The natural hallucinogen 5-MeO-DMT, component of Ayahuasca, disrupts cortical function in rats: reversal by antipsychotic drugs

Int J Neuropsychopharmacol. 2014 Aug;17(8):1269-82. doi: 10.1017/S1461145714000261. Epub 2014 Mar 20.

Abstract

5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) is a natural hallucinogen component of Ayahuasca, an Amazonian beverage traditionally used for ritual, religious and healing purposes that is being increasingly used for recreational purposes in US and Europe. 5MeO-DMT is of potential interest for schizophrenia research owing to its hallucinogenic properties. Two other psychotomimetic agents, phencyclidine and 2,5-dimethoxy-4-iodo-phenylisopropylamine (DOI), markedly disrupt neuronal activity and reduce the power of low frequency cortical oscillations (<4 Hz, LFCO) in rodent medial prefrontal cortex (mPFC). Here we examined the effect of 5-MeO-DMT on cortical function and its potential reversal by antipsychotic drugs. Moreover, regional brain activity was assessed by blood-oxygen level dependent (BOLD) functional magnetic resonance imaging (fMRI). 5-MeO-DMT disrupted mPFC activity, increasing and decreasing the discharge of 51 and 35% of the recorded pyramidal neurons, and reducing (-31%) the power of LFCO. The latter effect depended on 5-HT1A and 5-HT2A receptor activation and was reversed by haloperidol, clozapine, risperidone, and the mGlu2/3 agonist LY379268. Likewise, 5-MeO-DMT decreased BOLD responses in visual cortex (V1) and mPFC. The disruption of cortical activity induced by 5-MeO-DMT resembles that produced by phencyclidine and DOI. This, together with the reversal by antipsychotic drugs, suggests that the observed cortical alterations are related to the psychotomimetic action of 5-MeO-DMT. Overall, the present model may help to understand the neurobiological basis of hallucinations and to identify new targets in antipsychotic drug development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / pharmacology
  • Animals
  • Antipsychotic Agents / pharmacology*
  • Banisteriopsis / chemistry*
  • Brain Waves / drug effects*
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology
  • Clozapine / pharmacology
  • Excitatory Amino Acid Agonists / pharmacology
  • Functional Neuroimaging
  • Hallucinogens / antagonists & inhibitors
  • Hallucinogens / pharmacology*
  • Haloperidol / pharmacology
  • Magnetic Resonance Imaging
  • Male
  • Methoxydimethyltryptamines / antagonists & inhibitors
  • Methoxydimethyltryptamines / pharmacology*
  • Prefrontal Cortex / blood supply
  • Prefrontal Cortex / drug effects*
  • Prefrontal Cortex / physiology
  • Pyramidal Cells / drug effects
  • Pyramidal Cells / physiology
  • Rats
  • Risperidone / pharmacology
  • Visual Cortex / blood supply
  • Visual Cortex / drug effects*
  • Visual Cortex / physiology

Substances

  • Amino Acids
  • Antipsychotic Agents
  • Bridged Bicyclo Compounds, Heterocyclic
  • Excitatory Amino Acid Agonists
  • Hallucinogens
  • LY 379268
  • Methoxydimethyltryptamines
  • Clozapine
  • Haloperidol
  • Risperidone