Hallucinogens Recruit Specific Cortical 5-HT2A Receptor-Mediated Signaling Pathways to Affect Behavior

@article{GonzlezMaeso2007HallucinogensRS,
  title={Hallucinogens Recruit Specific Cortical 5-HT2A Receptor-Mediated Signaling Pathways to Affect Behavior},
  author={Javier Gonz{\'a}lez-Maeso and Noelia V. Weisstaub and Mingming Zhou and Pokman Chan and Lidija Ivi{\'c} and Rosalind L. Ang and Alena Lira and Maria Bradley-Moore and Yongchao Ge and Qiang Zhou and Stuart C. Sealfon and Jay A Gingrich},
  journal={Neuron},
  year={2007},
  volume={53},
  pages={439-452}
}

Figures from this paper

Hallucinogens induce a specific barcode of phosphorylation on the serotonin2A receptor that underlies a weaker receptor desensitization and internalization

TLDR
A biased phosphorylation of the 5-HT 2A receptor is demonstrated in response to hallucinogenic versus non-hallucinogenic agonists that leads to a weaker receptor desensitization and internalization by hallucinogens.

Hallucinogenic 5-hydroxytryptamine 2A receptor agonist effects in senescence-accelerated mice.

TLDR
Results indicate that SAMP6 increases DOI-dependent ERK1/2-CREB signaling leading to more head-twitch responses than SAMR1, and that Samp6 could provide a useful model for examining the relationship between 5-HT2AR regulatory signaling and behavioral phenotypes.

Mechanism of the 5-hydroxytryptamine 2A receptor-mediated facilitation of synaptic activity in prefrontal cortex

TLDR
The results from these experiments do not support the idea that 5-HT2ARs elicit the release of an excitatory retrograde messenger nor that they activate thalamocortical afferents, the two dominant hypotheses, and suggest that5-HT 2ARs facilitate intrinsic networks within the PFC.

Hallucinogens and Serotonin 5-HT2A Receptor-Mediated Signaling Pathways.

TLDR
Recent advances in understanding hallucinogen drug action are reviewed through characterization of structure, neuroanatomical location, and function of the 5-HT2A receptor.

Chronic Phenethylamine Hallucinogen Treatment Alters Behavioral Sensitivity to a Metabotropic Glutamate 2/3 Receptor Agonist

TLDR
It was discovered that the repeated dosing regimen required for discrimination training attenuated the behavioral effects of the mGlu2/3 receptor agonist LY379268, and chronic studies confirmed that repeated hallucinogen treatment causes a loss of behavioral activity of mGglutamatergic receptors.

Serotonin and serotonin receptors in hallucinogen action

The serotonin 5-HT2C receptor and the non-addictive nature of classic hallucinogens

TLDR
It is argued that activation of 5-HT2C receptors on NAc shell, GABAergic, medium spiny neurons inhibits potassium Kv1.x channels, thereby enhancing inhibitory activity via intrinsic mechanisms and providing a potential reason for the non-addictive nature of classic hallucinogens.
...

References

SHOWING 1-10 OF 69 REFERENCES

Transcriptome Fingerprints Distinguish Hallucinogenic and Nonhallucinogenic 5-Hydroxytryptamine 2A Receptor Agonist Effects in Mouse Somatosensory Cortex

TLDR
The results demonstrate that chemicals acting at the 5-HT2AR induce specific cellular response patterns in vivo that are reflected in unique changes in the somatosensory cortex transcriptome.

Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats

TLDR
It is demonstrated that the behavioral effects of low doses of lisuride are clearly mediated by stimulation of 5-HT1A receptors.

Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: evidence for agonist-directed trafficking of receptor stimulus.

TLDR
Concentration-response curves to 5-HT2C agonists were fit well by a three-state model of receptor activation, suggesting that two active receptor states may be sufficient to explain pathway-dependent agonist efficacy.

The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs I: Antagonist correlation analysis

TLDR
The data indicate that the stimulus effects of LSD, and the substitution of (−)DOM for the LSD stimulus are mediated by agonist activity at 5-HT2A receptors.

Localization of 5-HT2A receptors on dopamine cells in subnuclei of the midbrain A10 cell group

Effects of lisuride and LSD on cerebral monoamine systems and hallucinosis

TLDR
The present findings do not support the hypothesis that the hallucinogenic effect of LSD is reflected by variations in the level and turnover of the brain amines, and a stimulation of 5-HT autoreceptors is also evident after the non-hallucinogenic lisuride.

DOI-Induced Activation of the Cortex: Dependence on 5-HT2A Heteroceptors on Thalamocortical Glutamatergic Neurons

TLDR
It is found that DOI did not induce Fos in cortical 5-HT2A immunoreactive neurons but did increase expression in a band of neurons spanning superficial layer V to deep III, within the apical dendritic fields of layer V 5- HT2A-immunoreactive cells.
...