The roles of 5-HT1A and 5-HT2 receptors in the effects of 5-MeO-DMT on locomotor activity and prepulse inhibition in rats

@article{KrebsThomson2006TheRO,
  title={The roles of 5-HT1A and 5-HT2 receptors in the effects of 5-MeO-DMT on locomotor activity and prepulse inhibition in rats},
  author={Kirsten Krebs-Thomson and Erbert M. Ruiz and Virginia L. Masten and Mah{\'a}lah R. Buell and Mark A Geyer},
  journal={Psychopharmacology},
  year={2006},
  volume={189},
  pages={319-329}
}
RationaleThe hallucinogen 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) is structurally similar to other indoleamine hallucinogens such as LSD. The present study examined the effects of 5-MeO-DMT in rats using the Behavioral Pattern Monitor (BPM), which enables analyses of patterns of locomotor activity and exploration, and the prepulse inhibition of startle (PPI) paradigm.ObjectivesA series of interaction studies using the serotonin (5-HT)1A antagonist WAY-100635 (1.0 mg/kg), the 5-HT2A… Expand
Modification of the effects of 5-methoxy-N,N-dimethyltryptamine on exploratory behavior in rats by monoamine oxidase inhibitors
TLDR
The ability of harmaline to modify the behavioral effects of 5-MeO-DMT is mediated by the inhibition of MAOA, and 5-HT2A receptors are responsible for the late hyperactivity induced by 5- MeO- DMT in the presence ofMAOA inhibitors. Expand
Modification of 5-methoxy-N,N-dimethyltryptamine-induced hyperactivity by monoamine oxidase A inhibitor harmaline in mice and the underlying serotonergic mechanisms.
TLDR
Co-administration of MAOI with 5-MeO-DMT provokes excessive late-phase hyperactivity, which involves the activation of both 5-HT1A and5-HT2A receptors, which could be abolished by either WAY-100635 or MDL-100907. Expand
Behavioral effects of α,α,β,β-tetradeutero-5-MeO-DMT in rats: comparison with 5-MeO-DMT administered in combination with a monoamine oxidase inhibitor
TLDR
Deuterated tryptamines may be useful in behavioral and pharmacological studies to mimic the effects of tryptamine/MAOI combinations to indicate that the hyperactivity induced by 5- MeO-DMT after MAO inhibition is a consequence of reduced metabolism of 5-MeO- DMT, leading to prolonged occupation of central serotonin receptors. Expand
Potentiation of 5-methoxy-N,N-dimethyltryptamine-induced hyperthermia by harmaline and the involvement of activation of 5-HT1A and 5-HT2A receptors
TLDR
The results indicate that co-administration of monoamine oxidase inhibitor largely potentiates 5-MeO-DMT-induced hyperthermia that involves the activation of both 5-HT1A and5-HT2A receptors and shall provide insights into development of anxiolytic drugs and new strategies to relieve the lethalhyperthermia in serotonin toxicity. Expand
Behavioral and pharmacokinetic interactions between monoamine oxidase inhibitors and the hallucinogen 5-methoxy-N,N-dimethyltryptamine
  • A. Halberstadt
  • Medicine, Chemistry
  • Pharmacology Biochemistry and Behavior
  • 2016
TLDR
It is confirmed that 5-MeO-DMT can disrupt PPI by activating 5-HT2A, and indicate that MAOIs alter 5- MeO- DMT pharmacodynamics by increasing its accumulation in the central nervous system. Expand
The serotonergic hallucinogen 5-methoxy-N,N-dimethyltryptamine disrupts cortical activity in a regionally-selective manner via 5-HT1A and 5-HT2A receptors
TLDR
The present results suggest that the hallucinogen action of 5-MeO-DMT is mediated by simultaneous alterations of the activity of sensory (S1, Au1, V1) and associative (PFC) cortical areas, also supporting a role of 5.HT(1A)-R stimulation in V1 and PFC, in addition to the well-known action on 5-HT(2A-R. Expand
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
The 5-hydroxytryptamine 2A receptor agonists DOI and 25CN-NBOH decrease marble burying and reverse 8-OH-DPAT-induced deficit in spontaneous alternation
TLDR
It is shown that agonism of 5-HT2AR reduces repetitive behavioral patterns, supporting the theory that this is a potential new treatment approach to disorders of cognitive or behavioral inflexibility. Expand
Involvement of serotoninergic 5-HT1A/2A, alpha-adrenergic and dopaminergic D1 receptors in St. John's wort-induced prepulse inhibition deficit: A possible role of hyperforin
TLDR
It is concluded that serotoninergic 5-HT1A and 5- HT2A, alpha-adrenergic and dopaminergic D1 receptors are involved in the disruptive effect of St. John's wort extract on PPI response in rats, and hyperforin, and not hypericin, is one of the active ingredients responsible for St.John's worts wort-induced PPI disruption with no relation to apoptotic processes. Expand
Pharmacokinetic Interactions between Monoamine Oxidase A Inhibitor Harmaline and 5-Methoxy-N,N-Dimethyltryptamine, and the Impact of CYP2D6 Status
TLDR
A unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed and may be further employed to predict harmaline and 5-Methoxy-N,N-dimethyltryptamine PK interactions at various doses, define the impact of CYP 2D6 status, and drive harmaline–5-Me O-D MT pharmacodynamics. Expand
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