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List of miscellaneous 5-HT2A receptor agonists

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This is a list of miscellaneous agonists of the serotonin receptor subtype 5-HT2A (and other 5-HT2 subtypes to a varying extent) that fall outside the common structural classes. Most agonists at this receptor are either substituted phenethylamine derivatives from the 2C, DOx and 25-NB groups, or substituted tryptamines and related compounds along with more complex derivatives of these such as lysergamides and iboga-type alkaloids.[1] There are however numerous 5-HT2A receptor agonists which do not fall within any of these groups, some representative examples of which are listed below. Ki and EC50 values vary depending on the assay conditions used and so may not be directly comparable between sources. Many of these compounds have been designed to be non-psychoactive derivatives for medical applications, and it should not be assumed that a compound which acts as a 5-HT2A agonist will necessarily be psychedelic in nature.[2]

Others

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Analogues of aripiprazole with serotonin 5-HT2A receptor agonism and psychedelic-like effects have been reported.[62]

See also

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References

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  1. ↑ Nichols DE (2018). Chemistry and Structure-Activity Relationships of Psychedelics. Current Topics in Behavioral Neurosciences. Vol. 36. pp. 1–43. doi:10.1007/7854_2017_475. ISBN 978-3-662-55878-2. PMID 28401524.
  2. ↑ Duan W, Cao D, Wang S, Cheng J (January 2024). "Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants". Chemical Reviews. 124 (1): 124–163. doi:10.1021/acs.chemrev.3c00375. PMID 38033123. S2CID 265512698.
  3. 1 2 3 Ennis MD, Hoffman RL, Ghazal NB, Olson RM, Knauer CS, Chio CL, et al. (July 2003). "2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists". Bioorganic & Medicinal Chemistry Letters. 13 (14): 2369–2372. doi:10.1016/s0960-894x(03)00403-7. PMID 12824036.
  4. ↑ Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, et al. (March 2005). "Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity". Bioorganic & Medicinal Chemistry Letters. 15 (5): 1467–1470. doi:10.1016/j.bmcl.2004.12.080. PMID 15713408.
  5. ↑ WO 2009/079765, Slassi A, Isaac M, Xin T, Higgins G, He Z, Sun G, Quach T, "Compounds with activity at the 5-ht2c receptor", published 2 July 2009, assigned to Cascade Therapeutics Inc.
  6. ↑ Sabnis RW. Novel Azepinoindole Compounds as 5‑HT2A Agonists for Treating Neuropsychiatric and Neurodegenerative Disorders. ACS Med Chem Lett. 2025 Oct 20;16(11):2181-2182. doi:10.1021/acsmedchemlett.5c00613 PMID 41256984
  7. ↑ Sabnis RW (August 2025). "Novel Azepinoindoles as 5‑HT2C Agonists for Treating Depression, Drug Addiction, Alcoholism, PTSD, and Neuropathic Pain". ACS Medicinal Chemistry Letters. 16 (8) acsmedchemlett.5c00426: 1507–1508. doi:10.1021/acsmedchemlett.5c00426. PMC 12358981. PMID 40832530.
  8. 1 2 Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, et al. (February 2013). "Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties". Journal of Medicinal Chemistry. 56 (3): 1211–1227. doi:10.1021/jm301656h. PMID 23301527.
  9. ↑ WO 2021076572, David E. Olson; Lee Dunlap & Florence Wagner et al., "Ergoline-like compounds for promoting neural plasticity", published 22 April 2021, assigned to Delix Therapeutics, Inc. and The Regents of the University of California
  10. ↑ Li R, Yan H, Chen Y, Liu Y, Tang L, Yu J, et al. (October 2025). "Structure-Guided Design of Novel 5-HT2A Partial Agonists as Psychedelic Analogues with Antidepressant Effects". Journal of Medicinal Chemistry. 68 (20) acs.jmedchem.5c02045. doi:10.1021/acs.jmedchem.5c02045. PMID 41087124.
  11. 1 2 Orr MJ, Cao AB, Wang CT, Gaisin A, Csakai A, Friswold AP, et al. (April 2022). "Discovery of Highly Potent Serotonin 5-HT2 Receptor Agonists Inspired by Heteroyohimbine Natural Products". ACS Medicinal Chemistry Letters. 13 (4): 648–657. doi:10.1021/acsmedchemlett.1c00694. PMC 9014500. PMID 35450369.
