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]
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| Other names | HBL-20017; 4-Fluoro-5-methylthio-N,N-dimethyltryptamine; 4-F-5-MeS-DMT |
| Drug class | Serotonin receptor agonist; Serotonin 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C receptor agonist; Non-hallucinogenic serotonin 5-HT2A receptor agonist; Antiobsessional agent |
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| Formula | C13H17FN2S |
| Molar mass | 252.35 g·mol−1 |
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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
editReferences
edit- 1 2 3 4 5 6 7 8 9 10 11 12 Lerer B, Golding P, Brownstien M, Kozikowski A, Lifschytz T (December 2024). "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). doi:10.1038/s41386-024-02013-y. PMID 39643635.
- 1 2 3 4 5 6 7 8 9 10 "Compounds and uses thereof as modulators of serotonin receptors". Google Patents. 10 April 2025. Retrieved 4 April 2026.