APP-FUBINACA
Indazole synthetic cannabinoid: moderate affinity at CB1 and CB2, no published human data.
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.
C₂₄H₂₁FN₄O₂
CAS 1185282-03-4
- Family
- Synthetic CB receptor agonistNew psychoactive substance
- Molar mass
- 416.40 g/mol
Updated on
In plain terms
APP-FUBINACA is a synthetic cannabinoid, that is, a molecule made in a laboratory that exists neither in hemp nor in any other plant. Described in 2009 in a patent of a pharmaceutical company, it was later reported among the synthetic cannabinoids sold online. What it produces in humans has not been studied: human data are lacking, and by its structure it falls under a family classified as a narcotic in France.
Receptors and activity
Target network
- Activates
The lower the cited value, the closer the target sits to APP-FUBINACA: 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 APP-FUBINACA.
CB1CB1 found in 7 regions of the body
- Basal gangliadenseMost dense in basal ganglia outflow nuclei1
- CerebellumdenseVery dense in the cerebellum1
- HippocampusdenseVery high concentrations in the hippocampus2
- AmygdaladenseHigh concentrations in the amygdala2
- CortexpresentPresent throughout the neocortex2
- Adipose tissuepresentExpressed in adipose tissue3
- GutpresentColonic epithelium, smooth muscle and plexus4
Map sources
- Herkenham M et al. Cannabinoid receptor localization in brain. Proc Natl Acad Sci U S A, 1990 (new tab)
- 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)
- Engeli S et al. Activation of the peripheral endocannabinoid system in human obesity. Diabetes, 2005 (new tab)
- Wright K et al. Differential expression of cannabinoid receptors in the human colon: cannabinoids promote epithelial wound healing. Gastroenterology, 2005 (new tab)
Cited values
- CB1Partial agonistKi = 50 nM · human55 out of 100
Schoeder et al. 2018, Forensic Toxicol (new tab) · [3H]CP55,940 displacement, human CB1 expressed in CHO cells; value rounded from the text (« around 50 nM »); partial activation in cAMP at 10 µM
- CB2AgonistKi = 50 nM · human55 out of 100
Schoeder et al. 2018, Forensic Toxicol (new tab) · [3H]CP55,940 displacement, human CB2 expressed in CHO cells; value rounded from the text (« around 50 nM »); full agonist in cAMP at 10 µM
Pharmacology
APP-FUBINACA belongs to the indazole-3-carboxamides, a chemical scaffold widespread among recent synthetic cannabinoids; it carries the variant with a 4-fluorobenzyl group, called FUBINACA, combined with a phenylalaninamide fragment. The pharmacological characterisation that we found is that of Schoeder et al. (2018): a potency of about 50 nM at CB1 as at CB2, with no selectivity between the two subtypes, and a dissociated functional profile, with only partial activation of CB1 at 10 µM but full activation of CB2. Outside the cannabinoid receptors, it proved practically inactive at GPR55 and GPR18. The risk specific to APP-FUBINACA also lies in its context of circulation: the products containing it are not labelled, and a difference of a single atom separates this molecule from far more active analogues that may be found in the same product. Everything else is missing: no metabolism study, no pharmacokinetic measurement and no published clinical observation were found for this particular substance.
Key sources.
