Nichols DE. Psychedelics. Pharm Rev. 2016;68:264–355. https://doi.org/10.1124/pr.115.011478.
Article CAS PubMed PubMed Central Google Scholar
McClure-Begley TD, Roth BL. The promises and perils of psychedelic pharmacology for psychiatry. Nat Rev Drug Discov. 2022;21:463–73. https://doi.org/10.1038/s41573-022-00421-7.
Article CAS PubMed Google Scholar
Griffiths RR, Johnson MW, Carducci MA, Umbricht A, Richards WA, Richards BD, et al. Psilocybin produces substantial and sustained decreases in depression and anxiety in patients with life-threatening cancer: a randomized double-blind trial. J Psychopharmacol. 2016;30:1181–97. https://doi.org/10.1177/0269881116675513.
Article CAS PubMed PubMed Central Google Scholar
Ross S, Bossis A, Guss J, Agin-Liebes G, Malone T, Cohen B, et al. Rapid and sustained symptom reduction following psilocybin treatment for anxiety and depression in patients with life-threatening cancer: a randomized controlled trial. J Psychopharmacol. 2016;30:1165–80. https://doi.org/10.1177/0269881116675512.
Article CAS PubMed PubMed Central Google Scholar
Davis AK, Barrett FS, May DG, Cosimano MP, Sepeda ND, Johnson MW, et al. Effects of psilocybin-assisted therapy on major depressive disorder: a randomized clinical trial. JAMA Psychiatry. 2021;78:481–9. https://doi.org/10.1001/jamapsychiatry.2020.3285.
Carhart-Harris R, Giribaldi B, Watts R, Baker-Jones M, Murphy-Beiner A, Murphy R, et al. Trial of psilocybin versus escitalopram for depression. N Engl J Med. 2021;384:1402–11. https://doi.org/10.1056/NEJMoa2032994.
Article CAS PubMed Google Scholar
Holze F, Gasser P, Muller F, Dolder PC, Liechti ME. Lysergic acid diethylamide-assisted therapy in patients with anxiety with and without a life-threatening illness: a randomized, double-blind, placebo-controlled Phase II study. Biol Psychiatry. 2023;93:215–23. https://doi.org/10.1016/j.biopsych.2022.08.025.
Goodwin GM, Aaronson ST, Alvarez O, Arden PC, Baker A, Bennett JC, et al. Single-dose psilocybin for a treatment-resistant episode of major depression. N Engl J Med. 2022;387:1637–48. https://doi.org/10.1056/NEJMoa2206443.
Article CAS PubMed Google Scholar
Wooley DW, Shaw E. A biochemical and pharmacological suggestion about certain mental disorders. Proc Natl Acad Sci USA. 1954;40:228–31.
Gaddum JH, Hameed KA. Drugs which antagonize 5-hydroxytryptamine. Br J Pharm. 1954;9:240–8.
Gaddum JH, Khan A, Hathway DE, Stephens FF. Quantitative studies of antagonists for 5-hydroxytryptamine. Q J Exp Physiol. 1955;40:49–74.
Article CAS PubMed Google Scholar
Aghjanian GK, Foote WE, Sheard MH. Lysergic acid diethylamide: sensitive neuronal units in the midbrain raphe. Science. 1968;161:706–8.
Kelly PH, Iversen LL. LSD as an agonist at mesolimbic dopamine receptors. Psychopharmacologia. 1975;45:221–4.
Article CAS PubMed Google Scholar
Geyer MA, Gordon J, Adams LM. Behavioral effects of xylamine-induced depletions of brain norepinephrine: interaction with LSD. Pharm Biochem Behav. 1985;23:619–25.
Peroutka SJ, Snyder SH. Multiple serotonin receptors: differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol. Mol Pharm. 1979;16:687–99.
Glennon RA, Seggel MR, Soine WH, Herrick-Davis K, Lyon RA, Titeler M. 125I-2,5-dimethoxy-4-iodophenyl-2-aminopropane (DOI): an iodinated radioligand that specifically labels the agonist high affinity state of the 5HT2 serotonin receptor. J Med Chem. 1988;31:5–7.
Article CAS PubMed Google Scholar
Johnson MP, Hoffman AJ, Nichols DE, Mathis CA. Binding to the serotonin 5-HT2 receptor by the enantiomers of 125I-DOI. Neuropharmacology. 1987;26:1803–6. https://doi.org/10.1016/0028-3908(87)90138-9.
Article CAS PubMed Google Scholar
Kroeze WK, Sassano MF, Huang XP, Lansu K, McCorvy JD, Giguère PM, et al. PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nat Struct Mol Biol. 2015;22:362–9. https://doi.org/10.1038/nsmb.3014.
Article CAS PubMed PubMed Central Google Scholar
Corne SJ, Pickering RW, Warner BT. A method for assessing the effects of drugs on the central actions of 5-hydroxytryptamine. Br J Pharm Chemother. 1963;20:106–20. https://doi.org/10.1111/j.1476-5381.1963.tb01302.x.
Malick JB, Doren E, Barnett A. Quipazine-induced head-twitch in mice. Pharm Biochem Behav. 1977;6:325–9.
Rodriguez R, Pardo EG. Quipazine, a new type of antidepressant agent. Psychopharmacologia. 1971;21:89–100. https://doi.org/10.1007/bf00404000.
