5-HT Modulation of Dopamine Release in Basal Ganglia in Psilocybin-Induced Psychosis in Man—A PET Study with [11C]raclopride
Abstract
The modulating effects of serotonin on dopamine neurotransmission are not well understood, particularly in acute psychotic states. Positron emission tomography was used to examine the effect of psilocybin on the in vivo binding of [11C]raclopride to D2-dopamine receptors in the striatum in healthy volunteers after placebo and a psychotomimetic dose of psilocybin (n = 7). Psilocybin is a potent indoleamine hallucinogen and a mixed 5-HT2A and 5-HT1A receptor agonist. Psilocybin administration (0.25 mg/kg p.o.) produced changes in mood, disturbances in thinking, illusions, elementary and complex visual hallucinations and impaired ego-functioning. Psilocybin significantly decreased [11C]raclopride receptor binding potential (BP) bilaterally in the caudate nucleus (19%) and putamen (20%) consistent with an increase in endogenous dopamine. Changes in [11C]raclopride BP in the ventral striatum correlated with depersonalization associated with euphoria. Together with previous reports of 5-HT receptor involvement in striatal dopamine release, it is concluded that stimulation of both 5-HT2A and 5-HT1A receptors may be important for the modulation of striatal dopamine release in acute psychoses. The present results indirectly support the hypothesis of a serotonin-dopamine dysbalance in schizophrenia and suggest that psilocybin is a valuable tool in the analysis of serotonin-dopamine interactions in acute psychotic states.
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In a PET study, healthy volunteers scanned with [11C]-raclopride first in a placebo baseline and again after psilocybin (0.25 mg/kg p.o.) showed a global 20% decline in [11C]-raclopride binding in the striatum, similar to displacements evoked by amphetamine or other strong releasers of dopamine.
“Comparison of the two scans revealed a global 20% decline in [11C]-raclopride (41) binding in the striatum, which is similar to the displacements evoked by amphetamine or other strong releasers of dopamine.”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [96]
The decline in ventral striatum correlated with individual ratings for euphoria and depersonalization.
“Furthermore, the decline in the ventral striatum correlated with individual ratings for euphoria and depersonalization.”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [96]
Psychedelics facilitate altered states of consciousness characterized by heightened introspection and diminished ego boundaries through influence on 5-HT1A, 5-HT2B, dopaminergic, and glutamatergic systems.
“The other explanation of psychedelics' ability to facilitate altered states of consciousness characterized by heightened introspection and diminished ego boundaries is their influence on 5-HT1A [64] and 5-HT2B [65], and interacting with the dopaminergic [66] and glutamatergic systems [67].”
From Mindfulness meditation and psychedelics: potential synergies and commonalities (2023) · cites this paper as [66]
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dos Santos, R. G., Osório, F. L., Crippa, J. A. S., Riba, J., Zuardi, A. W., & Hallak, J. E. C. (2016) · Therapeutic Advances in Psychopharmacology · doi:10.1177/2045125316638008 · Cited by 306 · see citing works
Psilocybin – Summary of knowledge and new perspectives
Tylš, F., Páleníček, T., & Horáček, J. (2014) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2013.12.006 · Cited by 276 · see citing works
“Psilocybin also indirectly increased (via 5HT receptors) the release of dopamine in the ventral striatum in humans, an effect that correlated with symptoms of depersonalization and euphoria (Vollenweider et al., 1999).”
BackgroundLiu, W.-H., Chuang, H.-L., Huang, Y.-T., Wu, C.-C., Chou, G.-T., Wang, S., & Tsai, Y.-C. (2016) · Behavioural Brain Research · doi:10.1016/j.bbr.2015.10.046 · Cited by 269 · see citing works
Effects of psilocybin on hippocampal neurogenesis and extinction of trace fear conditioning
Catlow, B. J., Song, S., Paredes, D. A., Kirstein, C. L., & Sanchez-Ramos, J. (2013) · Experimental Brain Research · doi:10.1007/s00221-013-3579-0 · Cited by 266 · see citing works
“However, PSOP administration decreases [ 11 C]raclopride receptor binding potential in the basal ganglia, which is indicative of increased DA levels (Vollenweider et al. 1999).”
