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A-796260

Selective CB2 receptor agonist designed in the laboratory, with no human data at all.

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.

C₂₂H₃₀N₂O₂

CAS 895155-26-7

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

Updated on

In plain terms

A-796260 is a laboratory molecule, developed by Abbott Laboratories to study pain. It exists in no plant. In rodents, it acts mainly on the CB2 receptor, the one of immune tissues, and at much higher concentrations on CB1; no study in humans was found.

Receptors and activity

Target network

CB2AgonistKi = 4.4 nM · humanradioligand binding, human CB2 (13.0 nM at rat CB2); cAMP inhibition: EC50 0.710 nM, efficacy 78% (CP 55,940 as reference)
  • Activates

The lower the cited value, the closer the target sits to A-796260: 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 A-796260.

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

Cited values

  1. CB2AgonistKi = 4.4 nM · human73 out of 100

    Yao et al., Br J Pharmacol 2008 (tables 1 and 2) (new tab) · radioligand binding, human CB2 (13.0 nM at rat CB2); cAMP inhibition: EC50 0.710 nM, efficacy 78% (CP 55,940 as reference)

  2. CB1AgonistEC50 = 983 nM · human33 out of 100

    Yao et al., Br J Pharmacol 2008 (tables 1 and 2) (new tab) · cAMP inhibition, human CB1, efficacy 118%; binding Ki 845 nM (395 nM at rat CB1, EC50 286 nM)

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

A-796260 is an indol-3-yl ketone of the aminoalkylindole family, bearing a 2,2,3,3-tetramethylcyclopropyl group on the carbonyl bridge and a 2-(morpholin-4-yl)ethyl chain on the indole nitrogen. Yao and colleagues measured an affinity of 4.37 nM at human CB2 against 845 nM at human CB1 (193-fold binding selectivity) and CB2 activation with an EC50 of 0.710 nM and 78% efficacy; at human CB1 the functional EC50 is 983 nM (118% efficacy). In rodent models of inflammatory, post-operative, neuropathic and osteoarthritic pain, the effect was blocked by CB2 antagonists but not by CB1 or μ-opioid antagonists, at doses (1 to 35 mg/kg intraperitoneally) with no significant effect on locomotor activity (Yao et al. 2008). The only toxicology study found, on human HepG2 liver cells, attributes to it a strong cytotoxic potential, comparable to that of the naphthoylindole JWH-200 and higher than that of 5F-EMB-PINACA (Gampfer et al. 2021). No clinical trial, human pharmacokinetic data or poisoning case was found in the sources consulted.

History

Source
A pharmaceutical laboratory compound. A-796260 comes from the medicinal chemistry programme of Abbott Laboratories on selective CB2 receptor agonists (Yao et al. 2008; Frost et al. 2010). It is not known in hemp or any other plant; no clinical trial registered on ClinicalTrials.gov was found.

Origin

Laboratory synthesis

No known biological pathway: the molecule is entirely synthetic and absent from any living organism. Chemically it belongs to the indol-3-yl ketones.

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)

A-796,260 (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

Identifiers

Names

IUPAC name
[1-(2-morpholin-4-ylethyl)indol-3-yl]-(2,2,3,3-tetramethylcyclopropyl)methanone
Other names
A-796,260

Identifiers

Formula
C₂₂H₃₀N₂O₂
CAS
895155-26-7
InChIKey
ZCFHOMLAFTWDFM-UHFFFAOYSA-N
SMILES
CC1(C(C1(C)C)C(=O)C2=CN(C3=CC=CC=C32)CCN4CCOCC4)C

Machine-readable entry (JSON)

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