Inhibition of Fatty Acid Binding Proteins Elevates Brain Anandamide Levels and Produces Analgesia

Kaczocha, Martin; Rebecchi, Mario J.; Ralph, Brian P.; Teng, Yu-Han Gary; Berger, William T.; Galbavy, William; Elmes, Matthew W.; Glaser, Sherrye T.; Wang, Liqun; Rizzo, Robert C.; Deutsch, Dale G.; Ojima, Iwao

doi:10.1371/journal.pone.0094200

Cited by 146Cannabis and Cannabinoid ResearchPain Mechanisms and TreatmentsFatty Acid Research and Health

Inhibition of Fatty Acid Binding Proteins Elevates Brain Anandamide Levels and Produces Analgesia

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Kaczocha, Martin, Rebecchi, Mario J., Ralph, Brian P., Teng, Yu-Han Gary, Berger, William T., Galbavy, William, Elmes, Matthew W., Glaser, Sherrye T. +4 more·2014·PLoS ONE

DOI 10.1371/journal.pone.0094200PMC PMC3976407

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Abstract

The endocannabinoid anandamide (AEA) is an antinociceptive lipid that is inactivated through cellular uptake and subsequent catabolism by fatty acid amide hydrolase (FAAH). Fatty acid binding proteins (FABPs) are intracellular carriers that deliver AEA and related N-acylethanolamines (NAEs) to FAAH for hydrolysis. The mammalian brain expresses three FABP subtypes: FABP3, FABP5, and FABP7. Recent work from our group has revealed that pharmacological inhibition of FABPs reduces inflammatory pain in mice. The goal of the current work was to explore the effects of FABP inhibition upon nociception in diverse models of pain. We developed inhibitors with differential affinities for FABPs to elucidate the subtype(s) that contributes to the antinociceptive effects of FABP inhibitors. Inhibition of FABPs reduced nociception associated with inflammatory, visceral, and neuropathic pain. The antinociceptive effects of FABP inhibitors mirrored their affinities for FABP5, while binding to FABP3 and FABP7 was not a predictor of in vivo efficacy. The antinociceptive effects of FABP inhibitors were mediated by cannabinoid receptor 1 (CB1) and peroxisome proliferator-activated receptor alpha (PPARα) and FABP inhibition elevated brain levels of AEA, providing the first direct evidence that FABPs regulate brain endocannabinoid tone. These results highlight FABPs as novel targets for the development of analgesic and anti-inflammatory therapeutics.

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FABP inhibitors SBFI26 and SBFI50 attenuate carrageenan-induced acute paw edema and thermal hyperalgesia.
“The FABP inhibitors SBFI26 and SBFI50 attenuate carrageenan-induced acute paw edema and thermal hyperalgesia (Kaczocha et al, 2014).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Kaczocha et al, 2014

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Cannabinoids and Pain: New Insights From Old Molecules
Vuckovic, S. M., Srebro, D., Vujović, K. S., Vučetić, Č., & Prostran, M. S. (2018) · Frontiers in Pharmacology · doi:10.3389/fphar.2018.01259 · Cited by 417 · see citing works
Fatty Acid-binding Proteins (FABPs) Are Intracellular Carriers for Δ9-Tetrahydrocannabinol (THC) and Cannabidiol (CBD)
Elmes, M. W., Kaczocha, M., Berger, W. T., Leung, K., Ralph, B. P., Wang, L., Sweeney, J., Miyauchi, J. T., Tsirka, S. E., Ojima, I., et al. (2015) · Journal of Biological Chemistry · doi:10.1074/jbc.m114.618447 · Cited by 315 · see citing works
“Inhibitors of the FABPs have recently been shown to raise brain levels of AEA by limiting its transport into the cell to FAAH (11, 12, 16).”
Self-citation
The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain
Donvito, G., Nass, S. R., Wilkerson, J. L., Curry, Z. A., Schurman, L. D., Kinsey, S. G., & Lichtman, A. H. (2018) · Neuropsychopharmacology · doi:10.1038/npp.2017.204 · Cited by 301 · see citing works
Recent insights into the biological functions of liver fatty acid binding protein 1
Wang, G., Bonkovsky, H. L., de Lemos, A., & Burczynski, F. J. (2015) · Journal of Lipid Research · doi:10.1194/jlr.r056705 · Cited by 275 · see citing works
The cannabinoid system and pain
Woodhams, S. G., Chapman, V., Finn, D. P., Hohmann, A. G., & Neugebauer, V. (2017) · Neuropharmacology · doi:10.1016/j.neuropharm.2017.06.015 · Cited by 272 · see citing works
“Fatty acid binding proteins have been strongly implicated (e.g. Kaczocha et al., 2009, 2015, 2014), but their roles have yet to be full elucidated.”
Cannabinoid Signaling in the Skin: Therapeutic Potential of the “C(ut)annabinoid” System
Tóth, K. F., Ádám, D., Bı́ró, T., & Oláh, A. (2019) · Molecules · doi:10.3390/molecules24050918 · Cited by 209 · see citing works
Oxidative stress-induced FABP5 S-glutathionylation protects against acute lung injury by suppressing inflammation in macrophages
Guo, Y., Liu, Y., Zhao, S., Xu, W., Li, Y., Zhao, P., Wang, D., Cheng, H., Ke, Y., & Zhang, X. Z. (2021) · Nature Communications · doi:10.1038/s41467-021-27428-9 · Cited by 194 · see citing works
Infiltrative and drug‐resistant slow‐cycling cells support metabolic heterogeneity in glioblastoma
Hoang-Minh, L., Siebzehnrübl, F. A., Yang, C., Suzuki‐Hatano, S., Dajac, K., Loche, T., Andrews, N., Massari, M. S., Patel, J., Amin, K., et al. (2018) · The EMBO Journal · doi:10.15252/embj.201798772 · Cited by 181 · see citing works
“Fatty acid transporter inhibitors SB-FI-26 (Cayman Chemicals, #14191) and BMS309403 (Millipore, #34310) were used to inhibit FABP7 (Kaczocha et al , 2014) and FABP3 (Furuhashi et al , 2007), respectively.”
Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years
Maccarrone, M., Di Marzo, V., Gertsch, J., Grether, U., Howlett, A. C., Hua, T., Makriyannis, A., Piomelli, D., Ueda, N., & van der Stelt, M. (2023) · Pharmacological Reviews · doi:10.1124/pharmrev.122.000600 · Cited by 183 · see citing works
Fatty Acid Signaling Mechanisms in Neural Cells: Fatty Acid Receptors
Falomir‐Lockhart, L. J., Cavazzutti, G. F., Giménez, E., & Toscani, A. M. (2019) · Frontiers in Cellular Neuroscience · doi:10.3389/fncel.2019.00162 · Cited by 162 · see citing works
Targeting Cannabinoid Signaling in the Immune System: “High”-ly Exciting Questions, Possibilities, and Challenges
Oláh, A., Szekanecz, Z., & Bı́ró, T. (2017) · Frontiers in Immunology · doi:10.3389/fimmu.2017.01487 · Cited by 123 · see citing works
Endocannabinoid Transport Revisited
Nicolussi, S., & Gertsch, J. (2015) · Vitamins and hormones · doi:10.1016/bs.vh.2014.12.011 · Cited by 123 · see citing works
Enhanced endocannabinoid tone as a potential target of pharmacotherapy
Toczek, M., & Malinowska, B. (2018) · Life Sciences · doi:10.1016/j.lfs.2018.04.054 · Cited by 104 · see citing works
Multiple endocannabinoid-mediated mechanisms in the regulation of energy homeostasis in brain and peripheral tissues
de Azúa, I. R., & Lutz, B. (2018) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-018-2994-6 · Cited by 88 · see citing works
Fatty-acid–binding protein 5 controls retrograde endocannabinoid signaling at central glutamate synapses
Haj-Dahmane, S., Shen, R.-Y., Elmes, M., Studholme, K., Kanjiya, M. P., Bogdan, D. M., Thanos, P. K., Miyauchi, J., Tsirka, S., Deutsch, D., et al. (2018) · Proceedings of the National Academy of Sciences of the United States of America · doi:10.1073/pnas.1721339115 · Cited by 67 · see citing works
“Consequently, inhibition of FABPs, which increases eCB levels in the brain (23), in principle should potentiate phasic retrograde eCB signaling at central synapses.”
BackgroundResultInfluentialSelf-citation
Rare genetic variants in the endocannabinoid system genes CNR1 and DAGLA are associated with neurological phenotypes in humans
Smith, D. R., Stanley, C. M., Foss, T., Boles, R. G., & McKernan, K. J. (2017) · PLoS ONE · doi:10.1371/journal.pone.0187926 · Cited by 77 · see citing works
Fatty acids, endocannabinoids and inflammation
Witkamp, R. F. (2015) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2015.08.051 · Cited by 76 · see citing works
Modulation of the Endocannabinoid System as a Potential Anticancer Strategy
Ramer, R., Schwarz, R., & Hinz, B. (2019) · Frontiers in Pharmacology · doi:10.3389/fphar.2019.00430 · Cited by 73 · see citing works
Fatty Acid Binding Protein Deletion Suppresses Inflammatory Pain through Endocannabinoid/<i>N</i>-Acylethanolamine-Dependent Mechanisms
Kaczocha, M., Glaser, S. T., Maher, T., Clavin, B., Hamilton, J., Rourke, J. O., Rebecchi, M., Puopolo, M., Owada, Y., & Thanos, P. K. (2015) · Molecular Pain · doi:10.1186/s12990-015-0056-8 · Cited by 68 · see citing works
“Enzyme assays AEA and 2-OG hydrolysis was performed exactly as described [6].”
BackgroundMethodInfluentialSelf-citation
FABP1: A Novel Hepatic Endocannabinoid and Cannabinoid Binding Protein
Huang, H., McIntosh, A. L., Martin, G. G., Landrock, D., Chung, S., Landrock, K. K., Dangott, L. J., Li, S., Kier, A. B., & Schroeder, F. (2016) · Biochemistry · doi:10.1021/acs.biochem.6b00446 · Cited by 64 · see citing works
Fatty acid–binding protein 5 controls microsomal prostaglandin E synthase 1 (mPGES-1) induction during inflammation
Bogdan, D., Falcone, J. I., Kanjiya, M. P., Park, S. H., Carbonetti, G., Studholme, K. M., Gomez, M., Lu, Y., Elmes, M. W., Smietalo, N., et al. (2018) · Journal of Biological Chemistry · doi:10.1074/jbc.ra118.001593 · Cited by 62 · see citing works
“Thus, in addition to cannabinoid and PPAR receptors (16, 17), suppression of PGE2 biosynthesis may contribute to the antinociceptive effects observed after FABP5 inhibition.”
BackgroundSelf-citation
Fatty Acid Binding Protein‐1 (FABP1) and the Human FABP1 T94A Variant: Roles in the Endocannabinoid System and Dyslipidemias
Schroeder, F., McIntosh, A. L., Martin, G. G., Huang, H., Landrock, D., Chung, S., Landrock, K. K., Dangott, L. J., Li, S., Kaczocha, M., et al. (2016) · Lipids · doi:10.1007/s11745-016-4155-8 · Cited by 60 · see citing works
“Since high endocannabinoid levels produce analgesia [108], the FABP1 gene ablation-induced increase in brain AEA level may decrease pain sensitivity (Fig.”