BackgroundInfluentialUmbricht, D., Koller, R., Vollenweider, F. X., & Schmid, L. (2002) · Biological Psychiatry · doi:10.1016/s0006-3223(01)01242-2 · Cited by 258 · see citing works
“In addition, both NMDAR antagonists and 5-HT2A agonists lead to excessive dopamine release in humans (Kegeles et al 2000; Breier et al 1998; Vollenweider et al 2000; Vollenweider et al 1999).”
BackgroundSelf-citationThe Therapeutic Potential of Psilocybin
Lowe, H. I. C., Toyang, N., Steele, B., Valentine, H., Grant, J. F., Ali, A., Ngwa, W., & Gordon, L. (2021) · Molecules · doi:10.3390/molecules26102948 · Cited by 206 · see citing works
“This suggests that psilocybin may have significant potential in the treatment of schizophrenia and possibly other psychiatric disorders [168].”
BackgroundEffects of psilocybin on time perception and temporal control of behaviour in humans
Wittmann, M., Carter, O. L., Hasler, F., Cahn, B. R., Grimberg, U., Spring, P., Hell, D., Flohr, H., & Vollenweider, F. X. (2006) · Journal of Psychopharmacology · doi:10.1177/0269881106065859 · Cited by 240 · see citing works
Self-citationPsychedelics in Psychiatry: Neuroplastic, Immunomodulatory, and Neurotransmitter Mechanisms
Inserra, A., De Gregorio, D., & Gobbi, G. (2021) · Pharmacological Reviews · doi:10.1124/pharmrev.120.000056 · Cited by 232 · see citing works
Assessment of addiction severity among ritual users of ayahuasca.
Fábregas, J. M., González, D., Fondevila, S., Cutchet, M., Fernández, X., Barbosa, P. C. R., Alcázar-Córcoles, M. Á., Barbanoj, M. J., Riba, J., & Bouso, J. C. (2010) · Drug and Alcohol Dependence · doi:10.1016/j.drugalcdep.2010.03.024 · Cited by 227 · see citing works
Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance
Dinis-Oliveira, R. J. (2017) · Drug Metabolism Reviews · doi:10.1080/03602532.2016.1278228 · Cited by 224 · see citing works
“Indeed, the administration of psilocybin to healthy human volunteers, decreased the binding of the dopamine D2 antagonist [ (11)C] raclopride in both caudate nucleus and putamen (Vollenweider et al., 1999).”
BackgroundVollenweider, F. X., Vontobel, P., Øye, I., Hell, D., & Leenders, K. L. (2000) · Journal of Psychiatric Research · doi:10.1016/s0022-3956(99)00031-x · Cited by 223 · see citing works
Self-citationEffect of Psilocybin on Empathy and Moral Decision-Making
Pokorny, T., Preller, K. H., Kometer, M., Dziobek, I., & Vollenweider, F. X. (2017) · International Journal of Neuropsychopharmacology · doi:10.1093/ijnp/pyx047 · Cited by 197 · see citing works
“Although psilocybin also has downstream effects on the dopamine system (Vollenweider et al., 1998; Vollenweider et al., 1999; Halberstadt and Geyer, 2011), an involvement of the dopamine system in the current results is unlikely since administration of the dopamine reuptake inhibitor methylphenidate did not lead to in…”
ResultSelf-citationClinical applications of hallucinogens: a review
Garcia-Romeu, A., Kersgaard, B., & Addy, P. H. (2016) · Experimental and Clinical Psychopharmacology · doi:10.1037/pha0000084 · Cited by 201 · see citing works
“However, differential actions at other serotonergic, dopaminergic, and downstream glutamatergic targets are known to modulate the effects of distinct psychedelics (Moreno et al., 2011; Nichols, 2016; Pieri et al., 1974; Ray, 2010; Vollenweider et al., 1999; Vollenweider & Kometer, 2010).”
