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CPI-CG-8

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Pharmaceutical compound
CPI-CG-8
Clinical data
Other namesN-Methyl-N-(2-indolylethyl)tryptamine
Drug class Serotonin 5-HT2C receptor agonist
ATC code
  • None
Chemical and physical data
Formula C21H23N3
Molar mass 317.436g·mol−1
3D model (JSmol)
  • CN(CCC1=CNC2=CC=CC=C12)CCC3=CC(C=CC=C4)=C4N3
  • InChI=1S/C21H23N3/c1-24(12-10-17-15-22-21-9-5-3-7-19(17)21)13-11-18-14-16-6-2-4-8-20(16)23-18/h2-9,14-15,22-23H,10-13H2,1H3
  • Key:PJYCXUOZLVUZNU-UHFFFAOYSA-N

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 1,000nM, had an activational potency (EC50 Tooltip half-maximal effective concentration) of 12.46nM, and showed an activational efficacy (Emax Tooltip maximal efficacy) 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

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References

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  1. 1 2 3 4 5 Jones T, Harris JS, Raman R, Ekins S (2025). "Discovery of a selective 5-HT2C agonist by generative machine learning using MegaSyn with applications to treating opioid use disorder". Neurotherapeutics. 22 (4) e00655. doi:10.1016/j.neurot.2025.e00655 . Retrieved 27 March 2026.
  2. 1 2 3 4 Ekins S (6 February 2024). Applying Artificial Intelligence in a Small Drug Discovery Company. SLAS 2024, Boston, MA, February 3-7, Boston Convention and Exhibition Center. 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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