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Research tools

AEF0117

A pregnenolone derivative studied as a selective brake on the CB1 receptor, with no known effect of its own.

Unscheduled
Level of detail

C₂₉H₄₀O₃

CID 139433957

Family
ECS pharmacological toolAllosteric modulator
Molar mass
436.60 g/mol

Updated on

In plain terms

AEF0117 is a laboratory molecule derived from a natural hormone, pregnenolone. It has nothing to do with CBD, is found in no plant and is sold nowhere. It was designed to dampen only part of the effects of THC at the CB1 receptor without blocking this receptor entirely, and tested in clinical trials in cannabis users; a phase 2b trial did not reach its primary endpoint.

Receptors and activity

Target network

CB1ModulatorIC50 = 3 nM · humaninhibition of the THC-induced (1 µM) fall in cellular respiration, HEK293 cells expressing human CB1; no effect on cAMP; p-ERK1/2: IC50 of about 300 nM; no effect on [3H]CP 55,940 binding
  • Binds or modulates

The lower the cited value, the closer the target sits to AEF0117: one ring per factor of 100. A target with no measured value stays on the edge.

Where these targets live

Where each target has been found in humans, according to the cited studies. The map shows the target, not an effect of AEF0117.

Brain, side view
Body, front view
Blood

CB1CB1 found in 7 regions of the body

  1. Basal gangliadenseMost dense in basal ganglia outflow nuclei1
  2. CerebellumdenseVery dense in the cerebellum1
  3. HippocampusdenseVery high concentrations in the hippocampus2
  4. AmygdaladenseHigh concentrations in the amygdala2
  5. CortexpresentPresent throughout the neocortex2
  6. Adipose tissuepresentExpressed in adipose tissue3
  7. GutpresentColonic epithelium, smooth muscle and plexus4

Map sources

  1. Herkenham M et al. Cannabinoid receptor localization in brain. Proc Natl Acad Sci U S A, 1990 (new tab)
  2. Glass M et al. Cannabinoid receptors in the human brain: a detailed anatomical and quantitative autoradiographic study in the fetal, neonatal and adult human brain. Neuroscience, 1997 (new tab)
  3. Engeli S et al. Activation of the peripheral endocannabinoid system in human obesity. Diabetes, 2005 (new tab)
  4. Wright K et al. Differential expression of cannabinoid receptors in the human colon: cannabinoids promote epithelial wound healing. Gastroenterology, 2005 (new tab)

Cited values

  1. CB1ModulatorIC50 = 3 nM · human75 out of 100

    Haney et al., Nat Med 2023 (new tab) · inhibition of the THC-induced (1 µM) fall in cellular respiration, HEK293 cells expressing human CB1; no effect on cAMP; p-ERK1/2: IC50 of about 300 nM; no effect on [3H]CP 55,940 binding

Bar length follows the measured value (Ki, Kd, EC50 or IC50), on one scale shared by every entry, from 100 µM to 0.1 nM. A target with no cited value has no bar.

Measured effects

Not characterised. No placebo-controlled human trial has measured the effects of AEF0117, so no level is shown.

Levels computed from placebo-controlled human trials: difference from placebo on 100, at the dose and route stated. Read the method

Pharmacology

AEF0117 is not a cannabinoid but a steroid derived from pregnenolone, designed as a signalling-specific inhibitor of the CB1 receptor (CB1-SSi). It inhibits part of the intracellular effects of THC binding (fall in cellular respiration, ERK1/2 phosphorylation), with an IC50 of 3 nM on cellular respiration in a cell model, without changing the cAMP pathway or the binding of the agonist [3H]CP 55,940; this selectivity goes with the absence of any behavioural effect of its own. In mice and squirrel monkeys, it decreased cannabinoid self-administration and THC-related behavioural disruption without notable adverse effects; in mice, none of the effects associated with CB1 antagonists (reduced food intake, anxiety-like or depression-like behaviours, precipitated withdrawal, glucocorticoid secretion) was observed (Haney et al. 2023). In the phase 1 trials (0.2 to 6 mg), the molecule was well tolerated; in a crossover phase 2a trial in cannabis users (0.06 mg and 1 mg), it reduced the positive subjective effects of cannabis by 19% (0.06 mg) and 38% (1 mg) compared with placebo, and cannabis self-administration at 1 mg, without precipitating withdrawal. A phase 2b trial in 333 treatment-seeking participants (0.1, 0.3 and 1 mg per day for 12 weeks) did not meet its primary or secondary endpoints, according to the sponsor's press release of 4 September 2024. No marketing authorisation was found.

Key sources.

History

Source
A laboratory molecule derived from pregnenolone, a steroid hormone present in humans: it was designed by modifying carbons C3 and C17 of the steroid nucleus in order to obtain non-metabolisable derivatives (Haney et al. 2023). It is known neither in hemp nor in any other plant.

Origin

Research tool

No known biosynthetic pathway, plant or human: AEF0117 is a synthetic compound, a 3-O-(4-methoxybenzyl) derivative of pregnenolone, which is not converted in animals or humans into steroids downstream of pregnenolone (Haney et al. 2023).

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Allosteric modulator

Verification

Classification, sources and binding values checked on 20 October 2026; text read against its sources and Wikipedia.

Wikipedia (English)

No dedicated article.

References

  1. Haney M et al. Signaling-specific inhibition of the CB1 receptor for cannabis use disorder: phase 1 and phase 2a randomized trials. Nat Med, 2023;29(6):1487-1499 (new tab)PMID 37291212
  2. Vallée M et al. Pregnenolone can protect the brain from cannabis intoxication. Science, 2014;343(6166):94-98 (new tab)PMID 24385629
  3. ClinicalTrials.gov NCT05322941, phase 2b of AEF0117 in treatment-seeking users, Aelis Farma, 333 participants, from 05/2022 to 07/2024, no results posted (new tab)
  4. ClinicalTrials.gov NCT05554926, mass balance study of [4-14C]AEF0117 in 8 healthy volunteers, phase 1, completed in 02/2023 (new tab)
  5. Aelis Farma, press release of 4 September 2024: results of the phase 2b trial of AEF0117 (primary endpoint not met; good tolerability) (new tab)
  6. PubChem, lixosicone (AEF0117), CID 139433957 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
1-[(3S,8S,9S,10R,13S,14S,17S)-3-[(4-methoxyphenyl)methoxy]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone
Other names
lixosicone · AEF-0117 · 3beta-[(4-methoxyphenyl)methoxy]pregn-5-en-20-one

Identifiers

Formula
C₂₉H₄₀O₃
PubChem CID
139433957(new tab)
InChIKey
AAZPIQPULVRHOW-SFKJMYEFSA-N
SMILES
CC(=O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC=C4[C@@]3(CC[C@@H](C4)OCC5=CC=C(C=C5)OC)C)C

Machine-readable entry (JSON)

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