BackgroundDepersonalisation Disorder: A Contemporary Overview
Simeon, D. (2004) · CNS Drugs · doi:10.2165/00023210-200418060-00002 · Cited by 198 · see citing works
Vollenweider, F., Csomor, P., Knappe, B., Geyer, M., & Quednow, B. (2007) · Neuropsychopharmacology · doi:10.1038/sj.npp.1301324 · Cited by 159 · see citing works
“Moreover, we previously reported that the 5-HT releasing agent MDMAF which indirectly stimulates both 5-HT 2A and 5-HT 1A receptorsFalso increases PPI at long (120 ms) but not short ISI (30 ms) in healthy human volunteers and disrupts PPI in rats (Vollenweider et al, 1999a).”
Self-citationUmbricht, D., Vollenweider, F. X., Schmid, L., Grübel, C., Skrabo, A., Huber, T., & Koller, R. (2003) · Neuropsychopharmacology · doi:10.1038/sj.npp.1300005 · Cited by 187 · see citing works
“Similarly, administration of psilocybin in healthy volunteers is associated with increased dopamine release (Vollenweider et al, 1999).”
BackgroundSelf-citationMadsen, M. K., Fisher, P. M., Stenbæk, D. S., Kristiansen, S., Burmester, D., Lehel, S., Páleníček, T., Kuchař, M., Svarer, C., Ozenne, B., et al. (2020) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2020.02.001 · Cited by 183 · see citing works
Exaggerated 5-HT1A but Normal 5-HT2A Receptor Activity in Individuals Ill with Anorexia Nervosa
Bailer, U. F., Frank, G. K., Henry, S. E., Price, J. C., Meltzer, C. C., Mathis, C. A., Wagner, A., Thornton, L., Hoge, J., Ziolko, S. K., et al. (2007) · Biological Psychiatry · doi:10.1016/j.biopsych.2006.07.018 · Cited by 161 · see citing works
The dopaminergic basis of human behaviors: a review of molecular imaging studies
Egerton, A., Mehta, M., Montgomery, A., Lappin, J., Howes, O., Reeves, S., Cunningham, V., & Grasby, P. (2009) · Neuroscience and Biobehavioral Reviews · doi:10.1016/j.neubiorev.2009.05.005 · Cited by 180 · see citing works
“These techniques, used in combination with administration of pharmacological compounds that target non-dopaminergic neurotransmitter systems, have allowed examination of the neuropharmacology of DA release in the human brain (Breier et al., 1998; Brody et al., 2004; Dewey et al., 1993; Vollenweider et al., 1999), and…”
BackgroundExploring the effect of microdosing psychedelics on creativity in an open-label natural setting
Prochazkova, L., Lippelt, D. P., Colzato, L. S., Kuchar, M., Sjoerds, Z., & Hommel, B. (2018) · Psychopharmacology · doi:10.1007/s00213-018-5049-7 · Cited by 177 · see citing works
“Previous research has shown a relationship between 5-HT2A receptor activity and goal directed behavior likely due to indirect modulation of DA release (Vollenweider et al. 1999; Sakashita,et al. 2015; Dalley et al. 2002; Boureau and Dayan 2011).”
