O-1057

O-1057 is an amino ester of Δ8-tetrahydrocannabinol, designed to be more potent than Δ9-tetrahydrocannabinol and to dissolve in water. Classical cannabinoids dissolve poorly in water and require a solubilising agent that may itself have pharmacological activity; esterifying the phenol at position 1 with 4-morpholinobutyric acid, used as the hydrochloride salt, yields a compound soluble in water or in saline solution. On membranes of CHO cells expressing the CB1 and CB2 receptors, its pKi is 8.36 for CB1 and 7.95 for CB2, that is, affinities in the nanomolar range, and it inhibits cyclic AMP with a pEC50 of 9.16 and 9.72 (Pertwee et al., 2000). In mice, intravenous injection reduces spontaneous activity, lowers rectal temperature and produces antinociception with an ED50 of 0.02 mg/kg, an effect that SR 141716A blocks. In rats, the agonist is self-administered into the shell of the nucleus accumbens, and rats selected for their preference for alcohol self-administer it at lower concentrations and at a higher rate than Wistar rats (Hauser et al., 2020). The authors judge its clinical potential as an analgesic worth investigating, but no human data are published: no pharmacokinetics, no characterised metabolism, no clinical trial, no safety profile.

Source

Synthetic molecule, with no plant species recorded in the reference data. It was described as a new water-soluble cannabinoid, studied in cells and rodents, and the sources consulted do not report it in any food or cosmetic product.

No biosynthetic pathway: the molecule is obtained by organic synthesis and belongs to the class of water-soluble amino esters of tetrahydrocannabinols, used as the hydrochloride salt.

European Union

No harmonised measure at European Union level has been found in the sources consulted: control therefore falls to national legislation. Internationally, the molecule is not named in the 2026 Green List of the International Narcotics Control Board, which lists isomers of tetrahydrocannabinol all bearing a pentyl chain at position 3 and a free hydroxyl at position 1, which O-1057 is not. No marketing authorisation and no clinical trial has been found in the sources consulted.

France

Narcotic status in France through a generic clause. O-1057 is named by its code in no annex of the ANSM consolidated list updated on 16 February 2026. Annex III does, however, name « tetrahydrocannabinols, their esters, ethers, salts and the salts of the aforementioned derivatives », and the text does not settle whether that entry extends to a molecule whose position-3 chain differs; this sheet therefore relies only on the clause. The clause covers any substance derived from the benzo[c]chromene nucleus, un-, partially or fully hydrogenated on ring A (the unsaturated ring bearing the methyl at position 9), and substituted at one of the places it lists; the list cites the decision of 22 May 2024 in the same entry. O-1057 meets each of its conditions. The skeleton is that of Δ8-tetrahydrocannabinol; the hydroxyl at position 1 is esterified, a case the clause expressly provides for; position 3 carries a cyanoalkyl chain itself substituted by two methyl groups, also provided for; position 6 carries two alkyl groups and position 9 a methyl. None of the clause's exceptions (cannabinol, cannabinolic acid, THCV, THCVA and THCA, under their conditions) applies. No marketing authorisation and no admission as a food or cosmetic ingredient has been found in the sources consulted, and the classification opens no right of use.

Sources: EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA. Our method.

1. 1Pertwee et coll., O-1057, un agoniste cannabinoïde hydrosoluble puissant aux propriétés antinociceptives, Br J Pharmacol 2000 (new tab)PMID 10780961
2. 2Lichtman et coll., Évaluation pharmacologique de cannabinoïdes administrés en aérosol chez la souris, Eur J Pharmacol 2000 (new tab)PMID 10884513
3. 3Martin et coll., Caractérisation pharmacologique de nouveaux cannabinoïdes hydrosolubles, J Pharmacol Exp Ther 2006 (new tab)PMID 16757541
4. 4Hauser et coll., Sélection pour la préférence pour l'alcool et sensibilité accrue au renforcement cannabinoïde dans la coquille du noyau accumbens, Pharmacol Biochem Behav 2020 (new tab)PMID 32710885
5. 5PubChem, composé CID 9829239 (O-1057), National Library of Medicine (new tab)
6. 6ANSM, liste consolidée des substances classées comme stupéfiants, mise à jour du 16 février 2026 (clause du noyau benzo[c]chromène) (new tab)
7. 7ANSM, décision du 22 mai 2024 portant modification de la liste des substances classées comme stupéfiants (new tab)
8. 8OICS, Liste verte 2026 des substances psychotropes sous contrôle international (convention de 1971) (new tab)

SMILES

CC1=CC[C@@H]2[C@@H](C1)c1c(OC(=O)CCCN3CCOCC3)cc(C(C)(C)CCCCC#N)cc1OC2(C)C

InChIKey

YRDNBEPFVBMTNP-CLJLJLNGSA-N

Machine-readable entry (JSON)

LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.