Self-citation
Molecular mechanism with regard to the binding selectivity of inhibitors toward FABP5 and FABP7 explored by multiple short molecular dynamics simulations and free energy analyses
Chen, J., Liu, X., Zhang, S., Chen, J., Sun, H., Zhang, L., & Zhang, Q. (2019) · Physical Chemistry Chemical Physics · doi:10.1039/c9cp05704h · Cited by 57 · see citing works
The Role of Nuclear Hormone Receptors in Cannabinoid Function
Pistis, M., & O’Sullivan, S. E. (2017) · Advances in pharmacology · doi:10.1016/bs.apha.2017.03.008 · Cited by 56 · see citing works
Mechanisms of Endocannabinoid Transport in the Brain
Kaczocha, M., & Haj-Dahmane, S. (2021) · British Journal of Pharmacology · doi:10.1111/bph.15469 · Cited by 39 · see citing works
“Indeed, pharmacological or genetic inhibition of FABP5 reduces the cellular uptake and metabolism of anandamide and elevates its levels in the brain (Bjorklund et al., 2014; Kaczocha et al., 2014, 2015; Kaczocha, Vivieca, et al., 2012; Yu et al., 2014).”
BackgroundSelf-citation
Joints for joints: cannabinoids in the treatment of rheumatoid arthritis
Lowin, T., Schneider, M., & Pongratz, G. (2019) · Current Opinion in Rheumatology · doi:10.1097/bor.0000000000000590 · Cited by 55 · see citing works
Inhibitor SBFI26 suppresses the malignant progression of castration-resistant PC3-M cells by competitively binding to oncogenic FABP5
Al-Jameel, W. H., Gou, X., Forootan, S. S., Fayi, M. S. A., Rudland, P. S., Forootan, F. S., Zhang, J., Cornford, P. A., Hussain, S. A., & Ke, Y. (2017) · Oncotarget · doi:10.18632/oncotarget.16055 · Cited by 54 · see citing works
“In a strategy to develop anti-inflammatory and anti-nociceptive reagents by targeting fatty acid protein anandamide transporters, SBFI26 was used to increase the brain anandamide levels and thus to produce analgesia effect [18, 19].”
Targeting the endocannabinoid system as a potential anticancer approach
Schwarz, R., Ramer, R., & Hinz, B. (2018) · Drug Metabolism Reviews · doi:10.1080/03602532.2018.1428344 · Cited by 54 · see citing works
“…with these data, chemically synthesized FABP inhibitors caused antinociceptive effects in rodents in a CB1- and PPARadependent manner associated with elevated brain levels of AEA (Kaczocha et al. 2014), implying FABPs as novel targets for the development of analgesic and anti-inflammatory drugs.”
BackgroundResult
Fetal Alcohol Spectrum Disorder: Potential Role of Endocannabinoids Signaling
Basavarajappa, B. S. (2015) · Brain Sciences · doi:10.3390/brainsci5040456 · Cited by 48 · see citing works
“Similar to FAAH inhibition, inhibitors of FABPs also reduce hydrolysis of AEA and its uptake into cells, raising levels of extracellular AEA [194–197].”
Background
Endocannabinoid signaling in brain diseases: Emerging relevance of glial cells
Bernal‐Chico, A., Tepavčević, V., Manterola, A., Utrilla, C. L., Matute, C., & Mato, S. (2022) · Glia · doi:10.1002/glia.24172 · Cited by 48 · see citing works
“N-acylethanolamines leading to analgesic and anti-inflammatory effects (Kaczocha et al., 2014; Kaczocha et al., 2015).”
Background
SAR studies on truxillic acid mono esters as a new class of antinociceptive agents targeting fatty acid binding proteins
Su, Y., Elmes, M. W., Tong, S., Hu, K., Awwa, M., Teng, G. Y. H., Jing, Y., Freitag, M., Gan, Q., Clement, T., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.04.050 · Cited by 48 · see citing works
“The compound has a half-life of ~3 hours in vivo and is efficacious in producing anti-inflammatory and anti-nociceptive effects in rodent models of visceral, thermal, neuropathic, and inflammatory pain [6].”
BackgroundResultInfluentialSelf-citation
Docetaxel/cabazitaxel and fatty acid binding protein 5 inhibitors produce synergistic inhibition of prostate cancer growth
Carbonetti, G., Converso, C., Clement, T., Wang, C., Trotman, L. C., Ojima, I., & Kaczocha, M. (2019) · The Prostate · doi:10.1002/pros.23921 · Cited by 48 · see citing works
“Our group has previously developed FABP5 inhibitors based upon the truxillic acid monoester scaffold, including the first‐generation inhibitor Stony Brook fatty acid‐binding protein inhibitor 26 (SBFI‐ 26).(15,16) Our recent efforts have led to the identification of second‐ generation FABP5 inhibitors that show enhanc…”
Self-citation
The Antinociceptive Agent SBFI-26 Binds to Anandamide Transporters FABP5 and FABP7 at Two Different Sites
Hsu, H.-C., Tong, S., Zhou, Y., Elmes, M. W., Su, Y., Kaczocha, M., Deutsch, D. G., Rizzo, R. C., Ojima, I., & Li, H. (2017) · Biochemistry · doi:10.1021/acs.biochem.7b00194 · Cited by 46 · see citing works
Self-citation
The Potential of Inhibitors of Endocannabinoid Metabolism for Drug Development: A Critical Review
Fowler, C. J. (2015) · Handbook of experimental pharmacology · doi:10.1007/978-3-319-20825-1_4 · Cited by 45 · see citing works
“No overt cannabinoid-like effects upon locomotion were seen (Berger et al. 2012; Kaczocha et al. 2014).”