BackgroundLiechti, M. E., & Vollenweider, F. X. (2000) · European Neuropsychopharmacology · doi:10.1016/s0924-977x(00)00086-9 · Cited by 145 · see citing works
Self-citationBrain mechanisms of hallucinogens and entactogens
Vollenweider, F. X. (2001) · Dialogues in Clinical Neuroscience · doi:10.31887/dcns.2001.3.4/fxvollenweider · Cited by 129 · see citing works
“Indeed, both Sketamine and psilocybin significantly reduced [(11)C]raclopride BP in ventral striatum consistent with an increase in striatal DA concentration.(73,74) Moreover, these changes in [(11)C]raclopride BP significantly correlated with depersonalization, supporting the view that excessive DA transmission at D2…”
BackgroundSelf-citationMolecular Mechanisms of Psilocybin and Implications for the Treatment of Depression
Ling, S., Ceban, F., Lui, L. M. W., Lee, Y., Teopiz, K. M., Rodrigues, N. B., Lipsitz, O., Gill, H., Subramaniapillai, M., Mansur, R. B., et al. (2022) · CNS Drugs · doi:10.1007/s40263-021-00877-y · Cited by 127 · see citing works
Miller, D. D., Andreasen, N. C., OʼLeary, D. S., Watkins, G. L., Ponto, L. L. B., & Hichwa, R. D. (2001) · Biological Psychiatry · doi:10.1016/s0006-3223(00)01001-5 · Cited by 127 · see citing works
Riba, J., Anderer, P., Morte, A., Urbano, G., Jané, F., Saletu, B., & Barbanoj, M. J. (2002) · British Journal of Clinical Pharmacology · doi:10.1046/j.1365-2125.2002.01609.x · Cited by 125 · see citing works
Bogenschutz, M. P., & Pommy, J. M. (2012) · Drug Testing and Analysis · doi:10.1002/dta.1376 · Cited by 125 · see citing works
“Psilocybin also increases striatal dopamine concentrations, but haloperidol (an antagonist of D2, D3, and D4 receptors) decreases the euphoria and depersonalization effects of psilocybin by only 30%,([41]) and actually increases its psychotomimetic effects,([35])”
BackgroundA Review of Neurotransmitters Sensing Methods for Neuro-Engineering Research
Niyonambaza, S. D., Kumar, P., Xing, P., Mathault, J., Koninck, P. D., Boisselier, É., Boukadoum, M., & Miled, A. (2019) · Applied Sciences · doi:10.3390/app9214719 · Cited by 121 · see citing works
Delusional parasitosis and the dopamine transporter. A new insight of etiology?
Huber, M. K., Kirchler, E., Kärner, M., & Pycha, R. (2006) · Medical Hypotheses · doi:10.1016/j.mehy.2006.07.061 · Cited by 114 · see citing works
“psilocybin) results in increased striatal dopamine release [68].”
BackgroundClassic Psychedelic Drugs: Update on Biological Mechanisms
Vollenweider, F. X., & Smallridge, J. W. (2022) · Pharmacopsychiatry · doi:10.1055/a-1721-2914 · Cited by 112 · see citing works
“Recent behavioral and neuroimaging studies demonstrated that psychedelics produce their psychological effects primarily via agonist action at 5-HT2A receptors in the brain [15, 16], although modulatory downstream effects upon the gamma-aminobutyric acid (GABA)ergic [17], dopaminergic [18] and glutamatergic [17] system…”
Self-citationThe role of the extrapersonal brain systems in religious activity
Previc, F. H. (2006) · Consciousness and Cognition · doi:10.1016/j.concog.2005.09.009 · Cited by 105 · see citing works
“Further complicating the effects of 5-HT on hallucinatory experiences is the fact that serotonergic systems are also known to modulate DA transmission, predominantly by inhibiting the latter in the striatum and elsewhere (Di Matteo et al., 2002; Ennis et al., 1981; Herve et al., 1979; Joyce, 1993; Kapur & Remington, 1…”
BackgroundInfluentialHasler, F., Bourquin, D., Brenneisen, R., & Vollenweider, F. X. (2002) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/s0731-7085(02)00278-9 · Cited by 100 · see citing works
Self-citationKometer, M., Cahn, B. R., Andel, D., Carter, O. L., & Vollenweider, F. X. (2010) · Biological Psychiatry · doi:10.1016/j.biopsych.2010.10.002 · Cited by 99 · see citing works
Self-citationAlterations of Serotonin Transmission in Schizophrenia
Abi‐Dargham, A. (2007) · International review of neurobiology · doi:10.1016/s0074-7742(06)78005-9 · Cited by 98 · see citing works
Classical hallucinogens and neuroimaging: A systematic review of human studies
dos Santos, R. G., Osório, F. L., Crippa, J. A. S., & Hallak, J. E. C. (2016) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2016.10.026 · Cited by 107 · see citing works
“…Swiss group used PET to analyze the effects of silocybin [0.25 mg/kg, oral] on the binding of [11C]raclopride o D2-dopamine receptors in the striatum of seven healthy ale volunteers [age: 27 ± 2.3 years] (Vollenweider et al., 1999). silocybin was administered 80 min before [11C]raclopride injecion.”
