Deupsilocin

Deupsilocin
Clinical data
Other namesPsilocin-d10; Psilocin-D10; HLP003; HLP-003; CYB003; CYB-003; Deuterated psilocybin analogue; Deuterated psilocin analogue; Deuterated psilocin; Decadeuteropsilocin
Routes of
administration		Oral[1]
Drug classSerotonergic psychedelic; Hallucinogen[1][2]
Pharmacokinetic data
Onset of action<15 minutes[3]
Duration of action4–6 hours[3]
Identifiers
  • 3-[2-[bis(trideuteriomethyl)amino]-1,1,2,2-tetradeuterioethyl]-1H-indol-4-ol
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC12H16N2O
Molar mass204.273 g·mol−1
3D model (JSmol)
  • [2H]C([2H])([2H])N(C([2H])([2H])[2H])C([2H])([2H])C([2H])([2H])C1=CNC2=C1C(=CC=C2)O
  • InChI=1S/C12H16N2O/c1-14(2)7-6-9-8-13-10-4-3-5-11(15)12(9)10/h3-5,8,13,15H,6-7H2,1-2H3/i1D3,2D3,6D2,7D2
  • Key:SPCIYGNTAMCTRO-HXOHQZFQSA-N

Deupsilocin (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; former developmental code names HLP003 and CYB0003), also known as deuterated psilocin or as psilocin-d10, is a psychedelic drug of the tryptamine family related to psilocin which is under development for the treatment of major depressive disorder, alcoholism, and other psychiatric disorders.[1][4][5][6][7][2][8] It is taken orally.[1] The drug is a deuterated isotopologue of psilocin with altered pharmacokinetics.[1][5][6][2]

Interactions

Pharmacology

The pharmacodynamic profile of deupsilocin, including its interactions with serotonin receptors and its effects in animals, is similar to that of psilocin.[2] As with psilocin, deupsilocin is a potent agonist of the serotonin 5-HT2A receptor and produces psychedelic-like effects in animals.[2] However, it was developed to have improved pharmacokinetic properties compared to psilocybin, including reduced variability in circulating levels, a faster onset of action, and a shorter duration.[8]

In humans, deupsilocin has been reported to have 2.2-fold higher peak levels and 3.5-fold higher area-under-the-curve (AUC) levels than psilocybin at equivalent doses.[3] It is said to have a rapid onset of less than 15 minutes and a duration of 4 to 6 hours.[3]

Chemistry

Analogues

In addition to deupsilocin, Helus Pharma has also patented other deuterated psilocin isotopologues.[9] Other deuterated drugs related to deupsilocin include the deuterated dimethyltryptamine (DMT) isotopologues deudimethyltryptamine (HLP004; CYB004; DMT-d10; deudimethyltryptamine) and SPL028 (D2-DMT) and the deuterated phenethylamine HLP005 (CYB005).[5][10]

Research

In 2024, deupsilocin received a breakthrough therapy designation from the U.S. FDA[11] and was in phase 3 clinical trials for major depressive disorder and is in the preclinical stage of development for alcoholism and other psychiatric disorders.[1][4][12] Two phase 3 clinical trials for major depressive disorder are being initiated in November 2024 and February 2025.[1][4][12] The drug is under development by Helus Pharma (formerly Cybin).[1][4][12]

See also

References

  1. 1 2 3 4 5 6 7 8 "Deupsilocin". AdisInsight. 4 October 2024. Retrieved 23 October 2024.
  2. 1 2 3 4 5 Palfreyman M, Krakowsky J, Morgan M, Canal C, Pathare P, Avery K, et al. (December 2022). "ACNP 61st Annual Meeting: Poster Abstracts P271-P540: P361. In Vitro and In Vivo Profile of CYB003: A Novel, Deuterated Psilocybin Analog for the Potential Treatment of Major Depressive Disorder" (PDF). Neuropsychopharmacology. 47 (Suppl 1): 220–370 (271). doi:10.1038/s41386-022-01485-0. PMC 9714399. PMID 36456694.
  3. 1 2 3 4 "Corporate Presentation - Helping Minds Heal" (PDF). s28.q4cdn.com. March 2026. Archived from the original (PDF) on 2026-03-27.
  4. 1 2 3 4 "Delving into the Latest Updates on CYB-003 with Synapse". Synapse. 12 October 2024. Retrieved 23 October 2024.
  5. 1 2 3 Cano GH, Dean J, Abreu SP, Rodríguez AH, Abbasi C, Hinson M, et al. (December 2022). "Key Characteristics and Development of Psychoceuticals: A Review". Int J Mol Sci. 23 (24) 15777. doi:10.3390/ijms232415777. PMC 9779201. PMID 36555419.
  6. 1 2 Di Martino RM, Maxwell BD, Pirali T (July 2023). "Deuterium in drug discovery: progress, opportunities and challenges". Nat Rev Drug Discov. 22 (7): 562–584. doi:10.1038/s41573-023-00703-8. PMC 10241557. PMID 37277503.
  7. ↑ Rhee TG, Davoudian PA, Sanacora G, Wilkinson ST (December 2023). "Psychedelic renaissance: Revitalized potential therapies for psychiatric disorders". Drug Discov Today. 28 (12) 103818. doi:10.1016/j.drudis.2023.103818. PMID 37925136.
  8. 1 2 Inamdar A, Morgan M, Krakowsky J, Reichelt A, Canal C, Mueller T, et al. (December 2022). "ACNP 61st Annual Meeting: Poster Abstracts P271-P540: P362. Pharmacokinetic Profile of CYB003: A Novel, Deuterated Psilocybin Analog for the Potential Treatment of Major Depressive Disorder" (PDF). Neuropsychopharmacology. 47 (Suppl 1): 220–370 (271–272). doi:10.1038/s41386-022-01485-0. PMC 9714399. PMID 36456694.
  9. ↑ "Deuterated tryptamine derivatives and methods of use". Google Patents. 17 July 2023. Retrieved 23 October 2024. Binding affinity (Ki) and functional potency (EC50) values of PI and PI-α-d2 are summarized in Table 1. Deuteration was found to have little effect on the affinity and function at key receptor targets. [...] TABLE 1: PI and PI-α,α-d2 Affinities and Functions at Target Serotonin Receptors [...]
  10. ↑ Peplow M (June 2024). "Next-generation psychedelics: should new agents skip the trip?". Nat Biotechnol. 42 (6): 827–830. doi:10.1038/s41587-024-02285-1. PMID 38831049.
  11. ↑ Jenkins C (19 March 2024). "FDA grants breakthrough designation to psilocybin analog for major depressive disorder". Healio. Retrieved 7 August 2025.
  12. 1 2 3 Kuntz L (10 February 2025). "CYB003 for the Adjunctive Treatment of Major Depressive Disorder". Psychiatric Times. Retrieved 7 August 2025.
This page is issued from Wikipedia. The text is available under Creative Commons Attribution-Share Alike 4.0 unless otherwise noted. Additional terms may apply for the media files.