The DOI matches its Crossref record; 458 of the 462 references it cites were found in a registry or an index.
Recent advances in the neuropsychopharmacology of serotonergic hallucinogens
Open accessAbstract
Serotonergic hallucinogens, such as (+)-lysergic acid diethylamide, psilocybin, and mescaline, are somewhat enigmatic substances. Although these drugs are derived from multiple chemical families, they all produce remarkably similar effects in animals and humans, and they show cross-tolerance. This article reviews the evidence demonstrating the serotonin 5-HT2A receptor is the primary site of hallucinogen action. 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. Many recent clinical trials have yielded important new findings regarding the psychopharmacology of these substances. Furthermore, the use of modern imaging and electrophysiological techniques is beginning to help unravel how hallucinogens work in the brain. Evidence is also emerging that hallucinogens may possess therapeutic efficacy.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
A default mode of brain function
Raichle, M. E., MacLeod, A. M., Snyder, A. Z., Powers, W. J., Gusnard, D. A., & Shulman, G. L. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.98.2.676 · Cited by 12,190 · cited 1×
“…that psilocybin reduces activity and connectivity in core nodes of the default-mode network, brain regions that are active during the resting state and potentially involved in introspective processes (for more information, see: Raichle et al., 2001; Mason et al., 2007; Buckner et al., 2008).”
BackgroundThe Brain's Default Network: Anatomy, Function, and Relevance to Disease
Buckner, R. L., Andrews‐Hanna, J. R., & Schacter, D. L. (2008) · Annals of the New York Academy of Sciences · doi:10.1196/annals.1440.011 · Cited by 9,761 · cited 2×
“…that psilocybin reduces activity and connectivity in core nodes of the default-mode network, brain regions that are active during the resting state and potentially involved in introspective processes (for more information, see: Raichle et al., 2001; Mason et al., 2007; Buckner et al., 2008).”
BackgroundResultParallel organization of functionally segregated circuits linking basal ganglia and cortex
Alexander, G. E., DeLong, M. R., & Strick, P. L. (1986) · Annual Review of Neuroscience · doi:10.1146/annurev.ne.09.030186.002041 · Cited by 8,527 · cited 1×
“CSTC loops are parallel, anatomically segregated circuits relaying information between the basal ganglia, thalamus, and cortex (Alexander et al., 1986, 1990).”
BackgroundLeDoux, J. E. (2000) · Annual Review of Neuroscience · doi:10.1146/annurev.neuro.23.1.155 · Cited by 8,444
Neuronal Oscillations in Cortical Networks
Buzsáki, G., & Draguhn, A. (2004) · Science · doi:10.1126/science.1099745 · Cited by 6,576 · cited 2×
“Since cortical oscillations play a fundamental role in a diverse set of mental processes and are required for the coordination of neural processing (Gray et al., 1989; Singer, 1999; Buzsaki and Draguhn, 2004; Sejnowski and Paulsen, 2006; Fries, 2009; Klimesch, 2012), it is tempting to speculate that the reduction of n…”
BackgroundNeurophysiological investigation of the basis of the fMRI signal
Logothetis, N. K., Pauls, J., Augath, M., Trinath, T., & Oeltermann, A. (2001) · Nature · doi:10.1038/35084005 · Cited by 6,551 · cited 1×
“One potential explanation is that the hemodynamic responses measured by fMRI are actually better correlated with cortical oscillatory activity than with neuronal firing (Mathiesen et al., 1998; Logothetis et al., 2001; Behav Brain Res.”
BackgroundGray, C. M., König, P., Engel, A. K., & Singer, W. (1989) · Nature · doi:10.1038/338334a0 · Cited by 4,183 · cited 2×
“Since cortical oscillations play a fundamental role in a diverse set of mental processes and are required for the coordination of neural processing (Gray et al., 1989; Singer, 1999; Buzsaki and Draguhn, 2004; Sejnowski and Paulsen, 2006; Fries, 2009; Klimesch, 2012), it is tempting to speculate that the reduction of n…”
BackgroundThalamocortical oscillations in the sleeping and aroused brain
Steriade, M., McCormick, D. A., & Sejnowski, T. J. (1993) · Science · doi:10.1126/science.8235588 · Cited by 3,564 · cited 1×
“Under anesthesia or during slow-wave sleep, cortical networks display slow (0.5–1 Hz) and delta (1–4 Hz) oscillations (Steriade et al., 1993a,b; Steriade, 1997) that reflect alternations between periods of silence (DOWN states) and periods of depolarization with repetitive spiking (UP states).”
BackgroundInfluentialAlpha-band oscillations, attention, and controlled access to stored information
Klimesch, W. (2012) · Trends in Cognitive Sciences · doi:10.1016/j.tics.2012.10.007 · Cited by 3,310 · cited 2×
“Since cortical oscillations play a fundamental role in a diverse set of mental processes and are required for the coordination of neural processing (Gray et al., 1989; Singer, 1999; Buzsaki and Draguhn, 2004; Sejnowski and Paulsen, 2006; Fries, 2009; Klimesch, 2012), it is tempting to speculate that the reduction of n…”
BackgroundInternational Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).