Background
Endocannabinoids and Acute Pain Following Total Knee Arthroplasty
Azim, S., Nicholson, J., Rebecchi, M., Galbavy, W., Feng, T., Reinsel, R., Volkow, N., Benveniste, H., & Kaczocha, M. (2015) · Pain · doi:10.1097/01.j.pain.0000460315.80981.59 · Cited by 37 · see citing works
“Endocannabinoid quantification was performed exactly as described.(25)”
Self-citation
Mining the Nav1.7 interactome: Opportunities for chronic pain therapeutics
Chew, L. A., Bellampalli, S. S., Dustrude, E. T., & Khanna, R. (2019) · Biochemical Pharmacology · doi:10.1016/j.bcp.2019.01.018 · Cited by 43 · see citing works
Fatty-acid-binding protein inhibition produces analgesic effects through peripheral and central mechanisms
Peng, X., Studholme, K. M., Kanjiya, M. P., Luk, J., Bogdan, D., Elmes, M. W., Carbonetti, G., Tong, S., Teng, Y. G., Rizzo, R. C., et al. (2017) · Molecular Pain · doi:10.1177/1744806917697007 · Cited by 39 · see citing works
“In our previous work, we have shown that FABP5 inhibition reduces thermal hyperalgesia.(15,26,32) In nociceptors, thermal pain is transduced by the TRPV1 channel.”
BackgroundMethodInfluentialSelf-citation
Inactivated FABP5 suppresses malignant progression of prostate cancer cells by inhibiting the activation of nuclear fatty acid receptor PPARγ
Al-Jameel, W. H., Gou, X., Jin, X., Zhang, J., Wei, Q., Ai, J., Li, H., Al-Bayati, A. M. S., Platt-Higgins, A. M., Pettitt, A. R., et al. (2019) · Genes & Cancer · doi:10.18632/genesandcancer.192 · Cited by 39 · see citing works
“Recently-developed FABP5 inhibitors, which produce approximately 50% of the inhibitory effect of BMS309403, were originally effective analgesics and anti-inflammatory agents in mice [21-23].”
Background
SBFI26 induces triple‐negative breast cancer cells ferroptosis via lipid peroxidation
He, G., Zhang, Y., Feng, Y., Chen, T., Liu, M., Zeng, Y., Yin, X., Qu, S., Huang, L., Ke, Y., et al. (2024) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.18212 · Cited by 37 · see citing works
Fatty Acid Binding Protein 5 Modulates Docosahexaenoic Acid-Induced Recovery in Rats Undergoing Spinal Cord Injury
Figueroa, J. D., Serrano‐Illán, M., Campbell, J. L., Cordero, K., Miranda, J. D., & León, M. A. D. (2015) · Journal of Neurotrauma · doi:10.1089/neu.2015.4186 · Cited by 38 · see citing works
The endocannabinoid system in the amygdala and modulation of fear
Gunduz‐Cinar, O. (2020) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/j.pnpbp.2020.110116 · Cited by 38 · see citing works
Analysis of natural product regulation of opioid receptors in the treatment of human disease
Badal, S. A. M., Turfus, S. C., Rajnarayanan, R. V., Wilson-Clarke, C. F., & Sandiford, S. L. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.10.021 · Cited by 36 · see citing works
Fatty Acid-Binding Protein 5 Modulates Brain Endocannabinoid Tone and Retrograde Signaling in the Striatum
Fauzan, M., Oubraim, S., Yu, M., Glaser, S. T., Kaczocha, M., & Haj‐Dahmane, S. (2022) · Frontiers in Cellular Neuroscience · doi:10.3389/fncel.2022.936939 · Cited by 34 · see citing works
“Accordingly, FABP5 inhibition elevates AEA levels in the whole brain (Kaczocha et al., 2014; Yu et al., 2014).”
BackgroundMethodInfluentialSelf-citation
Retinol-binding protein 2 (RBP2) binds monoacylglycerols and modulates gut endocrine signaling and body weight
Lee, S., Yang, K. J. Z., Brun, P., Silvaroli, J. A., Yuen, J. J., Shmarakov, I. O., Jiang, H., FERANIL, J. B., Li, X., Lackey, A. I., et al. (2020) · Science Advances · doi:10.1126/sciadv.aay8937 · Cited by 32 · see citing works
N-Docosahexaenoylethanolamine Attenuates Neuroinflammation and Improves Hippocampal Neurogenesis in Rats with Sciatic Nerve Chronic Constriction Injury
Tyrtyshnaia, A. A., Egorova, E., Starinets, A., Ponomarenko, A. I., Ermolenko, E. V., & Manzhulo, I. (2020) · Marine Drugs · doi:10.3390/md18100516 · Cited by 31 · see citing works
“This is consistent with our results, a cording to which we observed an increas in locomotor activity in sham-operated syna tamide-tr ated rats, although lipid analysis revealed a significant increase in the anan amide brain concentration i synaptamide-treated rats, which can still stimulate CB1 receptors nd have analg…”
Result
FABP ‐1 gene ablation impacts brain endocannabinoid system in male mice
Martin, G. G., Chung, S., Landrock, D., Landrock, K. K., Huang, H., Dangott, L. J., Peng, X., Kaczocha, M., Seeger, D. R., Murphy, E. J., et al. (2016) · Journal of Neurochemistry · doi:10.1111/jnc.13664 · Cited by 30 · see citing works
“Earlier studies showed that ablation (FABP3 null, FABP5 null) or chemical inhibition of brain FABPs increased brain AEA levels because of decreased AEA transport/targeting for intracellular degradation/hydrolysis by FAAH in the endoplasmic reticulum (Kaczocha 2009; Berger et al. 2012; Leung et al. 2013; Kaczocha et al…”
BackgroundMethodInfluentialSelf-citation
Examination of the Addictive and Behavioral Properties of Fatty Acid-Binding Protein Inhibitor SBFI26
Thanos, P. K., Clavin, B. H., Hamilton, J., O’Rourke, J. R., Maher, T., Koumas, C., Miao, E., Lankop, J., Elhage, A., Haj‐Dahmane, S., et al. (2016) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2016.00054 · Cited by 30 · see citing works
“One possible explanation for the lack of significant differences in behavior in the present study is the degree to which SBFI26 raises AEA levels – URB597 has been shown to cause a fourfold increase of this endocannabinoid in mouse brain (5), whereas our group detected significant but smaller increases from SBFI26 (26…”
BackgroundMethodResultInfluentialSelf-citation
Defects in fatty acid amide hydrolase 2 in a male with neurologic and psychiatric symptoms
Sirrs, S., van Karnebeek, C. D., Peng, X., Shyr, C., Tarailo-Graovac, M., Mandal, R., Testa, D., Dubin, D., Carbonetti, G., Glynn, S. E., et al. (2015) · Orphanet Journal of Rare Diseases · doi:10.1186/s13023-015-0248-3 · Cited by 28 · see citing works
“Endocannabinoid levels were quantified exactly as described [30].”