  12. ↑ Sabnis RW. Novel Tricyclic Psychedelic Psychoplastogens as 5‑HT2C Agonists for Treating Neurological Diseases. ACS Med Chem Lett. 2025 Jun 29;16(7):1268-1269. doi:10.1021/acsmedchemlett.5c00381 PMID 40666469
  13. ↑ Yao R, Jensen AA, Bryce-Rogers HP, Schultz-Knudsen K, Zhou L, Hovendal NP, et al. (August 2023). "Identification of 5-HT2 Serotonin Receptor Modulators through the Synthesis of a Diverse, Tropane- and Quinuclidine-alkaloid-Inspired Compound Library". Journal of Medicinal Chemistry. 66 (16): 11536–11554. doi:10.1021/acs.jmedchem.3c01059. PMID 37566000. S2CID 260806387.
  14. 1 2 WO 2004/058722, Teegarden B, Jayakumar H, Strah-Pleynet S, "Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a.", published 15 July 2004, assigned to Arena Pharmaceuticals, Inc.
  15. ↑ US 2021/0137908, Kristensen JL, Jensen AA, Märcher-Rørsted E, "5-HT2A Agonists for Use in Treatment of Depression.", published 13 May 2021, assigned to Lophora ApS.
  16. ↑ Evans-Brown M, Gallegos A, Christie R, Jorge R, De Morais J, Almeida A, et al. (European Monitoring Center for Drugs and Drug Addiction) (December 2020). New Psychoactive Substances: Global Markets, Glocal Threats and the COVID-19 Pandemic. An update from the EU Early Warning System (PDF). Luxembourg: Publications Office of the European Union. doi:10.2810/921262. ISBN 978-92-9497-557-7.
  17. ↑ Glennon RA, Bondarev ML, Khorana N, Young R, May JA, Hellberg MR, et al. (November 2004). "Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane". Journal of Medicinal Chemistry. 47 (24): 6034–41. doi:10.1021/jm040082s. PMID 15537358.
  18. 1 2 Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, et al. (January 2008). "Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity". J Med Chem. 51 (2): 305–313. doi:10.1021/jm0709034. PMID 18095642.
  19. ↑ Arias HR, Rudin D, Hines DJ, Contreras A, Gulsevin A, Manetti D, et al. (March 2024). "The novel non-hallucinogenic compound DM506 (3-methyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole) induces sedative- and anxiolytic-like activity in mice by a mechanism involving 5-HT2A receptor activation". European Journal of Pharmacology. 966 176329. doi:10.1016/j.ejphar.2024.176329. hdl:2158/1354752. PMID 38253116.
  20. ↑ Beckett JOS, et al. Transforming Amino Acids into Serotonin 5-HT2A Receptor Ligands Using Photochemistry. J. Am. Chem. Soc. 2025; 147(52): 48400–48415. doi:10.1021/jacs.5c19817
  21. ↑ Rorsted EM, Jensen AA, Smits G, Frydenvang K, Kristensen JL (May 2024). "Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT2A Receptor Agonists". Journal of Medicinal Chemistry. 67 (9): 7224–7244. doi:10.1021/acs.jmedchem.4c00082. PMC 11089506. PMID 38648420.
  22. ↑ Lyon RA, Titeler M, McKenney JD, Magee PS, Glennon RA (May 1986). "Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents". Journal of Medicinal Chemistry. 29 (5): 630–634. doi:10.1021/jm00155a008. PMID 3701781.
  23. ↑ WO 2023130117, Vadodaria K, Vanover K, Serrats J, Sudarsan V, Garvey D, "Preparation of deuterated pyrrolidin derivatives as modulators of dopamine and serotonin neurotransmission useful in treatment of diseases", assigned to Engrail Therapeutics, Inc.
  24. ↑ Carlsson ML, Carlsson A, Nilsson M (February 2004). "Schizophrenia: from dopamine to glutamate and back". Curr Med Chem. 11 (3): 267–277. doi:10.2174/0929867043456034. PMID 14965231. (+)-UH232 was brought to clinical testing on healthy volunteers as well as schizophrenic patients, though only after single doses. In the former group the drug had some mixed actions with respect to mood and wakefulness. However, a rather striking effect was some abnormalities in perception observed in a number of individuals (illusions with a trend to hallucinations). In some of the schizophrenic patients the psychotic symptoms worsened. These effects may be due to 5-HT2-receptor agonist effects of (+)-UH232 [25]. In spite of this disappointing result it was felt that the pharmacological profile of (+)-UH232 was intriguing and clearly worthy of further exploration.