- Schoeder CT, Hess C, Madea B, Meiler J, Müller CE. Pharmacological evaluation of new constituents of Spice: synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds. Forensic Toxicol, 2018 (APP-FUBINACA, compound 29: about 50 nM at CB1 and CB2; partial activation of CB1, full activation of CB2 in cAMP) (new tab)PMID 29963207
- Buchler IP et al. Indazole derivatives. International application WO 2009/106982, Pfizer Inc., priority of 29 February 2008, published 3 September 2009 (example 4: L-phenylalaninamide of 1-(4-fluorobenzyl)indazole-3-carboxylate) (new tab)
- Giorgetti A et al. Development and validation of a rapid LC-MS/MS method for the detection of 182 novel psychoactive substances in whole blood. Drug Test Anal, 2022 (APP-FUBINACA: retention time 10.8 min, LOD-LOQ 0.02 to 0.05 ng/mL) (new tab)PMID 34599648
- Florou D, Boumba VA. Hair analysis for New Psychoactive Substances (NPS): still far from becoming the tool to study NPS spread in the community? Toxicol Rep, 2021 (APP-FUBINACA in hair, LOD 5 pg/mg, LOQ 25 pg/mg, table 3) (new tab)PMID 34646750
- Spinella I et al. A comprehensive HPLC-HRMS/MS targeted screening method to detect 90 new psychoactive substances in oral fluid samples. Biology (Basel), 2026 (APP-FUBINACA, identification limit of 5 ng/mL) (new tab)PMID 42041894
- López-Rabuñal Á et al. Simultaneous determination of 137 drugs of abuse, new psychoactive substances, and novel synthetic opioids in meconium by UHPLC-QTOF. Anal Bioanal Chem, 2021 (APP-FUBINACA in the panel, LOD 0.3 ng/g) (new tab)PMID 34286357
- Almeida AS et al. Exploring the impact of chirality of synthetic cannabinoids and cathinones: a systematic review on enantioresolution methods and enantioselectivity studies. Int J Mol Sci, 2025 (chiral resolution of APP-FUBINACA on (R,R)-Whelk-O 1) (new tab)PMID 40650252
- Presley BC, Logan BK, Jansen-Varnum SA. In Vitro Metabolic Profile Elucidation of Synthetic Cannabinoid APP-CHMINACA (PX-3). J Anal Toxicol. 2020;44:226-236 (related analogue) (new tab)PMID 31665324
- Mercier G, Mohamed KA, Zagzoog A, et al. In vitro pharmacological activity of twenty-eight synthetic cannabinoid receptor agonists at the type 1 and 2 cannabinoid receptors. Neurochem Int. 2025 (abstract: class toxicities) (new tab)PMID 40876783
- Zangani C et al. The e-Psychonauts' Spiced world: assessment of the synthetic cannabinoids' information available online. Curr Neuropharmacol, 2020 (APP-FUBINACA in the UNODC, EUDA and NPSFinder lists) (new tab)PMID 32116194
- ANSM, consolidated list of substances classified as narcotics, updated 16 February 2026 (annex IV, family of 3-carboxamide indazole derivatives; APP-FUBINACA not named) (new tab)
- Légifrance, order of 3 October 2017 amending the order of 22 February 1990 setting the list of substances classified as narcotics, annex IV (JORF of 10 October 2017) (new tab)
- PubChem, APP-FUBINACA, CID 58124515 (new tab)
History
- Source
- An entirely synthetic molecule. It exists in no plant, neither hemp nor any other, and has no known natural origin. It appeared on the market of new psychoactive substances, where it figures in the lists of the EUDA and of UNODC recording the synthetic cannabinoids reported (Zangani et al., 2020). Products containing this type of compound are sold under names that give no information on their real content.
Origin
Laboratory synthesis
There is no biosynthetic pathway: the molecule comes from no living organism and derives from no plant precursor. It belongs exclusively to synthetic chemistry. No operational detail is given here.
Legal framework
- European Union
The substance is not listed in the Annex to Council Framework Decision 2004/757/JHA (consolidated version of 12 January 2026), which lists the new psychoactive substances controlled at European Union level; control is a matter for national law. It appears in the lists of the EUDA and of UNODC recording the synthetic cannabinoids reported (Zangani et al., 2020), which is monitoring and not control. It does not appear in the schedules of the 1971 Convention on Psychotropic Substances (green list of the INCB, 35th and 36th editions). France ties it to a generic definition by chemical family in annex IV of its list (see the French status).
- France
APP-FUBINACA is named in no entry of the consolidated ANSM list (updated 16 February 2026), which does, however, cite the neighbouring molecule 5F-APP-PINACA (PX-2), with the same phenylalaninamide fragment. By its structure it falls under the generic family of the « 3-carboxamide indazole derivatives » of annex IV, which the text of the decree of 3 October 2017 (JORF of 10 October 2017) already contains: a substituent on nitrogen 1 of the indazole of the alkyl, haloalkyl, halobenzyl, cycloalkylmethyl or related type, an indazole ring substituted or not, and a carboxamide-bridge nitrogen bearing in particular a 1-amino-1-oxo group substituted at position 3. The 4-fluorobenzyl group (halobenzyl) and the phenylalaninamide fragment of APP-FUBINACA meet this description. This is a reading of the text applied to the structure, not a nominative listing. The clause covering tetrahydrocannabinols, their esters, ethers and salts (annex III since the decision of 6 February 2026) does not apply here, the molecule not being a THC derivative. Production, possession, transfer, importation and use fall under the regime for narcotics.
Sources: EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA. Our method.
