Chemistry:Tabernanthalog
Tabernanthalog (TBG; developmental code name DLX-007) is a non-selective serotonin receptor modulator and putatively non-psychedelic psychoplastogen of the ibogalog group related to the iboga alkaloid tabernanthine but with a simplified chemical structure.[1][2] It was developed by David E. Olson and colleagues at the University of California, Davis.[2] The drug is being developed by Delix Therapeutics as a potential pharmaceutical drug for treatment of neuropsychiatric disorders.[3][4]
Use and effects
There have been informal anecdotal reports of the effects of tabernanthalog.[5][6][7] It is said to be psychoactive and mildly hallucinogenic at sufficiently high doses and to have a long duration.[6] Its hallucinogenic effects have been said to be similar to but weaker than those of serotonergic psychedelics.[6][7] There were also reports of side effects like nausea, dizziness, stomach discomfort, and diarrhea.[6][7] However, it is unclear whether the reports have always employed actual tabernanthalog.[6]
Interactions
Pharmacology
Pharmacodynamics
| Target | Affinity (Ki, nM) |
|---|---|
| 5-HT1A | 39% BI @ 10 μM 14,600 (EC50) 95% (Emax) |
| 5-HT1B | 66% BI @ 10 μM 34 (EC50) 87% (Emax) |
| 5-HT1D | ND (Ki) 2,180 (EC50) 76% (Emax) |
| 5-HT1E | ND (Ki) 2,784 (EC50) 117% (Emax) |
| 5-HT1F | ND (Ki) 40 (EC50) 64% (Emax) |
| 5-HT2A | 4,440 (Ki) 57% BI @ 10 μM 147–4,570 (EC50) 8–91% (Emax) |
| 5-HT2B | 439 (Ki) 86% BI @ 10 μM 2,827 or IA (EC50) 46% or IA (Emax) |
| 5-HT2C | 28,590 (Ki) 99% BI @ 10 μM 13–69 (EC50) 21–99% (Emax) |
| 5-HT3 | 14% BI @ 10 μM |
| 5-HT4 | ND (Ki) >10,000 (EC50) |
| 5-HT5A | ND (Ki) >10,000 (EC50) |
| 5-HT6 | ND (Ki) 132–214 (EC50) 88–133% (Emax) |
| 5-HT7 | ND (Ki) >10,000 (EC50) |
| α1A–α1D | 15–20% BI @ 10 μM |
| α2A | 81% BI @ 10 μM |
| α2B | 27% BI @ 10 μM |
| α2C | ND |
| β1–β2 | 9% BI @ 10 μM |
| D1, D2 | 3–18% BI @ 10 μM |
| D3–D5 | ND |
| H1 | 35% BI @ 10 μM |
| H2 | –12% BI @ 10 μM |
| H3, H4 | ND |
| M1–M4 | 2–18% BI @ 10 μM |
| M5 | ND |
| nACh | 16–19% BI @ 10 μM |
| I1, I2 | ND |
| σ1, σ2 | ND |
| MOR | 17% BI @ 10 μM IA (EC50) |
| DOR | 14% BI @ 10 μM IA (EC50) |
| KOR | 7% BI @ 10 μM >10,000 (EC50) |
| NMDAR | 0–3% BI @ 10 μM (rat) |
| TAAR1 | ND |
| SERT | 88% BI @ 10 μM 600 (IC50) |
| NET | ND (Ki) 5,400 (IC50) |
| DAT | ND (Ki) 65,000 (IC50) |
| VMAT | 10% BI @ 10 μM |
| MAO-A | 66% BI @ 10 μM 15,100 (IC50) |
| MAO-B | 16% BI @ 10 μM 28% FI @ 100 μM |
| Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: [2][8][1][9][10][11] | |
Tabernanthalog is a non-selective and non-psychedelic serotonin receptor modulator, including acting as an agonist of the serotonin 5-HT1B, 5-HT1F, 5-HT2A, 5-HT2C, and 5-HT6 receptors and as an agonist or antagonist of the serotonin 5-HT2B receptor.[2][8][10] It also shows significant binding to the serotonin transporter (SERT) (acting as a serotonin reuptake inhibitor), the α2A-adrenergic receptor, and monoamine oxidase A (MAO-A).[2] In contrast to iboga alkaloids like ibogaine and noribogaine, tabernanthalog showed negligible interactions with opioid receptors, the NMDA receptor, and certain nicotinic acetylcholine receptors.[2] However, in subsequent research, it weakly inhibited certain nicotinic acetylcholine receptors, as well as, to a much lesser extent, the GABAA receptor.[12] Tabernanthalog was found to be 100-fold less potent at the hERG antitarget compared to ibogaine, and hence is thought to have a much lower potential for cardiotoxicity.[2]
Tabernanthalog did not produce the head-twitch response, a behavioral proxy of psychedelic effects, in rodents, and hence appears to be non-hallucinogenic.[2] However, it was found to promote structural neuroplasticity (i.e., to act as a psychoplastogen), reduce drug-seeking behavior, and produce antidepressant-like effects.[2][13][14][15] It has also been shown that it reduces motivation for heroin and alcohol in rodents.[15]
History
Tabernanthalog was first described in the scientific literature by David E. Olson and colleagues at the University of California, Davis in January 2021.[2][16]
Society and culture
Grey market use
Tabernanthalog has been known to be sold online by research chemical vendors for purposes such as "nootropic" use.[6]
Legal status
Canada
Tabernanthalog is not a controlled substance in Canada.[17]
United States
Tabernanthalog is not an explicitly controlled substance in the United States.[18]
Research
Tabernanthalog is under development for the treatment of central nervous system disorders (CNS disorders).[3][19] It is being developed by Delix Therapeutics.[3][19] As of May 2025, no recent development has been reported.[3] It had reached the preclinical research stage of development.[3][19] A phase 1 clinical trial was being planned for the first half of 2023.[3] Delix Therapeutics also partnered with National Institute on Drug Abuse (NIDA) to evaluate tabernanthalog for the treatment of substance-related disorders in December 2021.[3]
See also
- Ibogalog
- Tabernanthine
- Catharanthalog
- DLX-159
- Ibogainalog
- Ibogaminalog (DM-506)
- Noribogainalog
- PNU-22394
- Non-hallucinogenic 5-HT2A receptor agonist
References
- ↑ 1.0 1.1 "Neuropsychopharmacology of hallucinogenic and non-hallucinogenic 5-HT2A receptor agonists". Br J Pharmacol. May 2025. doi:10.1111/bph.70050. PMID 40405723.
- ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 "A non-hallucinogenic psychedelic analogue with therapeutic potential". Nature 589 (7842): 474–479. January 2021. doi:10.1038/s41586-020-3008-z. PMID 33299186. Bibcode: 2021Natur.589..474C.
- ↑ 3.0 3.1 3.2 3.3 3.4 3.5 3.6 "DLX 7". 28 May 2025. https://adisinsight.springer.com/drugs/800063581.
- ↑ "Can we take the high out of psychedelics?". Wired. 6 March 2021. https://www.wired.co.uk/article/psychedelics-without-the-high. Retrieved 12 July 2022.
- ↑ Love, Shayla (20 October 2024). "Tripping on Nothing". https://www.theatlantic.com/health/archive/2024/10/psychedelic-trip-high-hallucination-medicine/680314/.
- ↑ 6.0 6.1 6.2 6.3 6.4 6.5 Hardman, Josh (19 July 2023). "Non-Hallucinogenic Trip Reports: Searching for the Tabernanthalog Tasters". https://psychedelicalpha.com/news/non-hallucinogenic-trip-reports-searching-for-the-tabernanthalog-tasters.
- ↑ 7.0 7.1 7.2 Juliani, Arthur (30 December 2023). "A Phenomenological Report on the Novel Non-Hallucinogenic Psychedelic Tabernanthalog". https://awjuliani.medium.com/a-phenomenological-report-on-the-novel-non-hallucinogenic-psychedelic-tabernanthalog-ed2fc601c1dc.
- ↑ 8.0 8.1 "Non-hallucinogenic compounds derived from iboga alkaloids alleviate neuropathic and visceral pain in mice through a mechanism involving 5-HT2A receptor activation". Biomed Pharmacother 177. August 2024. doi:10.1016/j.biopha.2024.116867. PMID 38889634.
- ↑ "Evidence that 5-HT2A receptor signalling efficacy and not biased agonism differentiates serotonergic psychedelic from non-psychedelic drugs". Br J Pharmacol. June 2025. doi:10.1111/bph.70109. PMID 40545270.
- ↑ 10.0 10.1 "The psychoplastogens ibogaminalog and ibogainalog induce antidepressant-like activity in naïve and depressed mice by mechanisms involving 5-HT2A receptor activation and serotonergic transmission". Prog Neuropsychopharmacol Biol Psychiatry 136. January 2025. doi:10.1016/j.pnpbp.2024.111217. PMID 39662723.
- ↑ "Ibogalogs decrease neuropathic pain in mice through a mechanism involving crosstalk between 5-HT2A and mGlu2 receptors". Biomed Pharmacother 184. March 2025. doi:10.1016/j.biopha.2025.117887. PMID 39938347.
- ↑ "Tabernanthalog and ibogainalog inhibit the α7 and α9α10 nicotinic acetylcholine receptors via different mechanisms and with higher potency than the GABAA receptor and CaV2.2 channel". Biochem Pharmacol 223. May 2024. doi:10.1016/j.bcp.2024.116183. PMID 38580167.
- ↑ "An analog of psychedelics restores functional neural circuits disrupted by unpredictable stress". Molecular Psychiatry 26 (11): 6237–6252. November 2021. doi:10.1038/s41380-021-01159-1. PMID 34035476.
- ↑ "Engineering Safer Psychedelics for Treating Addiction". Neuroscience Insights 16. 20 July 2021. doi:10.1177/26331055211033847. PMID 34350400.
- ↑ 15.0 15.1 "Tabernanthalog Reduces Motivation for Heroin and Alcohol in a Polydrug Use Model". Psychedelic Medicine 1 (2): 111–119. June 2023. doi:10.1089/psymed.2023.0009. PMID 37360328.
- ↑ Jaster, Alaina M. (13 January 2021). "Researchers Synthesize Novel Compound, Tabernanthalog, a Non-Hallucinogenic Ibogaine Analog". https://psychedelicreview.com/researchers-synthesize-novel-compound-tabernanthalog-a-non-hallucinogenic-ibogaine-analog/.
- ↑ "Controlled Drugs and Substances Act". 5 December 2025. https://laws-lois.justice.gc.ca/eng/acts/c-38.8/FullText.html.
- ↑ Orange Book: List of Controlled Substances and Regulated Chemicals (January 2026), United States: U.S. Department of Justice: Drug Enforcement Administration (DEA): Diversion Control Division, January 2026, https://www.deadiversion.usdoj.gov/schedules/orangebook/orangebook.pdf
- ↑ 19.0 19.1 19.2 "Delving into the Latest Updates on DLX-7 with Synapse". 7 August 2025. https://synapse.patsnap.com/drug/27dc3166d63441e88619c8b30cb536e4.
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