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Research tools

AM6545

Peripherally acting synthetic CB1 antagonist, studied in rodents.

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.

C₂₆H₂₃Cl₂N₅O₃S

CAS 1245626-05-4

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

Updated on

In plain terms

AM6545 is a laboratory molecule, entirely synthetic, that does not exist in hemp. It blocks the CB1 receptor, the one THC activates, but it passes little into the brain and acts mostly in the rest of the body. It has been used in rodents to study food intake and metabolism; the data cited are animal data.

Receptors and activity

Target network

CB1AntagonistKi = 1.7 nM · ratrat brain membranes, [3H]CP 55,940 displacement; neutral antagonist: no effect on forskolin-stimulated cAMP (HEK293 cells expressing human CB1, up to 3 µM)
  • Blocks or inhibits
  • Binds or modulates

The lower the cited value, the closer the target sits to AM6545: 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 AM6545.

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 = 1.7 nM · rat79 out of 100

    Cluny et al., Br J Pharmacol 2010 (new tab) · rat brain membranes, [3H]CP 55,940 displacement; neutral antagonist: no effect on forskolin-stimulated cAMP (HEK293 cells expressing human CB1, up to 3 µM)

  2. CB2Binding (function not established)Ki = 523 nM · mouse38 out of 100

    Cluny et al., Br J Pharmacol 2010 (new tab) · HEK293 cells expressing mouse CB2, [3H]CP 55,940 displacement; 38-fold selectivity for CB1 over human CB2

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

AM6545 is a diaryl pyrazole carboxamide of the rimonabant series, designed to limit brain penetration (Cluny et al. 2010). Its Ki is 1.7 nM at CB1 (rat brain membranes) and 523 nM at mouse CB2, a selectivity of about 300-fold; it is a neutral antagonist, with no effect on cAMP in transfected cells, whereas AM251, an inverse agonist, raises it. Brain-to-plasma ratios after 10 mg/kg intraperitoneally were 0.18 to 0.41 in rats (1.30 to 4.73 for AM4113, a centrally active antagonist) and 0.10 to 0.20 in mice at 5 mg/kg. In rats and mice, it dose-dependently reduced food intake and induced a sustained fall in body weight; unlike AM251, it caused neither conditioned gaping nor conditioned taste avoidance in rats, and the effect on food intake persisted after subdiaphragmatic vagotomy (Cluny et al. 2010). In mice made obese with monosodium glutamate, three weeks of treatment reduced body weight and intraperitoneal fat mass and corrected lipid parameters, without consistently changing food intake (Ma et al. 2018). It also potentiated the corticotropic response to stress in mice, including CB1-deficient mice (Roberts and Hillard 2021). All these data are animal data.

Key sources.

History

Source
A synthetic molecule of the diarylpyrazole series (a pyrazole carboxamide related to rimonabant), absent from cannabis and from any known natural source. A laboratory tool.

Origin

Research tool

No biosynthetic pathway: a synthetic molecule of the diaryl pyrazole carboxamide class, 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)

AM-6545 (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. Cluny NL et al., A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents, Br J Pharmacol 2010 (new tab)PMID 20880401
  2. Ma H et al., Peripheral CB1 Receptor Neutral Antagonist, AM6545, Ameliorates Hypometabolic Obesity and Improves Adipokine Secretion in Monosodium Glutamate Induced Obese Mice, Front Pharmacol 2018 (new tab)PMID 29615900
  3. Roberts CJ, Hillard CJ, Peripherally restricted cannabinoid type 1 receptor (CB1R) antagonist, AM6545, potentiates stress-induced hypothalamic-pituitary-adrenal axis activation via a non-CB1R mechanism, 2021 (new tab)PMID 33216305
  4. ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
  5. PubChem, compound CID 46912919 (AM6545) (new tab)

Identifiers

Names

IUPAC name
5-[4-(4-cyanobut-1-ynyl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxo-1,4-thiazinan-4-yl)-4-methylpyrazole-3-carboxamide
Other names
AM-6545

Identifiers

Formula
C₂₆H₂₃Cl₂N₅O₃S
CAS
1245626-05-4
PubChem CID
46912919(new tab)
InChIKey
XBHQLFVDGLPBCK-UHFFFAOYSA-N
SMILES
CC1=C(N(N=C1C(=O)NN2CCS(=O)(=O)CC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)C#CCCC#N

Machine-readable entry (JSON)

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