Classification
Family, origin and source verification
- Family
Synthetic CB receptor agonist › New psychoactive substance
- Class
indazole-3-carboxamide
- 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
- Schoeder CT, Hess C, Madea B, Meiler J, Müller CE. Pharmacological evaluation of new constituents of Spice: synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds. Forensic Toxicol, 2018 (APP-FUBINACA, compound 29: about 50 nM at CB1 and CB2; partial activation of CB1, full activation of CB2 in cAMP) (new tab)PMID 29963207
- Buchler IP et al. Indazole derivatives. International application WO 2009/106982, Pfizer Inc., priority of 29 February 2008, published 3 September 2009 (example 4: L-phenylalaninamide of 1-(4-fluorobenzyl)indazole-3-carboxylate) (new tab)
- Giorgetti A et al. Development and validation of a rapid LC-MS/MS method for the detection of 182 novel psychoactive substances in whole blood. Drug Test Anal, 2022 (APP-FUBINACA: retention time 10.8 min, LOD-LOQ 0.02 to 0.05 ng/mL) (new tab)PMID 34599648
- Florou D, Boumba VA. Hair analysis for New Psychoactive Substances (NPS): still far from becoming the tool to study NPS spread in the community? Toxicol Rep, 2021 (APP-FUBINACA in hair, LOD 5 pg/mg, LOQ 25 pg/mg, table 3) (new tab)PMID 34646750
- Spinella I et al. A comprehensive HPLC-HRMS/MS targeted screening method to detect 90 new psychoactive substances in oral fluid samples. Biology (Basel), 2026 (APP-FUBINACA, identification limit of 5 ng/mL) (new tab)PMID 42041894
- López-Rabuñal Á et al. Simultaneous determination of 137 drugs of abuse, new psychoactive substances, and novel synthetic opioids in meconium by UHPLC-QTOF. Anal Bioanal Chem, 2021 (APP-FUBINACA in the panel, LOD 0.3 ng/g) (new tab)PMID 34286357
- Almeida AS et al. Exploring the impact of chirality of synthetic cannabinoids and cathinones: a systematic review on enantioresolution methods and enantioselectivity studies. Int J Mol Sci, 2025 (chiral resolution of APP-FUBINACA on (R,R)-Whelk-O 1) (new tab)PMID 40650252
- Presley BC, Logan BK, Jansen-Varnum SA. In Vitro Metabolic Profile Elucidation of Synthetic Cannabinoid APP-CHMINACA (PX-3). J Anal Toxicol. 2020;44:226-236 (related analogue) (new tab)PMID 31665324
- Mercier G, Mohamed KA, Zagzoog A, et al. In vitro pharmacological activity of twenty-eight synthetic cannabinoid receptor agonists at the type 1 and 2 cannabinoid receptors. Neurochem Int. 2025 (abstract: class toxicities) (new tab)PMID 40876783
- Zangani C et al. The e-Psychonauts' Spiced world: assessment of the synthetic cannabinoids' information available online. Curr Neuropharmacol, 2020 (APP-FUBINACA in the UNODC, EUDA and NPSFinder lists) (new tab)PMID 32116194
- ANSM, consolidated list of substances classified as narcotics, updated 16 February 2026 (annex IV, family of 3-carboxamide indazole derivatives; APP-FUBINACA not named) (new tab)
- Légifrance, order of 3 October 2017 amending the order of 22 February 1990 setting the list of substances classified as narcotics, annex IV (JORF of 10 October 2017) (new tab)
- PubChem, APP-FUBINACA, CID 58124515 (new tab)
Identifiers
Names
- IUPAC name
- N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-1-[(4-fluorophenyl)methyl]indazole-3-carboxamide
- Other names
- N-(1-amino-3-phenyl-1-oxopropan-2-yl)-1-((4-fluorophenyl)methyl)-1H-indazole-3-carboxamide · N-[(1S)-2-amino-1-benzyl-2-oxoethyl]-1-[(4-fluorophenyl)methyl]indazole-3-carboxamide · 1H-Indazole-3-carboxamide, N-[(1S)-2-amino-2-oxo-1-(phenylmethyl)ethyl]-1-[(4-fluorophenyl)methyl]-
Identifiers
- Formula
- C₂₄H₂₁FN₄O₂
- CAS
- 1185282-03-4
- PubChem CID
- 58124515(new tab)
- InChIKey
- TZXBEYFALIFOAG-FQEVSTJZSA-N
- SMILES
- C1=
CC= C(C= C1) C[C@@H] (C(= O) N) NC(= O) C2= NN(C3= CC= CC= C32) CC4= CC= C(C= C4) F
LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.