InfluentialKalkman, H. O. (2001) · Neuropsychopharmacology · doi:10.1016/s0893-133x(01)00285-8 · Cited by 94 · see citing works
“Effective doses of psilocybin significantly decreased [11C]raclopride binding in the striatum, which is indicative for an increase in endogenous dopamine levels in this brain structure (Vollenweider et al. 1999).”
BackgroundNunes, A. A., SANTOS, R. G. D., Osório, F. D. L., Sanches, R. F., Crippa, J. A. S., & Hallak, J. E. C. (2016) · Journal of Psychoactive Drugs · doi:10.1080/02791072.2016.1188225 · Cited by 91 · see citing works
Inserra, A. (2018) · Frontiers in Pharmacology · doi:10.3389/fphar.2018.00330 · Cited by 91 · see citing works
“The authors suggested that, since psilocybin increases dopaminergic neurotransmission, and since drugs that increase dopamine availability are beneficial to fear extinction, psilocybin might be beneficial to fear extinction via enhancing dopaminergic neurotransmission (Aghajanian and Marek, 1999; Vollenweider et al.,…”
BackgroundPsilocybin modulates functional connectivity of the amygdala during emotional face discrimination
Grimm, O., Krähenmann, R., Preller, K. H., Seifritz, E., & Vollenweider, F. X. (2018) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2018.03.016 · Cited by 91 · see citing works
Self-citationPsychedelics, Sociality, and Human Evolution
Rodríguez Arce, J. M., & Winkelman, M. J. (2021) · Frontiers in Psychology · doi:10.3389/fpsyg.2021.729425 · Cited by 86 · see citing works
“Moreover, psilocybin has been found to increase striatal dopamine concentrations Frontiers in Psychology | www.frontiersin.org 10 September 2021 | Volume 12 | Article 729425 in humans, a mechanism partly underlying euphoria and depersonalization phenomena (Vollenweider et al., 1999).”
BackgroundUdina, M., Navinés, R., Egmond, E., Oriolo, G., Langohr, K., Giménez, D., Valdés, M., Gómez‐Gil, E., Grande, I., Gratacòs, M., et al. (2015) · The International Journal of Neuropsychopharmacology · doi:10.1093/ijnp/pyv135 · Cited by 88 · see citing works
Serotonin: Imaging Findings in Eating Disorders
Bailer, U. F., & Kaye, W. H. (2010) · Current topics in behavioral neurosciences · doi:10.1007/7854_2010_78 · Cited by 89 · see citing works
“, psilocybin, seem to disrupt the 5-HT1A/2A balance (Vollenweider et al. 1999) by driving 5-HT2A activity, resulting in excessive neuronal output contributing to extremes of disinhibition, disorganization, and loss of self-control.”
BackgroundSex differences and serotonergic mechanisms in the behavioural effects of psilocin
Tylš, F., Páleníček, T., Kadeřábek, L., Fujáková-Lipski, M., Kubešová, A., & Horáček, J. (2015) · Behavioural Pharmacology · doi:10.1097/fbp.0000000000000198 · Cited by 86 · see citing works
“In line with this, psilocin has been shown to induce dopamine release in the striatum in humans (Vollenweider et al., 1999) and, more recently, also in the nucleus accumbens of male Wistar rats, although only with a very high dose of 10 mg/kg of psilocin (Sakashita et al., 2015).”
BackgroundGuss, J. R., Krause, R., & Sloshower, J. (2020) · doi:10.31234/osf.io/u6v9y · Cited by 86 · see citing works
Neural Mechanisms and Psychology of Psychedelic Ego Dissolution
Stoliker, D., Egan, G. F., Friston, K. J., & Razi, A. (2022) · Pharmacological Reviews · doi:10.1124/pharmrev.121.000508 · Cited by 89 · see citing works
Therapeutic Applications of Classic Hallucinogens
Bogenschutz, M. P., & Ross, S. (2016) · Current topics in behavioral neurosciences · doi:10.1007/7854_2016_464 · Cited by 85 · see citing works
Heterogeneous effects of alcohol on dopamine release in the striatum: a PET study.
