Skip to content

Batch information on every product pageTHC < 0.3%Shipped from France10% off when you sign up

Research tools

ABD459

A neutral antagonist at the CB1 receptor, a preclinical research tool with no human data.

Unscheduled
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.

C₂₄H₁₇BrCl₂N₂O₂

CID 25003055

Family
ECS pharmacological toolAntagonist or inverse agonist
Molar mass
516.20 g/mol

Updated on

In plain terms

ABD459 is a molecule created in the laboratory for research, with no connection to hemp. Instead of activating the CB1 receptor as THC does, it blocks it, and it is used to study the role of this receptor in animals. No study in humans was found.

Receptors and activity

Target network

CB1AntagonistKi = 8.6 nM · mouse[3H]CP 55,940 displacement, MF1 mouse brain membranes (95% CI: 4.23 to 17.5 nM); KB of 7.7 nM in [35S]GTPγS, with no effect on basal binding (neutral antagonist)
  • Blocks or inhibits

The lower the cited value, the closer the target sits to ABD459: 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 ABD459.

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. CB1AntagonistKi = 8.6 nM · mouse68 out of 100

    Goonawardena et al., Behav Pharmacol 2015 (new tab) · [3H]CP 55,940 displacement, MF1 mouse brain membranes (95% CI: 4.23 to 17.5 nM); KB of 7.7 nM in [35S]GTPγS, with no effect on basal binding (neutral antagonist)

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

ABD459 is a diarylpyrazole ketone derived from the rimonabant skeleton, characterised as a neutral antagonist of the CB1 receptor. In mouse brain membranes, it completely displaces [3H]CP 55,940 with a Ki of 8.61 nM (95% confidence interval 4.23 to 17.5 nM) and antagonises CP 55,940-induced [35S]GTPγS stimulation (KB 7.7 nM), with no effect on basal binding: this last point distinguishes it from rimonabant, which reduces basal binding (Goonawardena et al. 2015). In mice, 3 to 20 mg/kg reduced food intake in non-fasted animals, with no effect on motor activity or water intake; active food seeking was reduced for 5 to 6 hours, with no rebound after washout. At 3 mg/kg, ABD459 reduced REM sleep without changing wakefulness or non-REM sleep, an effect shared with AM251 and WIN 55,212-2. Beyond this work, no data on CB2 affinity, pharmacokinetics, metabolism or toxicity were found, nor any study in humans.

Key sources.

History

Source
An entirely synthetic molecule with no known natural occurrence: designed as a neutral CB1 antagonist, derived from the rimonabant skeleton (Goonawardena et al. 2015).

Origin

Research tool

No biological pathway: ABD459 forms in no living organism. It is a synthetic compound of the 1,5-diarylpyrazole ketone class, related to rimonabant.

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Antagonist or inverse agonist

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. Goonawardena AV et al. Modulation of food consumption and sleep-wake cycle in mice by the neutral CB1 antagonist ABD459. Behav Pharmacol, 2015 (new tab)PMID 25356730
  2. Micale V et al. The cannabinoid CB1 antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice. Front Pharmacol, 2019 (new tab)PMID 30949045
  3. PubChem, ABD459, CID 25003055 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
[5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazol-3-yl]-(4-methoxyphenyl)methanone
Other names
ABD-459 · ABD 459

Identifiers

Formula
C₂₄H₁₇BrCl₂N₂O₂
PubChem CID
25003055(new tab)
InChIKey
ZUDJJNLJDWKCNV-UHFFFAOYSA-N
SMILES
CC1=C(N(N=C1C(=O)C2=CC=C(C=C2)OC)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Br

Machine-readable entry (JSON)

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