  25. ↑ Lahti AC, Weiler M, Carlsson A, Tamminga CA (1998). "Effects of the D3 and autoreceptor-preferring dopamine antagonist (+)-UH232 in schizophrenia". Journal of Neural Transmission. 105 (6–7): 719–734. doi:10.1007/s007020050091. PMID 9826114. S2CID 31976950. These behavioral observations are consistent with reports of perceptual disturbances and even visual hallucinations when the drug was administered to normal volunteers (M. Larsson, personal communication). [...] (+)-UH232 has several other lesser affinities for cloned central nervous system system (CNS) receptors: 5HT2 (118nM), 5HT1A (144nM), and D1 (159nM) (R. Lahti, personal communication). [...] Further, (+)-UH232 shows an affinity for the 5HT2 receptor, although with only about 1/10 the potency shown for the D2-family receptors (K. Svensson and R. Lahti, personal communications). [...] In the monoamine-depleted mouse model, (+)-UH232 combined with a subthreshold dose of the selective N-methyl-D-aspartate (NMDA) antagonist MK801 produced a marked locomotor stimulation (Svensson et al., 1991). This response was blocked effectively and specifically by the highly selective 5HT2A antagonist MDL 100,907, supporting the interpretation that (+)-UH232 might possess 5HT2 receptor agonist properties (Carlsson, 1995). Alternatively, in in vitro studies, the Ki of (+)-UH232 at the cloned r5HT2A receptor in the presence and absence of GTP was the same. This provides no evidence for two sites, indicating that at this receptor, (+)-UH232 is an antagonist (R. Lahti, personal communication). On the other hand, (+)-UH232 has been found to increase 5HT2-mediated phosphoinositol turnover in fibroblasts transfected with the rat 5HT2A receptor, again suggesting agonist action (C. Schmidt, personal communication). [...] A similar picture has been observed in studies in human volunteers, in whom the signs of stimulation following treatment with single doses of (+)-UH232 were especially conspicuous (perception disturbances, hallucinations). In the present study on schizophrenic patients, signs of psychostimulation were evident. [...] While this constellation of actions might well account for the behavioral stimulation induced by this agent, one cannot rule out that the 5HT2 receptor stimulation suggested by the animal experiments referred to above has played a role.
  26. ↑ Carlsson ML (1995). "The selective 5-HT2A receptor antagonist MDL 100,907 counteracts the psychomotor stimulation ensuing manipulations with monoaminergic, glutamatergic or muscarinic neurotransmission in the mouse--implications for psychosis". J Neural Transm Gen Sect. 100 (3): 225–237. doi:10.1007/BF01276460. PMID 8748668. Likewise, MK-801, as well as the muscarine receptor antagonist atropine and the α2-adrenoceptor agonist clonidine, were found to interact synergistically with the putative 5-HT2 receptor agonist UH-232 to produce locomotor activation in monoamine-depleted mice. All these responses were effectively blocked by the highly selective 5-HT2A receptor antagonist MDL 100,907. [...] A finding of serendipity in this laboratory was that the selective DA D-3 and autoreceptor preferring antagonists UH-232 and A J-76 interact synergistically with MK-801 in monoamine-depleted mice (Svensson et al., 1991). This was an unexpected finding since these agents were assumed to lack direct agonist effects on postsynaptic receptors (Svensson, 1986). [...] prompted us to try selective 5-HT2 receptor antagonists like ritanserin and MDL 100,907. Our observations with these latter two compounds support the interpretation that UH-232 possesses 5-HT2 receptor agonist properties. [...] This conclusion is further strengthened by results from ligand binding studies carried out at the Marion Merrell Dow Research Institute (C Schmidt, personal communication) and the Upjohn company (K Svensson, personal communication) showing affinity of UH 232 for the 5-HT2 receptor. Moreover UH-232 was found to increase 5-HT2-mediated phosphoinositol turnover in fibroblasts transfected with the rat 5-HTzA receptor (C Schmidt, personal communication). Interestingly, when given to healthy volunteers, UH-232 has been observed to give rise to both behavioral inhibition and stimulation as well as aberrations of perception of auditory, visual and tactile stimuli (M Larsson, personal communication).
