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CE-178253

Synthetic antagonist of the CB1 receptor, studied in rodents, with no human data published in the sources consulted.

Unscheduled
Level of detail

C₂₄H₂₃Cl₂N₇O

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.

Data sheet

Names

IUPAC name
1-[7-(2-chlorophenyl)-8-(4-chlorophenyl)-2-methylpyrazolo[1,5-a][1,3,5]triazin-4-yl]-3-(ethylamino)azetidine-3-carboxamide
Other names
FW6JCF60XU · NCGC00485051-01 · orb1740701 · T68779 · Q27278237

Identifiers

Formula
C₂₄H₂₃Cl₂N₇O
Molar mass
496.40 g/mol
PubChem CID
11191162(new tab)
InChIKey
XJFUIILGVMOOHV-UHFFFAOYSA-N

Class

Family
ECS modulator (research)

Legal status

Status
Unscheduled
See the legal framework

Updated on

Receptors and activity

  1. CB1Antagonist95 out of 100

    Ki 0,33 nM en liaison sur CB1 humain ; Ki 0,07 nM en test fonctionnel GTPγ[35S] (Hadcock et coll., 2010)

  2. CB2Antagonist5 out of 100

    Ki supérieur à 10 000 nM (Hadcock et coll., 2010)

Bar length shows the relative strength of the interaction, as an indication.

Subjective signature

Calm
3 out of 100
Relaxation of body and mind; reduced mental noise without marked drowsiness.
Clarity
3 out of 100
Sustained attention and clear thinking; functional lucidity, not euphoria.
High
2 out of 100
Euphoria and sensory intensity; altered perception of time and space.
Appetite
2 out of 100
Stimulation of hunger and of taste appreciation (the “munchies” effect).
Sleep
3 out of 100
Sedative effect: aids sleep onset and the continuity of deep sleep.
Editorial estimate, not clinical.

Pharmacology

CE-178253 is a synthetic antagonist of the cannabinoid receptor CB1, described as highly selective over CB2. The 2010 reference publication reports an inhibition constant of 0.33 nM at human CB1 in binding and 0.07 nM in a functional test, against more than 10 000 nM at CB2. In rats, the molecule is active by mouth: it reduces food intake, increases average oxygen consumption by 28% and 39% at 1 and 3 mg/kg, and reverses the four effects of CP-55940 in the tetrad test in a dose-dependent manner. In obese mice, 3 mg/kg per day for ten days led to an average weight loss of 18%. The same authors state that they had previously reported its efficacy in a model of parkinsonism, and suggest that selective CB1 antagonism may enhance the antiparkinsonian action of levodopa and other dopaminomimetics. No human clinical data are published in the sources consulted.

Key sources.

History

Source
Entirely synthetic molecule, studied by Pfizer teams as a CB1 receptor antagonist with obesity and metabolic disorders in view (Hadcock et al., 2010).

Origin (research tool)

No biosynthetic pathway: a chemically synthesised compound of the pyrazolo[1,5-a][1,3,5]triazine class.

References

  1. Hadcock et coll., profil pharmacologique quantitatif de CE-178253, antagoniste CB1, BMC Pharmacology, 2010 (new tab)PMID 20712891
  2. ANSM, liste consolidée des substances classées comme stupéfiants, mise à jour du 16 février 2026 (new tab)
  3. INCB, Green List 2026 (Convention de 1971) (new tab)
  4. PubChem, notice du composé CE-178253 (CID 11191162) (new tab)

Structured data

SMILES
CCNC1(CN(C1)C2=NC(=NC3=C(C(=NN32)C4=CC=CC=C4Cl)C5=CC=C(C=C5)Cl)C)C(=O)N
InChIKey
XJFUIILGVMOOHV-UHFFFAOYSA-N

Machine-readable entry (JSON)

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