is a relatively common complication of severe NBOME toxicity, an effect that may be linked toNBOMe-induced seizures, hyperthermia, and vasoconstriction. Expand
Hallucinogen-Like Action of the Novel Designer Drug 25I-NBOMe and Its Effect on Cortical Neurotransmitters in Rats
TLDR
The data from this study suggest that hallucinogenic activity of 25I-NBOMe seems to be related with the increase in extracellular GLU level-mediated via cortical 5-HT2A receptors, and may modulate its effect on neurotransmitters and HTR. Expand
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. Expand
Pharmacologic Similarities and Differences Among Hallucinogens
  • K. Waters
  • Medicine
  • Journal of clinical pharmacology
  • 2021
TLDR
The aim of this article is to compare the pharmacologic similarities and differences among substances within the hallucinogen class and their impact on physical and psychiatric effects. Expand
Effect of Hallucinogens on Unconditioned Behavior.
TLDR
This chapter focuses on three animal models that are frequently used to test the effects of hallucinogens on unconditioned behavior: head twitch response (HTR), prepulse inhibition of startle (PPI), and exploratory behavior. Expand
Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other species
TLDR
Evidence is presented that hallucinogens induce these three effects with remarkably consistent potencies and the use of the HTR paradigm as a preclinical model of hallucinogen psychopharmacology and in structure-activity relationship studies of hallucinationsinogens is supported. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 341 REFERENCES
Serotonin and serotonin receptors in hallucinogen action
Abstract Hallucinogens (psychedelics) are substances that induce profound changes in perception and cognition. The closely related 3,4-methylenedioxymethamphetamine (MDMA) produces euphoria and aExpand
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. Expand
Cross-tolerance studies of serotonin receptors involved in behavioral effects of LSD in rats
TLDR
The hypothesis that the effects of LSD in this model reflect a combination of 5-HT1A and5-HT2 effects is supported and support the view that there is an interaction between 5- HT 1A and 5-ht2 receptors. Expand
Hallucinogens and serotonergic mechanisms.
TLDR
Using [3H]DOB as radioligand to minimize differences observed between agonists and antagonists, 5-HT2 affinity is related both to the lipophilicity and electron withdrawing nature of the 4-position substituents. Expand
Hallucinogens Recruit Specific Cortical 5-HT2A Receptor-Mediated Signaling Pathways to Affect Behavior
TLDR
By genetically expressing 2AR only in cortex, it is shown that 2AR-regulated pathways on cortical neurons are sufficient to mediate the signaling pattern and behavioral response to hallucinogens. Expand
Do classical hallucinogens act as 5-HT2 agonists or antagonists?
  • R. Glennon
  • Chemistry, Medicine
  • Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
  • 1990
TLDR
A review of the existing literature suggests that where a 5-HT2 mechanism has been implicated (such as in phosphoinositide turnover, contraction of certain smooth muscle, rat-paw edema, head-twitch behavior, discriminative stimulus effects, hyperthermia, platelet aggregation, and in various other effects), the classical hallucinogens are most likely acting via an agonist, or at least via a partial agonists mechanism. Expand
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. Expand
Dissociations between the effects of hallucinogens on behavior and raphe unit activity in behaving cats
  • M. Trulson
  • Medicine, Psychology
  • Pharmacology Biochemistry and Behavior
  • 1986
The hypothesis that hallucinogenic drugs exert their behavioral effects by an action at pre- or postsynaptic serotonin receptors was evaluated by co-administering various drugs that possess eitherExpand
Some behavioral effects of hallucinogens are mediated by a postsynaptic serotonergic action: evidence from single unit studies in freely moving cats.
TLDR
It is demonstrated that at least some of the behavioral effects of LSD can be blocked by pharmacological antagonism of postsynaptic serotonin receptors which leaves LSD's presynaptic effect unaffected. Expand
Agonist Properties of N,N-Dimethyltryptamine at Serotonin 5-HT2A and 5-HT2C Receptors
TLDR
DMT behaves as an agonist at both 5- HT2A and 5-HT2A receptors, which suggests the 5-ht2C receptor plays a less prominent role in the action of DMT. Expand
...
1
2
3
4
5
...