MethodSelf-citation
Metal-Free [2 + 2]-Photocycloaddition of (Z)-4-Aryliden-5(4H)-Oxazolones as Straightforward Synthesis of 1,3-Diaminotruxillic Acid Precursors: Synthetic Scope and Mechanistic Studies
García-Montero, A., Rodríguez, A. M., Juan, A., Velders, A. H., Denisi, A., Jiménez‐Osés, G., Gómez‐Bengoa, E., Cativiela, C., Gómez, M. V., & Urriolabeitia, E. P. (2017) · ACS Sustainable Chemistry & Engineering · doi:10.1021/acssuschemeng.7b02140 · Cited by 27 · see citing works
Discovery and Preclinical Evaluation of a Novel Inhibitor of FABP5, ART26.12, Effective in Oxaliplatin-Induced Peripheral Neuropathy
Warren, W. G., Osborn, M., Tsantoulas, C., David-Pereira, A., Cohn, D., Duffy, P., Ruston, L., Johnson, C. T., Bradshaw, H. B., Kaczocha, M., et al. (2024) · Journal of Pain · doi:10.1016/j.jpain.2024.01.335 · Cited by 26 · see citing works
“Of note the hydroxyl group in NAE forms key hydrogen bonds with Tyr131 and Arg129 in FABP5, the same residues as the carboxylate in SBFI-26 (the first-generation FABP5 inhibitor).”
InfluentialSelf-citation
The Endocannabinoid System and Its Role in Regulating the Intrinsic Neural Circuitry of the Gastrointestinal Tract
Trautmann, S. M., & Sharkey, K. A. (2015) · International review of neurobiology · doi:10.1016/bs.irn.2015.10.002 · Cited by 26 · see citing works
Analysis of natural product regulation of cannabinoid receptors in the treatment of human disease
Badal, S. A. M., Smith, K. N., & Rajnarayanan, R. V. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.06.003 · Cited by 26 · see citing works
“These translate to antinociceptive action (Kaczocha et al., 2014), anxiolytic-like properties (Marco et al., 2015), antidepressant activity (Trezza & Campolongo, 2013), anti-tumour efficacy (Picardi, Ciaglia, Proto, & Pisanti, 2014), and the lowering of blood pressure in hypertensive experimental…”
Background
Application of target repositioning and in silico screening to exploit fatty acid binding proteins (FABPs) from Echinococcus multilocularis as possible drug targets
Bélgamo, J. A., Alberca, L. N., Pórfido, J. L., Romero, F. N. C., Rodrı́guez, S., Talevi, A., Córsico, B., & Franchini, G. R. (2020) · Journal of Computer-Aided Molecular Design · doi:10.1007/s10822-020-00352-8 · Cited by 25 · see citing works
Identification of Fatty Acid Binding Protein 5 Inhibitors Through Similarity-Based Screening
Zhou, Y., Elmes, M. W., Sweeney, J., Joseph, O. M., Che, J., Hsu, H.-C., Li, H., Deutsch, D. G., Ojima, I., Kaczocha, M., et al. (2019) · Biochemistry · doi:10.1021/acs.biochem.9b00625 · Cited by 24 · see citing works
Self-citation
FABP5 deletion in nociceptors augments endocannabinoid signaling and suppresses TRPV1 sensitization and inflammatory pain
Bogdan, D., Studholme, K. M., DiBua, A., Gordon, C., Kanjiya, M. P., Yu, M., Puopolo, M., & Kaczocha, M. (2022) · Scientific Reports · doi:10.1038/s41598-022-13284-0 · Cited by 22 · see citing works
Self-citation
Impact of fatty acid binding protein 5‐deficiency on COPD exacerbations and cigarette smoke‐induced inflammatory response to bacterial infection
Rao, D. M., Phan, D. T., Choo, M. J., Weaver, M. R., Oberley‐Deegan, R. E., Bowler, R. P., & Gally, F. (2019) · Clinical and Translational Medicine · doi:10.1186/s40169-019-0227-8 · Cited by 22 · see citing works
“Although FABP5 has been shown to be pro-inflammatory in several models, including high fat diet-induced skin inflammation [15], allergic asthma [16], LPS-induced liver damage [17] and neuropathic pain in mice [18], in this study we show that in the lungs of mice exposed to CS and infection, FABP5 expression, or re-exp…”
Prenatal ethanol exposure causes anxiety-like phenotype and alters synaptic nitric oxide and endocannabinoid signaling in dorsal raphe nucleus of adult male rats
Oubraim, S., Wang, R., Hausknecht, K. A., Kaczocha, M., Shen, R., & Haj‐Dahmane, S. (2022) · Translational Psychiatry · doi:10.1038/s41398-022-02210-7 · Cited by 21 · see citing works
“Endocannabinoids levels quantification The levels of 2-arachydonyl glycerol (2-AG) and anandamide (AEA) in rat DRn slices were quantified using mass spectrometry and deuterated internal 2-AG and AEA standards as described previously [30, 31].”
