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AM-4054

An adamantyl laboratory cannabinoid, a full CB1 agonist, far more potent than THC.

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.

C₂₆H₃₆O₃

CID 71661716

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

Updated on

In plain terms

AM-4054 is a laboratory molecule, developed in 2013 by an American university team to study the receptor on which cannabis acts. It does not come from hemp and is used in no product sold to the public. It switches this receptor on far more strongly than THC does, and no human data exist about it.

Receptors and activity

Target network

CB1AgonistKi = 4.9 nM · ratbinding at the rat CB1 receptor (rCB1)
  • Activates

The lower the cited value, the closer the target sits to AM-4054: 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-4054.

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

Cited values

  1. CB1AgonistKi = 4.9 nM · rat72 out of 100

    Thakur et al. 2013, J Med Chem, table 1 (new tab) · binding at the rat CB1 receptor (rCB1)

  2. CB2AgonistKi = 11.3 nM · human66 out of 100

    Thakur et al. 2013, J Med Chem, table 1 (new tab) · binding at the human CB2 receptor (hCB2)

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-4054 is a tricyclic classical cannabinoid: a hexahydrocannabinol whose usual pentyl chain is replaced by an adamantyl group, with a hydroxymethyl function at position 9. Thakur and colleagues measured in 2013 a nanomolar affinity for the CB1 receptor (Ki of 4.9 nM at rat CB1) and a similar affinity for CB2 (11.3 nM at human CB2), a modest selectivity of about 2.5-fold. The decisive difference from THC concerns efficacy: THC is only a partial agonist of CB1, whereas AM-4054 behaves as a full agonist, both in cAMP inhibition (EC50 of 1.29 nM) and in β-arrestin recruitment. In rats it produces the whole cannabinoid tetrad, antinociception, catalepsy, hypothermia and suppression of locomotor activity, effects reversed by the CB1 antagonist AM251, which confirms an action mediated by this receptor. In a discrimination test, it is more potent than THC. No activity is documented at TRPV1, GPR55, PPARγ or 5-HT1A. Human data are entirely lacking: no pharmacokinetics, metabolism or clinical observation has been published.

History

Source
None. AM-4054 is an entirely synthetic molecule, absent from hemp as from any other plant. It was designed as a pharmacological tool at the Center for Drug Discovery of Northeastern University, in Boston, in the group of Alexandros Makriyannis, from which the AM prefix of its designation comes. It was never intended for human use and is used in no consumer product.

Origin

Laboratory synthesis

No known biological pathway: this molecule is formed in no living organism. It is built on the classic tricyclic cannabinoid skeleton, obtained chemically, in which the pentyl chain at position 3 is replaced by an adamantyl group and the methyl at position 9 by a hydroxymethyl. It arises from optimisation work carried out around the compound AM411.

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)

No dedicated article.

References

Identifiers

Names

IUPAC name
(6aR,9R,10aR)-3-(1-adamantyl)-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydrobenzo[c]chromen-1-ol
Other names
AM4054 · AM 4054

Identifiers

Formula
C₂₆H₃₆O₃
InChIKey
GQYXNRWEEUCMOZ-MMSALSPUSA-N
SMILES
CC1([C@@H]2CC[C@H](C[C@H]2C3=C(C=C(C=C3O1)C45CC6CC(C4)CC(C6)C5)O)CO)C

Machine-readable entry (JSON)

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