Yoder, K., Constantinescu, C., Kareken, D., Normandin, M., Cheng, T., O'Connor, S., & Morris, E. (2007) · Alcoholism: Clinical and Experimental Research · doi:10.1111/j.1530-0277.2007.00390.x · Cited by 89 · see citing works
“…increases in DA levels and the subjective effects of the drugs, including methylphenidate (Volkow et al., 1999), amphetamine (Abi-Dargham et al., 2003; Drevets et al., 2001; Martinez et al., 2003; Oswald et al., 2005), nicotine (Barrett et al., 2004), and psilocybin (Vollenweider et al., 1999).”
BackgroundBailer, U. F., Frank, G., Price, J. C., MELTZER, C. C., Becker, C. R., Mathis, C. A., Wagner, A., Barbarich-Marsteller, N. C., Bloss, C. S., Putnam, K. T., et al. (2012) · Psychiatry Research Neuroimaging · doi:10.1016/j.pscychresns.2012.06.010 · Cited by 82 · see citing works
“In support of this idea, agents that are relatively 5-HT specific, such as psilocybin (Vollenweider et al., 1999), fenfluramine (Smith et al., 1997), and citalopram (Tiihonen et al., 1996) alter [ 11 C]raclopride binding.”
A triple-network organization for the mouse brain
Mandino, F., Vrooman, R. M., Foo, H. E., Yeow, L. Y., Bolton, T. A. W., Salvan, P., Teoh, C. L., Lee, C. Y., Beauchamp, A., Luo, S. X., et al. (2021) · Molecular Psychiatry · doi:10.1038/s41380-021-01298-5 · Cited by 83 · see citing works
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Sekssaoui, M., Bockaert, J., Marin, P., & Bécamel, C. (2024) · Neuropsychopharmacology · doi:10.1038/s41386-024-01794-6 · Cited by 82 · see citing works
“S5D, E and Table 1).”
Alterations of dopamine and serotonin transmission in schizophrenia
Remington, G. (2008) · Progress in brain research · doi:10.1016/s0079-6123(08)00906-0 · Cited by 81 · see citing works
“A second PET study involving psilocybin reported decreased [11C]raclopride binding in both the caudate and the putamen (19 and 20%, respectively), but this compound has mixed 5-HT1A and 5-HT2A agonist properties (Vollenweider et al., 1999).”
BackgroundThe neuroscientific study of spiritual practices
Newberg, A. B. (2014) · Frontiers in Psychology · doi:10.3389/fpsyg.2014.00215 · Cited by 83 · see citing works
“Some neuroimaging studies exploring hallucinogenic agents have already been performed (Vollenweider et al., 1997, 1999, 2000), but a more extensive study of such agents, particularly in relation to religious and spiritual experiences is required.”
BackgroundAbnormal Striatal Dopamine Transmission in Schizophrenia
Brunelin, J., Fecteau, S., & Suaud-Chagny, M. (2013) · Current Medicinal Chemistry · doi:10.2174/0929867311320030011 · Cited by 90 · see citing works
STEEVES, T., & FOX, S. (2008) · Progress in Brain Research · doi:10.1016/s0079-6123(08)00924-2 · Cited by 79 · see citing works
Romeo, B., Hermand, M., Pétillion, A., Karila, L., & Benyamina, A. (2021) · Journal of Psychiatric Research · doi:10.1016/j.jpsychires.2021.03.002 · Cited by 76 · see citing works
“, 2015), but also in the ventral striatum in humans (Vollenweider, 1999).”