MethodSelf-citation
Fatty acid binding proteins are novel modulators of synaptic epoxyeicosatrienoic acid signaling in the brain
Glaser, S. T., Jayanetti, K., Oubraim, S., Hillowe, A., Frank, E., de Jong, J. G., Wang, L., Wang, H., Ojima, I., Haj‐Dahmane, S., et al. (2023) · Scientific Reports · doi:10.1038/s41598-023-42504-4 · Cited by 20 · see citing works
Self-citation
Cannabidiol and positive effects on object recognition memory in an in vivo model of Fragile X Syndrome: Obligatory role of hippocampal GPR55 receptors
Manduca, A., Buzzelli, V., Rava, A., Feo, A., Carbone, E., Schiavi, S., Peruzzi, B., Doria, V., Pezzullo, M., Pasquadibisceglie, A., et al. (2024) · Pharmacological Research · doi:10.1016/j.phrs.2024.107176 · Cited by 20 · see citing works
Integration and Comparison of Transcriptomic and Proteomic Data for Meningioma
Dunn, J., Lenis, V. P. E., Hilton, D. A., Warta, R., Herold‐Mende, C. C., Hanemann, C. O., & Futschik, M. E. (2020) · Cancers · doi:10.3390/cancers12113270 · Cited by 19 · see citing works
“Interestingly, FABP7 acts as an intracellular transporter of the antinociceptive endocannabinoid, anandamide, to the fatty acid amide hydrolase for its inactivation, which has led to the development of readily available FABP7 inhibitors for their analgesic and anti-inflammatory properties [38,39].”
Background
Identification of small molecule inhibitors of botulinum neurotoxin serotype E via footprint similarity
Zhou, Y., McGillick, B. E., Teng, Y. G., Haranahalli, K., Ojima, I., Swaminathan, S., & Rizzo, R. C. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.07.031 · Cited by 19 · see citing works
Self-citation
Leptin Levels Are Negatively Correlated with 2-Arachidonoylglycerol in the Cerebrospinal Fluid of Patients with Osteoarthritis
Nicholson, J., Azim, S., Rebecchi, M. J., Galbavy, W., Feng, T., Reinsel, R. A., Rizwan, S., Fowler, C. J., Benveniste, H., & Kaczocha, M. (2015) · PLoS ONE · doi:10.1371/journal.pone.0123132 · Cited by 17 · see citing works
“Endocannabinoid quantification was performed exactly as described [35, 36].”
MethodSelf-citation
Unpredictable chronic mild stress differentially impacts resting brain glucose metabolism in fatty acid-binding protein 7 deficient mice
Hamilton, J., Roeder, N. M., Richardson, B., Hammond, N., Sajjad, M., Yao, R., Owada, Y., Kagawa, Y., & Thanos, P. K. (2022) · Psychiatry Research Neuroimaging · doi:10.1016/j.pscychresns.2022.111486 · Cited by 19 · see citing works
Female Mice are Resistant to Fabp1 Gene Ablation‐Induced Alterations in Brain Endocannabinoid Levels
Martin, G. G., Chung, S., Landrock, D., Landrock, K. K., Dangott, L. J., Peng, X., Kaczocha, M., Murphy, E. J., Kier, A. B., & Schroeder, F. (2016) · Lipids · doi:10.1007/s11745-016-4175-4 · Cited by 17 · see citing works
“Ablation/inhibition of cytosolic ‘chaperones’ is known to decrease NAE and 2-MG targeting for degradation which in turn increases their level [38, 47, 79].”
Self-citation
SAR study on Novel truxillic acid monoester-Based inhibitors of fatty acid binding proteins as Next-Generation antinociceptive agents
Wang, H., Taouil, A. K., Awwa, M., Clement, T., Zhu, C., Kim, J., Rendina, D., Jayanetti, K., Maharaj, A., Wang, L., et al. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.106184 · Cited by 17 · see citing works
Self-citation
Potential safety implications of fatty acid-binding protein inhibition
Warren, W. G., Osborn, M., Duffy, P., Yates, A., & O’Sullivan, S. E. (2024) · Toxicology and Applied Pharmacology · doi:10.1016/j.taap.2024.117079 · Cited by 17 · see citing works
Critical Review on the Chemical Aspects of Cannabidiol (CBD) and Harmonization of Computational Bioactivity Data
Mastinu, A., Ribaudo, G., Ongaro, A., Bonini, S. A., Memo, M., & Gianoncelli, A. (2020) · Current Medicinal Chemistry · doi:10.2174/0929867327666200210144847 · Cited by 17 · see citing works
Fatty acid-binding proteins 5 and 7 gene deletion increases sucrose consumption and diminishes forced swim immobility time
Hamilton, J., Koumas, C., Clavin, B. H., Marion, M., Figueiredo, A. M. P. D., Gonzalez, S., O’Rourke, J. R., Deutsch, D. G., Kaczocha, M., Haj‐Dahmane, S., et al. (2018) · Behavioural Pharmacology · doi:10.1097/fbp.0000000000000402 · Cited by 16 · see citing works
Self-citation
Time-resolved single-cell RNAseq profiling identifies a novel Fabp5+ subpopulation of inflammatory myeloid cells with delayed cytotoxic profile in chronic spinal cord injury
Hamel, R., Peruzzotti‐Jametti, L., Ridley, K., Testa, V., Yu, B., Rowitch, D. H., Marioni, J. C., & Pluchino, S. (2023) · Heliyon · doi:10.1016/j.heliyon.2023.e18339 · Cited by 19 · see citing works
“4D) [26], the next stage in the Monocle3 predicted trajectory (Fig.”
