CYB210010 explained

CYB210010, also known as 2C-T-TFM, is a lesser-known psychedelic drug of the phenethylamine family related to compounds such as 2C-T and 2C-T-21.

Alexander Shulgin attempted to synthesise this compound in the 1990s, and mentions it in his book PiHKAL under the entry for 2C-T-21, but was unsuccessful in producing a key intermediate and never assigned it a 2C-T number. This compound was ultimately first synthesised by Geoffrey Varty and colleagues at Irish biopharmaceutical company Cybin in 2023.

It has a K_i of 0.35nM at the serotonin 5-HT_2A receptor, and an of 4.1nM at the serotonin 5-HT_2A receptor and 7.3nM at the serotonin 5-HT_2C receptor, compared to 88nM at the serotonin 5-HT_2B receptor.^[1] It is a potent, selective, long acting, and orally active agonist for the serotonin 5-HT_2A and 5-HT_2C receptors and produces psychedelic-like responding in several different animal species.^{[2] [3]} It has only been studied preclinically as of 2024 and is not known to have been tested in humans.

Related drugs include the deuterated phenethylamine CYB005 and the deuterated substituted tryptamines CYB003 and CYB004.^{[4] [5]}

See also

• 2C (psychedelics)
• 2C-T-21.5
• 2C-T-28
• 2C-TFM
• 2C-TFE
• 3C-DFE
• DOPF
• Tiflorex
• Trifluoromescaline

Notes and References

1. WO . 2023156450 . Therapeutic phenethylamine compositions and methods of use . Nivorozhkin A, JA Hartsel, Canal CE, Salituro FG, Mueller TA, Greene BJ, Belser A, Avery KL, Reichelt AC, Varty GB, Palfreyman M . Cybin Irl Limited . 24 August 2023 .
2. Varty GB, Canal CE, Mueller TA, Hartsel JA, Tyagi R, Avery K, Morgan ME, Reichelt AC, Pathare P, Stang E, Palfreyman MG, Nivorozhkin A . Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist . Journal of Medicinal Chemistry . 67 . 8 . 6144–6188 . April 2024 . 38593423 . 10.1021/acs.jmedchem.3c01961 .
3. Palfreyman M, Varty G, Canal C, Hartsel J, Tyagi R, Avery K, Morgan M, Mueller T, Reichelt A, Pathare P, Stang E, Nivorozhkin A . December 2023 . ACNP 62nd Annual Meeting: Poster Abstracts P251 – P500: P405. Discovery and Preclinical Characterization of the Phenylalkylamine, CYB210010, a Potent and Long-Acting Serotonin 5-HT2A Receptor Agonist . Neuropsychopharmacology . 48 . Suppl 1 . 211–354 (299–299 . 10.1038/s41386-023-01756-4 . 38040810 . 10729596 .
4. Cano GH, Dean J, Abreu SP, Rodríguez AH, Abbasi C, Hinson M, Lucke-Wold B . Key Characteristics and Development of Psychoceuticals: A Review . Int J Mol Sci . 23 . 24 . December 2022 . 15777 . 36555419 . 9779201 . 10.3390/ijms232415777 . free .
5. Peplow M . Next-generation psychedelics: should new agents skip the trip? . Nat Biotechnol . 42 . 6 . 827–830 . June 2024 . 38831049 . 10.1038/s41587-024-02285-1 .