PF-3845
Selective covalent FAAH inhibitor, a research probe.
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
- 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.
FAAHFAAH found in 7 regions of the body
- CortexpresentCortical pyramidal neurons1
- Basal gangliapresentStriatal neurons1
- HypothalamuspresentPresent in hypothalamic nuclei1
- CerebellumpresentPurkinje cells and cerebellar layers1
- BrainstempresentInferior olivary nuclei1
- Adipose tissuepresentExpressed in mature adipocytes2
- BonepresentPresent on osteoclasts3
Map sources
- Romero J et al. Fatty acid amide hydrolase localization in the human central nervous system: an immunohistochemical study. Brain Res Mol Brain Res, 2002 (new tab)
- Engeli S et al. Activation of the peripheral endocannabinoid system in human obesity. Diabetes, 2005 (new tab)
- Rossi F et al. The endovanilloid/endocannabinoid system in human osteoclasts: possible involvement in bone formation and resorption. Bone, 2009 (new tab)
Cited values
- 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
- FAAH-2Inhibitorno measured value cited
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.
Key sources.
- Ahn K, Johnson DS, Mileni M et al., Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain, Chem Biol 2009 (new tab)PMID 19389627
- Booker L et al., The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice, Br J Pharmacol 2012 (new tab)PMID 21506952
- Huggins JP, Smart TS, Langman S, Taylor L, Young T, An efficient randomised, placebo-controlled clinical trial with the irreversible fatty acid amide hydrolase-1 inhibitor PF-04457845, which modulates endocannabinoids but fails to induce effective analgesia in patients with pain due to osteoarthritis of the knee, Pain 2012 (new tab)PMID 22727500
- ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
- PubChem, compound record CID 25154867 (PF-3845) (new tab)
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.
Legal framework
- European Union
A laboratory reagent; no European Union classification specific to the molecule was found in the sources consulted. Its status depends on the national law of each Member State.
- France
Not classified: absent from the ANSM list of narcotics (consolidated version updated 16/02/2026). A piperidine urea without an indole, indazole or benzo[c]chromene nucleus, it falls under none of the generic entries of Annex IV. The absence of classification is not a marketing authorisation.
Sources: EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA. Our method.
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)
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
- Ahn K, Johnson DS, Mileni M et al., Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain, Chem Biol 2009 (new tab)PMID 19389627
- Booker L et al., The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice, Br J Pharmacol 2012 (new tab)PMID 21506952
- Huggins JP, Smart TS, Langman S, Taylor L, Young T, An efficient randomised, placebo-controlled clinical trial with the irreversible fatty acid amide hydrolase-1 inhibitor PF-04457845, which modulates endocannabinoids but fails to induce effective analgesia in patients with pain due to osteoarthritis of the knee, Pain 2012 (new tab)PMID 22727500
- ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
- PubChem, compound record CID 25154867 (PF-3845) (new tab)
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
- PubChem CID
- 25154867(new tab)
- 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
LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.