Background
Identification of a novel fatty acid binding protein-5-CB2 receptor-dependent mechanism regulating anxiety behaviors in the prefrontal cortex
Uzuneser, T. C., Szkudlarek, H. J., Jones, M., Nashed, M. G., Clement, T., Wang, H., Ojima, I., Rushlow, W. J., & Laviolette, S. R. (2022) · Cerebral Cortex · doi:10.1093/cercor/bhac220 · Cited by 15 · see citing works
Self-citation
Fatty acid binding protein 5 inhibition attenuates pronociceptive cytokine/chemokine expression and suppresses osteoarthritis pain: A comparative human and rat study
Gordon, C., Trainor, J., Shah, R. J., Studholme, K. M., Gelman, A., Doswell, F., Sadar, F., Giovannetti, A., Gershenson, J., Khan, A., et al. (2023) · Osteoarthritis and Cartilage · doi:10.1016/j.joca.2023.11.010 · Cited by 17 · see citing works
Self-citation
Δ9-Tetrahydrocannabinol induces endocannabinoid accumulation in mouse hepatocytes: antagonism by Fabp1 gene ablation
McIntosh, A. L., Martin, G. G., Huang, H., Landrock, D., Kier, A. B., & Schroeder, F. (2018) · Journal of Lipid Research · doi:10.1194/jlr.m082644 · Cited by 15 · see citing works
“been demonstrated for FABP5 and FABP7 in cultured transfected cells (75, 78-82).”
Background
Pharmacological Inhibition of Brain Fatty Acid Binding Protein Reduces Ethanol Consumption in Mice
Figueiredo, A. M. P. D., Hamilton, J., Marion, M., Blum, K., Kaczocha, M., Haj‐Dahmane, S., Deutsch, D. G., & Thanos, P. K. (2017) · Journal of Reward Deficiency Syndrome and Addiction Science · doi:10.17756/jrdsas.2017-037 · Cited by 15 · see citing works
“SBFI26 was administered at a dose of 20 mg/kg, as this dose has been previously demonstrated to significantly elevate brain levels of AEA in mice [23].”
BackgroundInfluentialSelf-citation
Impact of Fabp1 Gene Ablation on Uptake and Degradation of Endocannabinoids in Mouse Hepatocytes
McIntosh, A. L., Huang, H., Landrock, D., Martin, G. G., Li, S., Kier, A. B., & Schroeder, F. (2018) · Lipids · doi:10.1002/lipd.12071 · Cited by 15 · see citing works
Functionalized 1,3‐Diaminotruxillic Acids by Pd‐Mediated C–H Activation and [2+2]‐Photocycloaddition of 5(4H)‐Oxazolones
Carrera, C., Denisi, A., Cativiela, C., & Urriolabeitia, E. P. (2019) · European Journal of Inorganic Chemistry · doi:10.1002/ejic.201900548 · Cited by 15 · see citing works
Identification of new dual FABP4/5 inhibitors based on a naphthalene-1-sulfonamide FABP4 inhibitor
He, Y., Dou, H., Gao, D., Wang, T., Zhang, M., Wang, H., & Li, Y. (2019) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2019.07.031 · Cited by 15 · see citing works
Environmental enrichment sex-dependently rescues memory impairment in FABP5 KO mice not mediated by brain-derived neurotrophic factor
Marion, M., Hamilton, J., Richardson, B., Roeder, N. M., Figueiredo, A. M. P. D., Nubelo, A., Hetelekides, E. M., Penman, S. L., Owada, Y., Kagawa, Y., et al. (2022) · Behavioural Brain Research · doi:10.1016/j.bbr.2022.113814 · Cited by 14 · see citing works
FABP5 is important for cognitive function and is an important regulator of the physiological effects and pharmacokinetics of acute Δ9 tetrahydrocannabinol inhalation in mice
Penman, S. L., Roeder, N. M., Berthold, E. C., Senetra, A. S., Marion, M., Richardson, B., White, O., Fearby, N. L., McCurdy, C. R., Hamilton, J., et al. (2023) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2023.173633 · Cited by 12 · see citing works
Two fatty acid‐binding proteins expressed in the intestine interact differently with endocannabinoids
Lai, M. P., Katz, F. S., Bernard, C., Storch, J., & Stark, R. E. (2020) · Protein Science · doi:10.1002/pro.3875 · Cited by 12 · see citing works
Human Liver Fatty Acid Binding Protein-1 T94A Variant, Nonalcohol Fatty Liver Disease, and Hepatic Endocannabinoid System.
Martin, G., Landrock, D., Dangott, L., McIntosh, A., Kier, A., & Schroeder, F. (2018) · Lipids · doi:10.1002/lipd.12008 · Cited by 13 · see citing works
A review from patents inspired by the genus Cannabis
Flores‐Sanchez, I. J., & Ramos-Valdivia, A. C. (2016) · Phytochemistry Reviews · doi:10.1007/s11101-016-9485-x · Cited by 12 · see citing works
“Fatty acid binding proteins (FABPs) are intracellular lipid chaperones that interact with the transport of fatty acids, endocannabinoids (Kaczocha et al. 2014, 2015) and cannabinoids (Elmes et al. 2015) to its catabolism; being important regulators of the endocannabinoid tone.”
Background
Contribution of diacylglycerol lipase β to pain after surgery
Luk, J., Lu, Y., Ackermann, A., Peng, X., Bogdan, D., Puopolo, M., Komatsu, D. E., Tong, S., Ojima, I., Rebecchi, M. J., et al. (2018) · Journal of Pain Research · doi:10.2147/jpr.s157208 · Cited by 11 · see citing works
“The parameters for the endocannabinoid quantification were as described.(25) AA and PGE 2 analysis was performed on a Thermo Fisher Scientific 3000 HPLC system equipped with a Luna C18 column (150×2 mm) coupled to the electrospray Scheme 1 Synthesis of KT109.”