Hoyer, D., Clarke, D. E., Fozard, J. R., Hartig, P. R., Martin, G. R., Mylecharane, E. J., Saxena, P. R., & Humphrey, P. P. A. (1994) · Pharmacological Reviews · doi:10.1016/s0031-6997(25)06783-3 · Cited by 3,025 · cited 2×
“The 5-HT2 receptor class was later reorganized to include three subtypes: 5-HT2A (equivalent to the site known historically as the 5-HT2 receptor or the D receptor), 5-HT2B (formerly known as the 5HT2F receptor), and 5-HT2C (formerly known as the 5-HT1C receptor) (Hoyer et al., 1994).”
Background
Flagged first, then by citations
4 of the 462 references couldn’t be matched to a known paper.
Research works printed but not linked: 7
- Glennon, 1982, The use of the drug discrimination paradigm for studying hallucinogenic agents. A review, 69
- Dittrich, 1975, Zusammenstellung eines Fragebogens (APZ) zur Erfassung abnormer psychischer Zustände, Z Klin Psychol Psychother, 23, 12
- Young, 1981, The hallucinogen DOM as a discriminative stimulus, Commun Psychopharmacol, 4, 501
- Glennon, 1985, Site-selective 5-HT agonists as discriminative stimuli, Pharmacologist, 27, 194
- Serko, 1913, Im Mescalinrausch, Jahrb Psychiatr Neurol, 31, 355
- Prentiss, 1895, Anhalonium lewinii (mescal buttons): a study of the drug, with especial reference to its physiological action upon man, with report of experiments, Ther Gaz, 19, 577
- Ellis, 1898, Mescal: a new artificial paradise, Annu Rep Smithsonian Inst, 537
Cited by
Sorted by citations
Griffiths, R. R., Johnson, M. W., Carducci, M. A., Umbricht, A., Richards, W. A., Richards, B. D., Cosimano, M. P., & Klinedinst, M. A. (2016) · Journal of Psychopharmacology · doi:10.1177/0269881116675513 · Cited by 2,201
“The classic hallucinogens, which include psilocybin (psilocin) and (+)-lysergic acid diethylamide (LSD), are a structurally diverse group of compounds that are 5-HT2A receptor agonists and produce a unique profile of changes in thoughts, perceptions, and emotions (Halberstadt, 2015; Nichols, 2016).”
BackgroundNichols, D. E. (2016) · Pharmacological Reviews · doi:10.1124/pr.115.011478 · Cited by 1,762
“In the study byHalberstadt et al. (2011a), the response to psilocin was not affected by deletion of the 5-HT2A receptor gene.”
BackgroundMethodInfluentialNeural correlates of the LSD experience revealed by multimodal neuroimaging
Carhart-Harris, R. L., Muthukumaraswamy, S., Roseman, L., Kaelen, M., Droog, W., Murphy, K., Tagliazucchi, E., Schenberg, E. E., Nest, T., Orban, C., et al. (2016) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1518377113 · Cited by 859
“LSD has a high affinity for a range of different neurotransmitter receptors, but its characteristic psychological effects are thought to be mediated by serotonin 2A receptor (5-HT2AR) agonism (7).”
BackgroundSerotonin and brain function: a tale of two receptors
Carhart-Harris, R., & Nutt, D. (2017) · Journal of Psychopharmacology · doi:10.1177/0269881117725915 · Cited by 739
“…this limitation, we also wish to emphasise that the evidence is compelling that 5-HT2AR agonism is key to psychedelics’ most characteristic effects (Halberstadt, 2015), 5-HT1AR agonism attenuates rather than augments these effects (Pokorny et al., 2016; Strassman, 1996) and more selective 5-HT2AR…”
BackgroundBogenschutz, M. P., Ross, S., Bhatt, S., Baron, T., Forcehimes, A. A., Laska, E., Mennenga, S. E., O’Donnell, K., Owens, L. T., Podrebarac, S., et al. (2022) · JAMA Psychiatry · doi:10.1001/jamapsychiatry.2022.2096 · Cited by 711
Metadata
- Authors
- Halberstadt, A. L.
- Affiliations
- University of California San Diego (US)
- Corresponding author
- Halberstadt, Adam L.
- ORCID
- Halberstadt, Adam L.
- Venue
- Behavioural Brain Research
- Publisher
- Elsevier BV
- Published
- 2015-01
- Volume
- 277
- Pages
- 99-120
- ISSN
- 0166-4328 (ISSN-L)
- PMC
- PMC4642895
- OpenAlex
- W2052466574
- Semantic Scholar
- 09d1ad0158732c17a145c95ba0ac4f6ed7bdf021
- Cited by
- 312
- References
- 462
- Citations by year
- 2026: 21 · 2025: 33 · 2024: 30 · 2023: 21 · 2022: 33 · 2021: 35 · 2020: 27 · 2019: 17 · 2018: 28 · 2017: 26 · 2016: 27 · 2015: 12
- FWCI
- 3.39
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Behavioural Brain Research (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- NIMH (K01 MH100644)
- NIDA (R01 DA002925)
- Brain and Behavior Research Foundation
- Topics
- Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Life Sciences › Neuroscience › Cognitive Neuroscience › Hallucinations in medical conditions
- Keywords
- serotonergic hallucinogens, 5-HT2A receptor, lysergic acid diethylamide, psilocybin, mescaline, cross-tolerance, drug discrimination, head-twitch response, exploratory behavior, interval timing, electrophysiology
- MeSH terms
- Animals, Behavior, Animal, Brain, Exploratory Behavior, Hallucinogens, Humans, Lysergic Acid Diethylamide, Receptor, Serotonin, 5-HT2A
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review