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Synthetic

AM-1241

A CB2-selective agonist used in pain research, whose behaviour depends on the species and the enantiomer.

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.

C₂₂H₂₂IN₃O₃

CAS 444912-48-5

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

Updated on

In plain terms

AM-1241 is a laboratory tool, not a consumer product. It activates the CB2 receptor and has been used in rodents to study the role of this receptor in pain models, without going through CB1. Its behaviour changes with the species studied, which calls for caution when reading results obtained in animals.

Receptors and activity

Target network

CB2Inverse agonistKi = 26.7 nM · ratracemic (R,S), membranes of CHO-K1 cells expressing rat CB2; inverse agonist on cAMP inhibition
  • Blocks or inhibits
  • Binds or modulates

The lower the cited value, the closer the target sits to AM-1241: 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-1241.

Brain, side view
Body, front view
Blood

CB2CB2 found in 5 regions of the body

  1. SpleendenseHighly abundant in the spleen1
  2. Immune cellspresentMainly B cells and natural killer cells1
  3. SkinpresentKeratinocytes, mast cells and nerve fibres2
  4. GutpresentImmune cells of the colonic mucosa3
  5. BonepresentPresent on osteoclasts4

Map sources

  1. Galiègue S et al. Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations. Eur J Biochem, 1995 (new tab)
  2. Ständer S et al. Distribution of cannabinoid receptor 1 (CB1) and 2 (CB2) on sensory nerve fibers and adnexal structures in human skin. J Dermatol Sci, 2005 (new tab)
  3. Wright K et al. Differential expression of cannabinoid receptors in the human colon: cannabinoids promote epithelial wound healing. Gastroenterology, 2005 (new tab)
  4. Rossi F et al. The endovanilloid/endocannabinoid system in human osteoclasts: possible involvement in bone formation and resorption. Bone, 2009 (new tab)

Cited values

  1. CB2AgonistKi = 28.7 nM · human59 out of 100

    Bingham et al., Br J Pharmacol 2007 (new tab) · racemic (R,S), membranes of CHO-K1 cells expressing human CB2, [3H]CP 55,940 displacement; agonist on cAMP inhibition

  2. CB2Inverse agonistKi = 26.7 nM · rat60 out of 100

    Bingham et al., Br J Pharmacol 2007 (new tab) · racemic (R,S), membranes of CHO-K1 cells expressing rat CB2; inverse agonist on cAMP inhibition

  3. CB1Binding (function not established)no measured value cited
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-1241 is a synthetic aminoalkylindole, a selective CB2 agonist, used as a tool in rodent nociception models. In 2001, Malan et al. showed that a local injection of AM1241 produced antinociception to a thermal stimulus, blocked by AM630 (a CB2 antagonist) but not by AM251 (a CB1 antagonist), without the central cannabinoid-type effects (hypothermia, catalepsy) seen with WIN 55,212-2. In 2005, Ibrahim et al. linked this effect to a peripheral release of β-endorphin by keratinocytes. In 2007, Bingham et al. showed that the racemate is an agonist at human CB2 but an inverse agonist at rat and mouse CB2 (Ki of 23.8 to 28.7 nM), whereas the S enantiomer is an agonist in all three species and proved the most effective in two rodent pain models; these results call for caution when reading conclusions drawn from the racemate.

Key sources.

History

Source
A synthetic molecule of the aminoalkylindole class, absent from cannabis and from any living organism. A research reagent, studied first as a racemic (R,S) mixture, then as its two enantiomers (Bingham et al. 2007).

Origin

Laboratory synthesis

No biosynthetic pathway: a synthetic molecule of the aminoalkylindole class.

Classification

Family, origin and source verification

Family

Synthetic CB receptor agonist › Research ligand or medicine

Class

aminoalkylindole

Verification

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

Wikipedia (English)

AM-1241 (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. Malan TP Jr, Ibrahim MM, Deng H et al., CB2 cannabinoid receptor-mediated peripheral antinociception, Pain 2001 (new tab)PMID 11514083
  2. Ibrahim MM, Deng H, Zvonok A et al., Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain, PNAS 2003 (new tab)PMID 12917492
  3. Ibrahim MM, Porreca F, Lai J et al., CB2 cannabinoid receptor activation produces antinociception by stimulating peripheral release of endogenous opioids, PNAS 2005 (new tab)PMID 15705714
  4. Bingham B, Jones PG, Uveges AJ et al., Species-specific in vitro pharmacological effects of the cannabinoid receptor 2 selective ligand AM1241 and its resolved enantiomers, British Journal of Pharmacology 2007 (new tab)PMID 17549048
  5. ANSM, consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV, heading « Indol-3-yl methanone » and entry AM-2233 (new tab)
  6. PubChem, Compound Summary CID 10141893, (R,S)-AM1241 (new tab)

Identifiers

Names

IUPAC name
(2-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone
Other names
AM 1241 · (R,S)-AM1241

Identifiers

Formula
C₂₂H₂₂IN₃O₃
CAS
444912-48-5
PubChem CID
10141893(new tab)
InChIKey
ZUHIXXCLLBMBDW-UHFFFAOYSA-N
SMILES
CN1CCCCC1CN2C=C(C3=CC=CC=C32)C(=O)C4=C(C=CC(=C4)[N+](=O)[O-])I

Machine-readable entry (JSON)

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