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Research tools

AM4113

Neutral CB1 antagonist: blocks the receptor without inverse agonism. A preclinical research tool.

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.

C₁₇H₁₂Cl₃N₃O

CAS 614726-85-1

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

Updated on

In plain terms

AM4113 is a laboratory molecule with no link to hemp. Instead of imitating cannabis, it sits on the CB1 receptor and blocks it without triggering anything itself: researchers call it a neutral antagonist. It is used as an experimental tool in animal studies.

Receptors and activity

Target network

CB1AntagonistKi = 0.8 nM · humanHEK-293 cells transfected with human CB1, competitive binding with [3H]CP 55,940; neutral antagonist: no effect on forskolin-stimulated cAMP up to 630 nM
  • Blocks or inhibits
  • Binds or modulates

The lower the cited value, the closer the target sits to AM4113: 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 AM4113.

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 = 0.8 nM · human85 out of 100

    Chambers et al., Am J Physiol Regul Integr Comp Physiol 2007 (new tab) · HEK-293 cells transfected with human CB1, competitive binding with [3H]CP 55,940; neutral antagonist: no effect on forskolin-stimulated cAMP up to 630 nM

  2. CB2Binding (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

AM4113 is a selective neutral antagonist of the CB1 receptor, a pyrazole-3-carboxamide analogue of rimonabant (SR141716A). In transfected HEK-293 cells it binds CB1 with a Ki of 0.80 nM, about 100 times more selectively than CB2, and does not change forskolin-stimulated cAMP production up to 630 nM (Chambers et al. 2007), which sets it apart from inverse agonists in this assay. In rats, it reduced food intake, weight gain and operant responding for food, without inducing conditioned gaping (a sign of nausea) at the doses that suppressed feeding (Sink et al. 2008); at 10 mg/kg, an anorectic dose, it did not significantly potentiate the vomiting induced by morphine-6-glucuronide, unlike AM251 at 5 mg/kg (Chambers et al. 2007). It inhibited heroin self-administration, but not cocaine or methamphetamine, with no effect on the brain-stimulation reward threshold that SR141716A raised (He et al. 2019). In squirrel monkeys, it reduced nicotine and THC self-administration and their reinstatement after abstinence, without changing operant behaviour for cocaine or food (Schindler et al. 2016). In mice, its effects on intestinal motility differ from those of AM251 (Storr et al. 2010). Gueye et al. (2016) saw no anxiety-like effect in rats, whereas Soler-Cedeño et al. (2024) report, from another study, anxiety-like effects in an open-field test. All these data are preclinical.

Key sources.

History

Source
A synthetic molecule of the diarylpyrazole series (a pyrazole-3-carboxamide, an analogue of rimonabant), absent from cannabis and from any living organism. A preclinical research reagent.

Origin

Research tool

No biological pathway: a synthetic molecule, an analogue of the rimonabant series.

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. Chambers AP, Vemuri VK, Peng Y, Wood JT, Olszewska T, Pittman QJ, Makriyannis A, Sharkey KA. A neutral CB1 receptor antagonist reduces weight gain in rat. Am J Physiol Regul Integr Comp Physiol, 2007 (new tab)PMID 17959701
  2. Sink KS et al. The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats. Neuropsychopharmacology, 2008 (new tab)PMID 17581535
  3. He XH et al. Cannabinoid CB1 receptor neutral antagonist AM4113 inhibits heroin self-administration without depressive side effects in rats. Acta Pharmacol Sin, 2019 (new tab)PMID 29967454
  4. Schindler CW et al. Blockade of nicotine and cannabinoid reinforcement and relapse by a cannabinoid CB1-receptor neutral antagonist AM4113 and inverse agonist rimonabant in squirrel monkeys. Neuropsychopharmacology, 2016 (new tab)PMID 26888056
  5. Gueye AB et al. The CB1 neutral antagonist AM4113 retains the therapeutic efficacy of the inverse agonist rimonabant for nicotine dependence and weight loss with better psychiatric tolerability. Int J Neuropsychopharmacol, 2016 (new tab)PMID 27493155
  6. Storr MA et al. Differential effects of CB1 neutral antagonists and inverse agonists on gastrointestinal motility in mice. Neurogastroenterol Motil, 2010 (new tab)PMID 20180825
  7. Soler-Cedeño O et al. AM6527, a neutral CB1 receptor antagonist, suppresses opioid taking and seeking, as well as cocaine seeking in rodents without aversive effects. Neuropsychopharmacology, 2024 (notes the low oral bioavailability of AM4113) (new tab)PMID 38600154
  8. ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
  9. PubChem, compound record CID 66844170, NCBI. (new tab)

Identifiers

Names

IUPAC name
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide
Other names
AM-4113 · AM 4113

Identifiers

Formula
C₁₇H₁₂Cl₃N₃O
CAS
614726-85-1
PubChem CID
66844170(new tab)
InChIKey
BBUKVPCUOHFAQN-UHFFFAOYSA-N
SMILES
CC1=C(N(N=C1C(=O)N)C2=C(C=C(C=C2)Cl)Cl)C3=CC=C(C=C3)Cl

Machine-readable entry (JSON)

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