  27. ↑ Walterscheid JP, Nghiem DX, Kazimi N, Nutt LK, McConkey DJ, Norval M, et al. (November 2006). "Cis-urocanic acid, a sunlight-induced immunosuppressive factor, activates immune suppression via the 5-HT2A receptor". Proceedings of the National Academy of Sciences of the United States of America. 103 (46): 17420–17425. doi:10.1073/pnas.0603119103. PMC 1859944. PMID 17085585.
  28. ↑ Shen L, Ji HF (September 2009). "Molecular basis for cis-urocanic acid as a 5-HT(2A) receptor agonist". Bioorganic & Medicinal Chemistry Letters. 19 (18): 5307–5309. doi:10.1016/j.bmcl.2009.07.143. PMID 19683920.
  29. ↑ Menezes AC, Raposo S, Simões S, Ribeiro H, Oliveira H, Ascenso A (March 2016). "Prevention of Photocarcinogenesis by Agonists of 5-HT1A and Antagonists of 5-HT2A Receptors". Molecular Neurobiology. 53 (2): 1145–1164. doi:10.1007/s12035-014-9068-z. PMID 25589005. S2CID 14282500.
  30. ↑ Ahmed A, Choo H, Cho YS, Park WK, Pae AN (July 2009). "Identification of novel serotonin 2C receptor ligands by sequential virtual screening". Bioorganic & Medicinal Chemistry. 17 (13): 4559–4568. doi:10.1016/j.bmc.2009.05.003. PMID 19464901.
  31. ↑ Gatch MB, Kozlenkov A, Huang RQ, Yang W, Nguyen JD, González-Maeso J, et al. (November 2013). "The HIV antiretroviral drug efavirenz has LSD-like properties". Neuropsychopharmacology. 38 (12): 2373–2384. doi:10.1038/npp.2013.135. PMC 3799056. PMID 23702798.
  32. ↑ Rudin D, Ren X, Liechti ME, Huang N, Arias HR (March 2026). "Ibogalogs Activate the 5-HT2A Receptor through a Mechanism Involving Outward and Inward Movements of the Respective Transmembrane Segment TM6 and TM7". Neurochem Res. 51 (2). doi:10.1007/s11064-026-04727-5. PMID 41870698.
  33. ↑ Glennon RA, De Vry J, Spencer DG, Glaser T (December 1990). "Stimulus properties of tiflucarbine: a novel antidepressant agent". Pharmacol Biochem Behav. 37 (4): 769–771. doi:10.1016/0091-3057(90)90561-u. PMID 2151199. THE structurally novel antidepressant tiflucarbine (TVX P 4495) has been demonstrated to act primarily via a serotonergic mechanism (2,3). Tiflucarbine binds both at 5-HT1 and 5-HT2 sites and displays little affinity (i.e., K i >3,000 nM) for adrenergic, dopaminergic, gaba, benzodiazepine, and other binding sites (3). In behavioral studies with rodents, tiflucarbine produces effects indicative of 5-HT1 agonism (such as forepaw treading, hindlimb abduction and flat body posture) and 5-HT2 agonism (such as head-twitch behavior) (3). Whereas its affinity for 5-HTI sites is not particularly high, tiflucarbine binds at 5-HT2 sites with an affinity (K i - 115 nM) comparable to that of the 5-HT2 agonist l-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) (3). Taken together, the available evidence suggests that this agent may be a novel 5-HT2 agonist.
  34. 1 2 Cao D, Yu J, Wang H, Luo Z, Liu X, He L, et al. (January 2022). "Structure-based discovery of nonhallucinogenic psychedelic analogs". Science. 375 (6579): 403–411. Bibcode:2022Sci...375..403C. doi:10.1126/science.abl8615. PMID 35084960. S2CID 246360313.
  35. ↑ Wen Y, Tang L, Duan W, Ren Q, Ni Y, Chen S, et al. (August 2026). "Targeting peripheral 5-HT2AR enhances antitumor immunity in colorectal cancer". Cell. doi:10.1016/j.cell.2026.07.028. PMID 42551424.
  36. ↑ Davis R, Dutheil SS, Zhang L, Lehmann E, Awadallah N, Yao W, et al. (December 2023). "ACNP 62nd Annual Meeting: Poster Abstracts P251 - P500: P358. Discovery and Characterization of ITI-1549, a Novel Non-Hallucinogenic Psychedelic for the Treatment of Neuropsychiatric Disorders". Neuropsychopharmacology. 48 (Suppl 1): 211–354 (272–273). doi:10.1038/s41386-023-01756-4. PMC 10729596. PMID 38040810.