BackgroundCerebral 5-HT2A receptor binding is increased in patients with Tourette's syndrome
Haugbøl, S., Pinborg, L. H., Regeur, L., Hansen, E. S., Bolwig, T. G., Nielsen, F. Å., Svarer, C., Skovgaard, L. T., & Knudsen, G. M. (2006) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145706006559 · Cited by 75 · see citing works
Fungal Hallucinogens Psilocin, Ibotenic Acid, and Muscimol
Stebelska, K. (2013) · Therapeutic Drug Monitoring · doi:10.1097/ftd.0b013e31828741a5 · Cited by 75 · see citing works
Psychedelics as an emerging novel intervention in the treatment of substance use disorder: a review
Divito, A. J., & Leger, R. F. (2020) · Molecular Biology Reports · doi:10.1007/s11033-020-06009-x · Cited by 75 · see citing works
Treatment-resistant depression: molecular mechanisms and management
Kajumba, M. M., Kakooza‐Mwesige, A., Nakasujja, N., Attix, D. K., & Canli, T. (2024) · Molecular Biomedicine · doi:10.1186/s43556-024-00205-y · Cited by 86 · see citing works
Hallucinogens as discriminative stimuli in animals: LSD, phenethylamines, and tryptamines
Winter, J. C. (2009) · Psychopharmacology · doi:10.1007/s00213-008-1356-8 · Cited by 65 · see citing works
“Finally, I will attempt no further definition of hallucinogen beyond saying that if a chemical mimics in human subjects the subjective effects of LSD or a tryptamine such as psilocybin or a phenethylamine such as mescaline, then it is a hallucinogen.”
BackgroundPsilocybin in neuropsychiatry: a review of its pharmacology, safety, and efficacy
Dodd, S., Norman, T. R., Eyre, H. A., Stahl, S. M., Phillips, A., Carvalho, A. F., & Berk, M. (2023) · CNS Spectrums · doi:10.1017/s1092852922000888 · Cited by 73 · see citing works
“42 Dopamine increases were correlated with euphoria and depersonalisation.”
Cumming, P. D., Rosa‐Neto, P., Watanabe, H., Smith, D. F., Bender, D., Clarke, P. B. S., & GJEDDE, A. H. (2003) · NeuroImage · doi:10.1016/s1053-8119(03)00079-x · Cited by 68 · see citing works
Psychedelic therapy's transdiagnostic effects: A research domain criteria (RDoC) perspective
Kelly, J. R., Gillan, C. M., Prenderville, J., Kelly, C., Harkin, A., Clarke, G., & O'Keane, V. (2021) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2021.800072 · Cited by 69 · see citing works
“A Positron emission tomography (PET) study in healthy humans showed that psilocybin increased striatal dopamine concentrations, and this increase correlated with euphoria and depersonalization phenomena (211), whereas the mixed 5-HT2/D2 antagonist risperidone attenuated the effects of psilocybin (212).”
BackgroundWienberg, M., Glenthoj, B., Jensen, K., & Oranje, B. (2010) · Journal of Psychopharmacology · doi:10.1177/0269881109102606 · Cited by 68 · see citing works
Winkelman, M. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.619890 · Cited by 72 · see citing works
“Psilocybin increases striatal dopamine concentrations (Vollenweider et al., 1999), an area of the brain mediating rewards from social interactions.”
BackgroundPsilocybin and LSD have no long-lasting effects in an animal model of alcohol relapse
Meinhardt, M. W., Güngör, C., Skorodumov, I., Mertens, L. J., & Spanagel, R. (2020) · Neuropsychopharmacology · doi:10.1038/s41386-020-0694-z · Cited by 65 · see citing works
Mertens, L. J., & Preller, K. H. (2021) · Pharmacopsychiatry · doi:10.1055/a-1341-1907 · Cited by 65 · see citing works
“Evidence is mostly derived from preclinical studies, but one human positron emission tomography (PET) trial also revealed increased striatal dopamine levels following a psilocybin dose [93].”
BackgroundPsilocybin lacks antidepressant-like effect in the Flinders Sensitive Line rat
Jefsen, O. H., Højgaard, K., Christiansen, S. L., Elfving, B., Nutt, D., Wegener, G., & Müller, H. K. (2019) · Acta Neuropsychiatrica · doi:10.1017/neu.2019.15 · Cited by 63 · see citing works
“35 mg/kg) have also been found to increase dopamine levels in ventral striatum (NAc and olfactory tuberculum) in human PET studies (Vollenweider et al., 1999).”
BackgroundInfluential5-HT2A and muscarinic receptors in schizophrenia: a postmortem study
Matsumoto, I., Inoue, Y., Iwazaki, T., Pavey, G., & Dean, B. (2005) · Neuroscience Letters · doi:10.1016/j.neulet.2004.12.059 · Cited by 62 · see citing works
Kuroki, T., Meltzer, H., & Ichikawa, J. (2003) · Brain Research · doi:10.1016/s0006-8993(03)02516-2 · Cited by 55 · see citing works
Leger, R. F., & Unterwald, E. M. (2021) · Journal of Psychopharmacology · doi:10.1177/02698811211044688 · Cited by 55 · see citing works
“They also have direct or indirect interactions with dopamine transmission (Nichols et al., 2017; Vollenweider et al., 1999; Watts et al., 1995).”