Article CAS PubMed Google Scholar
Glennon RA, Titler M, McKenney JD. Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sci. 1984;35:2505–11.
Article CAS PubMed Google Scholar
Halberstadt AL, Chatha M, Klein AK, Wallach J, Brandt SD. Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other species. Neuropharmacology. 2020;167:107933. https://doi.org/10.1016/j.neuropharm.2019.107933.
Article CAS PubMed PubMed Central Google Scholar
Sanders-Bush E, Burris KD, Knoth K. Lysergic acid diethylamide and 2,5-dimethoxy-4-methylamphetamine are partial agonists at serotonin receptors linked to phosphoinositide hydrolysis. J Pharmacol Exp Ther. 1988;246:924–8.
Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, et al. SAR of psilocybin analogs: discovery of a selective 5-HT(2C) agonist. Bioorg Med Chem Lett. 2005;15:4555–9.
Leysen JE, Niemegeers CJE, Van Nueten JM, Laduron PM. [3H]-ketanserin (R 41 468) a selective 3H-ligand for serotonin2 receptor binding sites. Mol Pharmacol. 1982;21:301–14.
Vollenweider FX, Vollenweider-Scherpenhuyzen MF, Babler A, Vogel H, Hell D. Psilocybin induces schizophrenia-like psychosis in humans via a serotonin-2 agonist action. Neuroreport. 1998;9:3897–902.
Article CAS PubMed Google Scholar
Quednow BB, Kometer M, Geyer MA, Vollenweider FX. Psilocybin-induced deficits in automatic and controlled inhibition are attenuated by ketanserin in healthy human volunteers. Neuropsychopharmacology. 2012;37:630–40. https://doi.org/10.1038/npp.2011.228.
Kometer M, Schmidt A, Bachmann R, Studerus E, Seifritz E, Vollenweider FX. Psilocybin biases facial recognition, goal-directed behavior, and mood state toward positive relative to negative emotions through different serotonergic subreceptors. Biol Psychiatry. 2012;72:898–906. https://doi.org/10.1016/j.biopsych.2012.04.005.
Article CAS PubMed Google Scholar
Kometer M, Schmidt A, Jancke L, Vollenweider FX. Activation of serotonin 2A receptors underlies the psilocybin-induced effects on alpha oscillations, N170 visual-evoked potentials, and visual hallucinations. J Neurosci. 2013;33:10544–51. https://doi.org/10.1523/JNEUROSCI.3007-12.2013.
Article CAS PubMed PubMed Central Google Scholar
Bernasconi F, Schmidt A, Pokorny T, Kometer M, Seifritz E, Vollenweider FX. Spatiotemporal brain dynamics of emotional face processing modulations induced by the serotonin 1A/2A receptor agonist psilocybin. Cereb Cortex. 2014;24:3221–31. https://doi.org/10.1093/cercor/bht178.
Pokorny T, Preller KH, Kraehenmann R, Vollenweider FX. Modulatory effect of the 5-HT1A agonist buspirone and the mixed non-hallucinogenic 5-HT1A/2A agonist ergotamine on psilocybin-induced psychedelic experience. Eur Neuropsychopharmacol. 2016;26:756–66. https://doi.org/10.1016/j.euroneuro.2016.01.005.
Article CAS PubMed Google Scholar
Barrett FS, Preller KH, Herdener M, Janata P, Vollenweider FX. Serotonin 2A receptor signaling underlies LSD-induced alteration of the neural response to dynamic changes in music. Cereb Cortex. 2018;28:3939–50. https://doi.org/10.1093/cercor/bhx257.
Preller KH, Burt JB, Ji JL, Schleifer CH, Adkinson BD, Stämpfli P, et al. Changes in global and thalamic brain connectivity in LSD-induced altered states of consciousness are attributable to the 5-HT2A receptor. Elife. 2018;7e35082. https://doi.org/10.7554/eLife.35082.
Abbas A, Roth B. Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders. Expert Opin Pharmacother. 2008;9:3251–9. https://doi.org/10.1517/14656560802532707.
Article CAS PubMed Google Scholar
Sorensen SM, Kehne JH, Fadayel GM, Humphreys TM, Ketteler HJ, Sullivan CK, et al. Characterization of the 5-HT2 antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. J Pharmacol Exp Ther. 1993;266:684–91.
Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan AJ, Levit A, et al. Crystal structure of an LSD-bound human serotonin receptor. Cell. 2017;168:377–89.e312. https://doi.org/10.1016/j.cell.2016.12.033.
Article CAS PubMed PubMed Central Google Scholar
Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE. et al. Structure of a hallucinogen activated gq-coupled 5-HT2A serotonin receptor. Cell. 2020;182:1574–88.e1519. https://doi.org/10.1016/j.cell.2020.08.024.
Article CAS PubMed PubMed Central Google Scholar
Kaplan AL, Confair DN, Kim K, Barros-Álvarez X, Rodriguiz RM, Yang Y, et al. Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity. Nature. 2022;610:582–91. https://doi.org/10.1038/s41586-022-05258-z.
Article CAS PubMed Google Scholar
Cao D, Yu J, Wang H, Luo Z, Liu X, He L, et al. Structure-based discovery of nonhallucinogenic psychedelic analogs. Science. 2022;375:403–11. https://doi.org/10.1126/science.abl8615.
留言 (0)