  37. ↑ "Analytical Report NDTDI" (PDF). Nacionalni Forenzični Laboratorij. Slovenia. June 2017.
  38. ↑ Janowsky A, Eshleman AJ, Johnson RA, Wolfrum KM, Hinrichs DJ, Yang J, et al. (July 2014). "Mefloquine and psychotomimetics share neurotransmitter receptor and transporter interactions in vitro". Psychopharmacology. 231 (14): 2771–2783. doi:10.1007/s00213-014-3446-0. PMC 4097020. PMID 24488404.
  39. ↑ Porter RH, Benwell KR, Lamb H, Malcolm CS, Allen NH, Revell DF, et al. (September 1999). "Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells". British Journal of Pharmacology. 128 (1): 13–20. doi:10.1038/sj.bjp.0702751. PMC 1571597. PMID 10498829.
  40. 1 2 Adhikari AS, Yadav A, Pandit S, Kumar S, Pandey VK, Maurya AK, et al. (December 2025). "Synthesis and Evaluation of Novel Aza-Aromatics as Dual 5‑HT2A and 5‑HT2C Receptor Agonists". ACS Med Chem Lett. 16 (12): 2435–2443. doi:10.1021/acsmedchemlett.5c00505. PMID 41404005.
  41. ↑ Knight AR, Misra A, Quirk K, Benwell K, Revell D, Kennett G, et al. (August 2004). "Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 370 (2): 114–123. doi:10.1007/s00210-004-0951-4. PMID 15322733. S2CID 8938111.
  42. ↑ Carlsson ML, Burstein ES, Kloberg A, Hansson S, Schedwin A, Nilsson M, et al. (November 2011). "I. In vivo evidence for partial agonist effects of (-)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors". Journal of Neural Transmission. 118 (11): 1511–1522. doi:10.1007/s00702-011-0704-8. PMID 21874578. S2CID 43580367.
  43. ↑ WO 2023115165, Banister S, Jorgensen W, Jinlong T, "Compounds", published 29 June 2023, assigned to Psylo Pty Ltd.
  44. ↑ WO 2023230649, Banister S, Jorgensen W, Jinlong T, Whish L, "Compounds", published 7 December 2023, assigned to Psylo Pty Ltd.
  45. 1 2 Kaplan AL, Confair DN, Kim K, Barros-Álvarez X, Rodriguiz RM, Yang Y, et al. (October 2022). "Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity". Nature. 610 (7932): 582–591. Bibcode:2022Natur.610..582K. doi:10.1038/s41586-022-05258-z. PMC 9996387. PMID 36171289. S2CID 252598838.
  46. ↑ Kargbo RB (November 2023). "Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment". ACS Medicinal Chemistry Letters. 14 (11): 1498–1500. doi:10.1021/acsmedchemlett.3c00444. PMC 10641896. PMID 37974947.
  47. ↑ WO 2023114472, Manish J, Slocum S, Skiniotis G, Barros X, Jin J, Kaniskan HU, Sun N, Xiong Y, Shen Y, Xu Z, Qui X, Qian C, Song X, Deng Z, Roth B, Biberto J, Kuglae K, Suomivuori CM, Daemgen MA, Dror R, Shoichet B, Kaplan AL, "Heterocyclic compounds as 5ht2a biased agonists.", published 22 June 2023, assigned to Icahn School of Medicine at Mount Sinai, The University of North Carolina at Chapel Hill, The Board of Trustees of The Leland Stanford Junior University, The Regents of The University of California
  48. ↑ Sabnis RW. Novel Fused Heterocycles as 5‑HT2A Receptor Agonists for Treating Neurological Diseases, Namely, Depression, Anxiety, Substance Abuse, and Headaches. ACS Med Chem Lett. 2025 Aug 13;16(9):1715-1716. doi:10.1021/acsmedchemlett.5c00477 PMID 40959255
  49. ↑ Wu Y, Vigneron S, Braz J, Srinivasan K, Fink EA, Huang XP, Xu X, Huebner H, Kim JY, Wang J, Pfeiffer T, Sakamoto K, Radchenko DS, Rodriguiz RM, Moroz YS, Irwin JJ, Gmeiner P, Billesboelle C, Roth BL, Basbaum AI, Manglik A, Wetsel WC, Shoichet BK. Large Library Docking for Polypharmacology. J Med Chem. 2026 Mar 12;69(5):6210-6229. doi:10.1021/acs.jmedchem.5c03810 PMID 41712624
  50. ↑ Silva ME, Heim R, Strasser A, Elz S, Dove S (January 2011). "Theoretical studies on the interaction of partial agonists with the 5-HT2A receptor". Journal of Computer-Aided Molecular Design. 25 (1): 51–66. Bibcode:2011JCAMD..25...51S. CiteSeerX 10.1.1.688.2670. doi:10.1007/s10822-010-9400-2. PMID 21088982. S2CID 3103050. {{cite journal}}: Cite uses deprecated parameter |citeseerx= (help)
  51. ↑ WO 2007149728, Mohapatra S, Hellberg MR, Feng Z, "Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma", assigned to Alcon Manufacturing, Ltd.
