Chemistry:CPI-CG-8

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CPI-CG-8, also known as N-methyl-N-(2-indolylethyl)tryptamine, is a "relatively" selective serotonin 5-HT2C receptor agonist of the tryptamine family.[1][2]

At the serotonin 5-HT2C receptor, it showed 99.4% binding inhibition (a measure of affinity) at a concentration of 1,000 nM, had an activational potency (EC50) of 12.46 nM, and showed an activational efficacy (Emax) of approximately 80%.[2] The pharmacokinetics of CPI-CG-8 in rodents have been studied.[1]

The drug was developed by Collaborations Pharmaceuticals and was derived via modification of the psychedelic drug psilocin using generative machine learning through a platform called MegaSyn.[1][2] CPI-CG-8 was first described in the scientific literature by 2024.[2][1] It is of interest for the potential treatment of opioid use disorder and other conditions.[1]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "Discovery of a selective 5-HT2C agonist by generative machine learning using MegaSyn with applications to treating opioid use disorder". Neurotherapeutics 22 (4). 2025. doi:10.1016/j.neurot.2025.e00655. https://linkinghub.elsevier.com/retrieve/pii/S1878747925001333. Retrieved 27 March 2026. 
  2. ↑ 2.0 2.1 2.2 2.3 "Applying Artificial Intelligence in a Small Drug Discovery Company". SLAS 2024, Boston, MA, February 3-7, Boston Convention and Exhibition Center. 6 February 2024. https://slas2024.eventscribe.net/fsPopup.asp?efp=UkFYWkZaU1cyMDM1NQ&PresentationID=1334212&rnd=0.1063697&mode=presInfo.  Slides. Slide #28. "[Slide 28:] First Round of Generative Design Validation: Starting point Psilocin. 5-HT2C agonists - obesity, psychiatric disorders, sexual dysfunction and urinary incontinence. 10 molecules synthesized - tested vs 5-HT2A, 2B, 2C at Eurofins at 1µM. 1 compound was selective vs 5-HT2C 99.4% inhibition - retested in dose response. CPI-CG-8 EC50 = 12.46nM, Serotonin (control) = 1.9 nM, (reference Lorcaserin = 9 nM). MACCS similarity to psilocin: 0.67 - IP dosing in mice - good brain levels. [Figures]. Jones et al., Manuscript submitted, Provisional patent submitted."



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