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PF-3845

Selective covalent FAAH inhibitor, a research probe.

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.

C₂₄H₂₃F₃N₄O₂

CAS 1196109-52-0

Family
ECS pharmacological toolEnzyme inhibitor
Molar mass
456.50 g/mol

Updated on

In plain terms

PF-3845 is a laboratory molecule, obtained by chemical synthesis: it does not come from hemp. It blocks an enzyme of the body, FAAH, which normally destroys anandamide, a natural messenger related to cannabinoids. Researchers use it as a tool to study this system; it is not a consumer product. The data cited are preclinical.

Receptors and activity

Target network

FAAHInhibitorKi = 230 nMcovalent inhibition (kinact 0.0033 ± 0.0002 s-1, Ki 0.23 ± 0.03 µM); enzyme preparation not specified in the text consulted
  • Blocks or inhibits

The lower the cited value, the closer the target sits to PF-3845: 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 PF-3845.

Brain, side view
Body, front view
Blood

FAAHFAAH found in 7 regions of the body

  1. CortexpresentCortical pyramidal neurons1
  2. Basal gangliapresentStriatal neurons1
  3. HypothalamuspresentPresent in hypothalamic nuclei1
  4. CerebellumpresentPurkinje cells and cerebellar layers1
  5. BrainstempresentInferior olivary nuclei1
  6. Adipose tissuepresentExpressed in mature adipocytes2
  7. BonepresentPresent on osteoclasts3

Cited values

  1. FAAHInhibitorKi = 230 nM44 out of 100

    Ahn et al., Chem Biol 2009 (new tab) · covalent inhibition (kinact 0.0033 ± 0.0002 s-1, Ki 0.23 ± 0.03 µM); enzyme preparation not specified in the text consulted

  2. FAAH-2Inhibitorno 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

PF-3845 is a covalent, irreversible inhibitor of FAAH, the enzyme that hydrolyses anandamide and other fatty acid amides. It carbamylates the nucleophilic serine of the active site (Ahn et al. 2009), with a kinact of 0.0033 s-1 and a Ki of 0.23 µM. In mice, activity-based profiling showed selective inhibition of FAAH in vivo at 10 mg/kg intraperitoneally, without touching the liver carboxylesterases labelled by URB597; brain anandamide stayed elevated for up to 24 h, with cannabinoid receptor-dependent reductions in inflammatory pain (Ahn et al. 2009). In a model of lipopolysaccharide-induced allodynia, the anti-allodynic effect was absent in mice expressing FAAH only in the nervous system and required activation of CB1 and CB2 (Booker et al. 2012). PF-3845 itself has not been tested in humans in the sources consulted; another Pfizer FAAH inhibitor, PF-04457845 (4 mg/day for 2 weeks), reduced FAAH activity by more than 96% in patients with knee osteoarthritis without differing from placebo on the WOMAC pain score (difference of 0.04 against -1.13 for naproxen), and the trial was stopped for futility (Huggins et al. 2012), which shows that the rodent results were not confirmed in that trial.

History

Source
A synthetic molecule of the piperidine urea class, from Pfizer research, absent from cannabis and from any living organism. A research reagent.

Origin

Research tool

No known biological pathway: a synthetic molecule of the piperidine urea class, formed in the laboratory and not by a living being.

Classification

Family, origin and source verification

Family

ECS pharmacological tool › Enzyme inhibitor

Verification

Classification, sources and binding values checked on 20 October 2026; text read against its sources and Wikipedia.

Wikipedia (English)

PF-3845 (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

Identifiers

Names

IUPAC name
N-pyridin-3-yl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methyl]piperidine-1-carboxamide
Other names
PF 3845

Identifiers

Formula
C₂₄H₂₃F₃N₄O₂
CAS
1196109-52-0
InChIKey
NBOJHRYUGLRASX-UHFFFAOYSA-N
SMILES
C1CN(CCC1CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=CN=CC=C4

Machine-readable entry (JSON)

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