Chemistry:4-Allyl-6-oxa-noribogainalog
4-Allyl-6-oxa-noribogainalog is a κ-opioid receptor (KOR) agonist of the oxa-ibogalog family related to oxa-noribogaine.[1][2] It is a highly potent full agonist of the KOR, with an EC50 of 1 nM and an Emax of 103% in a G protein BRET assay.[1][2] This is dramatically more potent than oxa-noribogaine or noribogaine at the KOR in the same assay per another study by the same group (EC50 (Emax) = 43 nM (82%) and 6,100 nM (52%), respectively).[3][2] The drug shows considerable selectivity for activation of the KOR over activation of the μ- and δ-opioid receptors.[1][2] 4-Allyl-6-oxa-noribogainalog was the most potent KOR agonist in a series of oxa-ibogalog compounds.[1][2] It was patented by Dalibor Sames and colleagues in 2025, with Sames being a co-founder of Gilgamesh Pharmaceuticals.[1][2]
See also
- κ-Opioid receptor agonist
- Ibogalog § Related compounds
- List of investigational hallucinogens and entactogens
- GM-3009
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "Advances in Psychedelic Therapeutics: Multimodal Iboga Analogs, EEG-Guided Psilocybin Dosing, and Optimized Harmine-DMT Formulations". ACS Medicinal Chemistry Letters 17 (1): 72–74. January 2026. doi:10.1021/acsmedchemlett.5c00714. PMID 41531985.
- ↑ 2.0 2.1 2.2 2.3 2.4 2.5 Sames D, Havel V, "Novel analogs of oxa-iboga class of therapeutics", WO patent 2025166273A1, published 7 August 2025
- ↑ "Oxa-Iboga alkaloids lack cardiac risk and disrupt opioid use in animal models". Nature Communications 15 (1). September 2024. doi:10.1038/s41467-024-51856-y. PMID 39304653. Bibcode: 2024NatCo..15.8118H.
 |  |
