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Synthetic

AM-11245

A laboratory probe of the hexahydrocannabinol type, a sub-nanomolar agonist of the CB1 and CB2 receptors.

FranceNarcotic: generic clauseInternationalUnscheduled
Level of detail

Harm-reduction warning

No characterised human dose: animal / in vitro data only. Effect profile, safety margin and acute toxicity are not documented in human clinical practice. Extremely potent compound: severe effects, seizures and deaths reported in the literature.

C₂₆H₃₉NO₃

CID 166636133

Family
Synthetic CB receptor agonistResearch ligand or medicine
Molar mass
413.60 g/mol

Updated on

In plain terms

AM-11245 is a molecule made in a university laboratory to study the receptors on which cannabis acts. It does not exist in the plant and is part of no cannabidiol product: it is a research reagent. It binds the same receptors as THC, but at much lower concentrations; what is known comes from cell and mouse experiments, and no study in humans was found.

Receptors and activity

Target network

CB1AgonistEC50 = 0.1 nM · humaninhibition of forskolin-stimulated cAMP, CHO-K1 cells expressing human CB1, maximal effect of 103% of that of CP 55,940; Ki of 0.4 nM on rat brain membranes ([3H]CP 55,940)
  • Activates

The lower the cited value, the closer the target sits to AM-11245: 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 AM-11245.

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. CB1AgonistEC50 = 0.1 nM · human100 out of 100

    Jiang et al., J Med Chem 2021 (values from ChEMBL, document CHEMBL5038575) (new tab) · inhibition of forskolin-stimulated cAMP, CHO-K1 cells expressing human CB1, maximal effect of 103% of that of CP 55,940; Ki of 0.4 nM on rat brain membranes ([3H]CP 55,940)

  2. CB2AgonistEC50 = 0.4 nM · human90 out of 100

    Jiang et al., J Med Chem 2021 (values from ChEMBL, document CHEMBL5038575) (new tab) · inhibition of forskolin-stimulated cAMP, CHO-K1 cells expressing human CB2, maximal effect of 70%; Ki of 0.4 nM (human CB2) and 0.8 nM (mouse CB2), HEK293 cells

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.

Pharmacology

AM-11245 is a pharmacological probe of the AM series, built on a hexahydrocannabinol skeleton whose side chain ends in a nitrile and whose position 9 carries a hydroxymethyl. Its established characteristic is potency: Ki of 0.4 nM at rat brain CB1 and at human CB2, EC50 of 0.088 nM at human CB1 in a cAMP assay with a maximal effect of 103% of that of CP 55,940, and 0.38 nM at human CB2 with a maximal effect of 70% (Jiang et al. 2021). The authors called it a « megagonist » because of its tight binding to the receptors. In mice, the same paper reports, after intraperitoneal injection, antinociception in a tail-withdrawal test (50% effective dose 0.12 mg/kg), a fall in body temperature still measured 24 hours after 0.1 mg/kg, reduced locomotor activity between 0.1 and 1 mg/kg and slowed colonic transit. No pharmacokinetic, metabolism or regulatory toxicology study, nor any trial in humans, was found.

Key sources.

History

Source
An entirely synthetic molecule, absent from cannabis and from any living organism: a pharmacological probe designed in a university medicinal chemistry laboratory (Jiang et al. 2021). It has no connection with hemp or cannabidiol products.

Origin

Laboratory synthesis

No biosynthetic pathway: the molecule is produced by no living organism. It is a synthetic compound of the hexahydrocannabinol type, whose side chain ends in a nitrile.

Classification

Family, origin and source verification

Family

Synthetic CB receptor agonist › Research ligand or medicine

Class

classical

Verification

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

Wikipedia (English)

AM-11245 (new tab)

Article paired by the molecule's structure (InChIKey), revision read on 19 October 2026. Read as a second opinion, never cited as a source.

References

  1. Jiang S et al. Novel functionalized cannabinoid receptor probes: development of exceptionally potent agonists. J Med Chem, 2021 (new tab)PMID 33761251
  2. ChEMBL, activities of compound CHEMBL5091754 (AM-11245), document CHEMBL5038575 (Jiang et al. 2021): Ki, EC50, Emax and mouse assays (new tab)
  3. PubChem, AM-11245, CID 166636133 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
8-[(6aR,9R,10aR)-1-hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydrobenzo[c]chromen-3-yl]-8-methylnonanenitrile
Other names
AM11245 · AM 11245

Identifiers

Formula
C₂₆H₃₉NO₃
PubChem CID
166636133(new tab)
InChIKey
IGSAQGJQMKOTAG-HMXCVIKNSA-N
SMILES
CC1(C)OC2=C([C@H]3[C@H]1CC[C@@H](CO)C3)C(O)=CC(C(C)(C)CCCCCCC#N)=C2

Machine-readable entry (JSON)

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