  52. ↑ Cameron LP, Tombari RJ, Lu J, Pell AJ, Hurley ZQ, Ehinger Y, et al. (January 2021). "A non-hallucinogenic psychedelic analogue with therapeutic potential". Nature. 589 (7842): 474–479. Bibcode:2021Natur.589..474C. doi:10.1038/s41586-020-3008-z. PMC 7874389. PMID 33299186.
  53. ↑ WO 2007/025144, Kozikowski A, Kurome T, Setola V, Roth B, "5-ht2c receptor agonists as anorectic agents", published 1 March 2007, assigned to University Of Illinois - Chicago
  54. ↑ Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP. Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. J Med Chem. 2017 Jul 27;60(14):6273-6288. doi:10.1021/acs.jmedchem.7b00584 PMID 28657744
  55. ↑ Sabb AL, Vogel RL, Welmaker GS, Sabalski JE, Coupet J, Dunlop J, et al. (May 2004). "Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor". Bioorganic & Medicinal Chemistry Letters. 14 (10): 2603–7. doi:10.1016/j.bmcl.2004.02.100. PMID 15109661.
  56. 1 2 3 4 5 6 7 8 Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, et al. (December 2023). "AlphaFold2 structures template ligand discovery". bioRxiv 10.1101/2023.12.20.572662.
  57. ↑ Taylor EW, Nikam S, Weck B, Martin A, Nelson D (October 1987). "Relative selectivity of some conformationally constrained tryptamine analogs at 5-HT1, 5-HT1A and 5-HT2 recognition sites". Life Sci. 41 (16): 1961–1969. doi:10.1016/0024-3205(87)90749-1. PMID 3657392.
  58. ↑ Heng HL, Chee CF, Thy CK, Tee JT, Chin SP, Herr DR, et al. (February 2019). "In vitro functional evaluation of isolaureline, dicentrine and glaucine enantiomers at 5-HT2 and α1 receptors". Chem Biol Drug Des. 93 (2): 132–138. doi:10.1111/cbdd.13390. PMID 30216681.
  59. ↑ Madapa S, Harding WW (April 2015). "Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors". J Nat Prod. 78 (4): 722–729. doi:10.1021/np500893h. PMID 25695425.
  60. 1 2 3 Qin W, Zhang B, Wang Q, Jiang G, Cui J, Chen F, et al. (November 2025). "Discovery of New N-H Aporphine Derivatives As Brain-Penetrant Gq-Biased 5-HT2C Receptor Agonists and Dual 5-HT2C/5-HT2A Receptor Agonists". J Med Chem. 68 (21): 23300–23323. doi:10.1021/acs.jmedchem.5c02115. PMID 41108743. Notably, the (2-methylallyl)oxy analogue 20s exhibited the highest potency at 5-HT2AR (EC50 = 6.3 nM, Emax = 82%) in this report, while displaying comparable potency at 5-HT2CR (EC50 = 8.0 nM, Emax = 95%).
  61. 1 2 3 "Aporphine derivative and preparation method and application thereof". Google Patents. 14 June 2022. Retrieved 4 April 2026.
  62. ↑ Li R, Yan H, Chen Y, Liu Y, Tang L, Yu J, et al. (October 2025). "Structure-Guided Design of Novel 5-HT2A Partial Agonists as Psychedelic Analogues with Antidepressant Effects". J Med Chem. 68 (20): 21683–21700. doi:10.1021/acs.jmedchem.5c02045. PMID 41087124.
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