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AZD-2207

A synthetic CB1 antagonist from AstraZeneca; one phase I absorption study, no other human data found.

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.

C₂₅H₂₅Cl₂F₃N₄O₄S

CID 11548933

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

Updated on

In plain terms

AZD-2207 is a laboratory molecule, unrelated to hemp: a pharmaceutical company designed it to block the CB1 receptor, the very one THC activates. It was evaluated in humans only in a phase I study of its absorption; it is not a consumer product and no efficacy or safety data were found.

Receptors and activity

Target network

CB1AntagonistKi = 0.1 nM · human[3H]CP 55,940 displacement, membranes of CHO-K1 cells expressing human CB1; IC50 of 1.0 to 1.1 nM in [35S]GTPγS (HEK293 cells); IC50 ratio CB2/CB1 of 110; kinetic retention index 1.02
  • Blocks or inhibits

The lower the cited value, the closer the target sits to AZD-2207: 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 AZD-2207.

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 = 0.1 nM · human99 out of 100

    Xia et al., J Med Chem 2017 (compound 11d; values from the text and from ChEMBL, document CHEMBL4020816) (new tab) · [3H]CP 55,940 displacement, membranes of CHO-K1 cells expressing human CB1; IC50 of 1.0 to 1.1 nM in [35S]GTPγS (HEK293 cells); IC50 ratio CB2/CB1 of 110; kinetic retention index 1.02

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

AZD-2207 belongs to the 1,2-diarylimidazole-4-carboxamides, analogues of rimonabant in which the pyrazole ring is replaced by an imidazole, the phenyl at position 1 carrying here an ester of 3,3,3-trifluoropropane-1-sulfonic acid. At recombinant human CB1, it displaces [3H]CP 55,940 with a Ki of 0.11 nM and inhibits the effect of this agonist with an IC50 of 1.0 to 1.1 nM in a [35S]GTPγS assay, with a 110-fold selectivity for CB1 over CB2 (Xia et al. 2017, values from ChEMBL): it occupies the receptor and prevents agonists from activating it. The 2016 work of Tannergren et al. describes it as highly lipophilic, at risk of not reaching therapeutic plasma concentrations through solubility-limited absorption; the chloride salt with a precipitation inhibitor gave favourable results in vitro and in dogs that could not be repeated in humans. No efficacy or tolerability data in humans were found, nor on brain penetration.

Key sources.

History

Source
No natural origin: AZD-2207 is found neither in hemp nor in any plant nor in the body. It is an entirely synthetic AstraZeneca drug candidate, described as an antagonist of the human CB1 receptor (Xia et al. 2017); no marketing authorisation was found.

Origin

Research tool

No biosynthetic pathway: the molecule is entirely synthetic and has no plant equivalent. It belongs to the 1,2-diarylimidazole-4-carboxamide class, here carrying a fluorinated sulfonic ester on the phenyl ring.

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. Xia L et al. Structure-affinity relationships and structure-kinetic relationships of 1,2-diarylimidazol-4-carboxamide derivatives as human cannabinoid 1 receptor antagonists. J Med Chem, 2017 (new tab)PMID 29111736
  2. Tannergren C et al. Biopharmaceutic profiling of salts to improve absorption of poorly soluble basic drugs. J Pharm Sci, 2016 (new tab)PMID 27637320
  3. Kourentas A et al. The BioGIT system: a valuable in vitro tool to assess the impact of dose and formulation on early exposure to low solubility drugs after oral administration. AAPS J, 2018 (new tab)PMID 29797293
  4. 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
  5. ChEMBL, activities of compound CHEMBL4087520 (AZD-2207), document CHEMBL4020816 (Xia et al. 2017) (new tab)
  6. PubChem, AZD-2207, CID 11548933 (identifiers and properties) (new tab)

Identifiers

Names

IUPAC name
[4-[2-(2,4-dichlorophenyl)-5-methyl-4-(piperidin-1-ylcarbamoyl)imidazol-1-yl]phenyl] 3,3,3-trifluoropropane-1-sulfonate
Other names
AZD 2207 · AZD2207

Identifiers

Formula
C₂₅H₂₅Cl₂F₃N₄O₄S
PubChem CID
11548933(new tab)
InChIKey
NHIXRYPUVCFFAF-UHFFFAOYSA-N
SMILES
CC1=C(N=C(N1C2=CC=C(C=C2)OS(=O)(=O)CCC(F)(F)F)C3=C(C=C(C=C3)Cl)Cl)C(=O)NN4CCCCC4

Machine-readable entry (JSON)

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