BackgroundThe Effect of Psilocin on Memory Acquisition, Retrieval, and Consolidation in the Rat
Rambousek, L., Páleníček, T., Valeš, K., & Stuchlı́k, A. (2014) · Frontiers in Behavioral Neuroscience · doi:10.3389/fnbeh.2014.00180 · Cited by 55 · see citing works
“BEHAVIORAL NEUROSCIENCE ORIGINAL RESEARCH ARTICLE published: 16 May 2014 doi: 10.3389/fnbeh.2014.00180 The effect of psilocin on memory acquisition, retrieval, and consolidation in the rat”
BackgroundInfluentialSerotonergic Hallucinogens and Emerging Targets for Addiction Pharmacotherapies
Ross, S. (2012) · Psychiatric Clinics of North America · doi:10.1016/j.psc.2012.04.002 · Cited by 54 · see citing works
Grandjean, J., Buehlmann, D., Buerge, M., Sigrist, H., Seifritz, E., Vollenweider, F. X., Pryce, C. R., & Rudin, M. (2020) · NeuroImage · doi:10.1016/j.neuroimage.2020.117456 · Cited by 54 · see citing works
Self-citationPáleníček, T., Fujáková, M., Brunovský, M., Horáček, J., Gorman, I., Balı́ková, M., Rambousek, L., Syslová, K., Kačer, P., Zach, P., et al. (2012) · Psychopharmacology · doi:10.1007/s00213-012-2797-7 · Cited by 52 · see citing works
Horsley, R. R., Páleníček, T., Kolin, J., & Valeš, K. (2018) · Behavioural Pharmacology · doi:10.1097/fbp.0000000000000394 · Cited by 52 · see citing works
A neurobiological perspective on social influence: Serotonin and social adaptation
Duerler, P., Vollenweider, F. X., & Preller, K. H. (2022) · Journal of Neurochemistry · doi:10.1111/jnc.15607 · Cited by 50 · see citing works
“In human and rodent studies Psi also showed downstream effects on the DA level in the VS in humans (Puig et al., 2003; Vollenweider, 1999; Vollenweider & Kometer, 2010).”
BackgroundSelf-citation
- Authors
- Vollenweider, F.
- Affiliations
- University Hospital Zurich (CH)
- Corresponding author
- Vollenweider, F
- Venue
- Neuropsychopharmacology
- Published
- 1999-05
- Volume
- 20
- Issue
- 5
- Pages
- 424-433
- ISSN
- 0893-133X (ISSN-L)
- OpenAlex
- W1986425243
- Cited by
- 305
- References
- 73
- Citations by year
- 2026: 15 · 2025: 18 · 2024: 28 · 2023: 28 · 2022: 20 · 2021: 18 · 2020: 19 · 2019: 6 · 2018: 13 · 2017: 7 · 2016: 14 · 2015: 7 · 2014: 6 · 2013: 9 · 2012: 11
- FWCI
- 8.62
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Neuropsychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- DORA PSI (Paul Scherrer Institute) (submittedVersion)
- University of Groningen research database (University of Groningen / Centre for Information Technology) (submittedVersion)
- Topics
- Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Keywords
- psilocybin, psychosis, serotonin, dopamine release, dopamine D2 receptor, [11C]raclopride, striatum, caudate nucleus, putamen, 5-HT2A receptor, 5-HT1A receptor, serotonin-dopamine interaction, hallucinations, depersonalization, schizophrenia
- MeSH terms
- Adult, Basal Ganglia, Dopamine, Hallucinogens, Humans, Male, Psilocybin, Psychometrics, Psychoses, Substance-Induced, Salicylamides, Serotonin, Tomography, Emission-Computed, Antipsychotic Agents, Dopamine Antagonists, Raclopride
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