Chemistry:HBL20017

From HandWiki

HBL20017, also known as 4-fluoro-5-methylthio-N,N-dimethyltryptamine (4-F-5-MeS-DMT), is a non-selective and putatively non-hallucinogenic serotonin receptor agonist of the tryptamine family related to 5-MeO-DMT which is being investigated for the potential treatment of obsessive–compulsive disorder (OCD).[1][2] It is the 4-fluoro derivative of 5-MeS-DMT and the 5-methylthio derivative of 4-fluoro-DMT.[2]

The drug acts as an agonist of the serotonin 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C receptors.[1][2] Its activational potencies (EC50) are 1.21 to 1.84 nM for the serotonin 5-HT1A receptor, 6.37 to 7.95 nM for the serotonin 5-HT2A receptor, 17.1 nM for the serotonin 5-HT2B receptor, and 0.80 to 22.56 nM for the serotonin 5-HT2C receptor.[1][2] Despite acting as a serotonin 5-HT2A receptor agonist, HBL20017 did not produce the head-twitch response (HTR), a behavioral proxy of psychedelic effects, in rodents, and hence appears to be non-hallucinogenic.[1][2] A related drug, HBL20016 (5-MeS-6-F-DMT), did robustly produce the HTR on the other hand, and thus may be hallucinogenic.[1][2]

HBL20017 has shown antiobsessional-like effects in rodents, for instance against obsessive marble burying and obsessive self-grooming.[1][2] HBL20017 produced antiobsessional effects in SAPAP3 knockout mice (an obsessional self-grooming model) that were apparent within 48 hours and that lasted for as long as 42 days following a single dose.[1][2] HBL20016 also showed antiobsessional-like effects but was not as effective as HBL20017.[1] HBL20017 might be more effective than psilocybin in terms of antiobsessional effects, at least based on animal studies.[1]

The chemical synthesis of HBL20017 has been described.[2]

HBL20017 was first described in the scientific literature by Alan P. Kozikowski and colleagues in December 2024.[1][2] It was developed by Negev Labs and Parow Entheobiosciences.[1] The drug is in the preclinical research stage of development.[1]

See also

References

  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 "ACNP 63rd Annual Meeting: Poster Abstracts P609-P914: P660. A Novel, Non-Hallucinogenic Psychedelic for the Treatment of Obsessive-Compulsive Disorder". Neuropsychopharmacology 49 (Suppl 1): 418–594 (448–449). December 2024. doi:10.1038/s41386-024-02013-y. PMID 39643635. 
  2. ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 "Compounds and uses thereof as modulators of serotonin receptors". 10 April 2025. https://patents.google.com/patent/WO2025220005A1/en.