MethodSelf-citation
Synthesis of esters of diaminotruxillic bis-amino acids by Pd-mediated photocycloaddition of analogs of the Kaede protein chromophore
Urriolabeitia, E. P., Sánchez, P., Pop, A., Silvestru, C., Laga, E., Jiménez, A. I., & Cativiela, C. (2020) · Beilstein Journal of Organic Chemistry · doi:10.3762/bjoc.16.98 · Cited by 11 · see citing works
Maternal supplementation with n-3 fatty acids affects placental lipid metabolism, inflammation, oxidative stress, the endocannabinoid system, and the neonate cytokine concentrations in dairy cows
Silva, P. D. S., Kra, G., Butenko, Y., Daddam, J. R., Levin, Y., & Zachut, M. (2024) · Journal of Animal Science and Biotechnology/Journal of animal science and biotechnology · doi:10.1186/s40104-024-01033-4 · Cited by 10 · see citing works
“Interestingly, FABP3, FABP5, and FAB7 are also involved in the uptake, intracellular transport, and hydrolysis of endocannabinoids [51, 55, 73–76].”
Background
FABP 4 blocker attenuates colonic hypomotility and modulates white adipose tissue‐derived hormone levels in mouse models mimicking constipation‐predominant IBS
Mosińska, P., Jacenik, D., Sałaga, M., Wasilewski, A., Cygankiewicz, A. I., Sibaev, A., Mokrowiecka, A., Malecka-Panas, E. I., Pintelon, I., Storr, M., et al. (2017) · Neurogastroenterology & Motility · doi:10.1111/nmo.13272 · Cited by 10 · see citing works
Inhibition of fatty acid binding protein-5 in the basolateral amygdala induces anxiolytic effects and accelerates fear memory extinction
Jones, M. J., Uzuneser, T. C., Clement, T., Wang, H., Ojima, I., Rushlow, W. J., & Laviolette, S. R. (2023) · Psychopharmacology · doi:10.1007/s00213-023-06468-7 · Cited by 9 · see citing works
“Previous studies have shown that pharmacological or genetic FABP5 inhibition can significantly raise AEA levels, whilst not impacting levels of the other main eCB, 2-AG (Yu et al. 2014; Kaczocha et al. 2014).”
InfluentialSelf-citation
FABP5 can substitute for androgen receptor in malignant progression of prostate cancer cells
Naeem, A. A., Abdulsamad, S. A., Zeng, H., He, G., Jin, X., Zhang, J., Alenezi, B. T., Ma, H., Rudland, P. S., & Ke, Y. (2023) · International Journal of Oncology · doi:10.3892/ijo.2023.5606 · Cited by 9 · see citing works
Sterol Carrier Protein‐2/Sterol Carrier Protein‐x/Fatty Acid Binding Protein‐1 Ablation Impacts Response of Brain Endocannabinoid to High‐Fat Diet
Martin, G. G., Seeger, D. R., McIntosh, A. L., Milligan, S., Chung, S., Landrock, D., Dangott, L. J., Golovko, M. Y., Murphy, E. J., Kier, A. B., et al. (2019) · Lipids · doi:10.1002/lipd.12192 · Cited by 9 · see citing works
Synthesis and Preliminary Evaluation of N-(16-18F-Fluorohexadecanoyl)ethanolamine (18F-FHEA) as a PET Probe of N-Acylethanolamine Metabolism in Mouse Brain
Pandey, M. K., DeGrado, T. R., Qian, K., Jacobson, M., Hagen, C. E., Duclos, R. I., & Gatley, S. J. (2014) · ACS Chemical Neuroscience · doi:10.1021/cn400214j · Cited by 9 · see citing works
The role of fatty acid-binding protein 5 and 7 on locomotor, anxiety and social behavior: Interaction with NMDA signaling
Khan, A., Richardson, B., Roeder, N. M., Hamilton, J., Marion, M., Fearby, N. L., White, O., Owada, Y., Kagawa, Y., & Thanos, P. K. (2024) · Neuroscience Letters · doi:10.1016/j.neulet.2024.137862 · Cited by 8 · see citing works
Astrocytic FABP5 mediates retrograde endocannabinoid transport at central synapses
Oubraim, S., Fauzan, M., Studholme, K. M., Gordon, C., Glaser, S. T., Shen, R., Ojima, I., Kaczocha, M., & Haj‐Dahmane, S. (2025) · iScience · doi:10.1016/j.isci.2025.112342 · Cited by 8 · see citing works
Self-citation
Endocannabinoid Interaction with Human FABP1: Impact of the T94A Variant
Martin, G. G., Huang, H., McIntosh, A. L., Kier, A. B., & Schroeder, F. (2017) · Biochemistry · doi:10.1021/acs.biochem.7b00647 · Cited by 8 · see citing works
Experimental treatment efficacy of dmrFABP5 on prostate cancer singly or in combination with drugs in use
Abdulsamad, S. A., Naeem, A. A., Zeng, H., He, G., Jin, X., Alenezi, B. T., Ai, J., Zhang, J., Ma, H., & Ke, Y. (2024) · American Journal of Cancer Research · doi:10.62347/yppt5752 · Cited by 8 · see citing works
FABP 1 in wonderland
Prinetti, A., & Mitro, N. (2016) · Journal of Neurochemistry · doi:10.1111/jnc.13685 · Cited by 8 · see citing works
“It has been recently reported that FABP3, 5 and 7 can shuttle endocannabinoids in the brain (Kaczocha et al. 2009, 2014), therefore given the increased circulating total levels of arachidonic acid-derived endocannabinoids found in LFABP1KO mice is tempting to speculate that also FABP1 might bind…”
Background
Fatty acid binding protein 7 plays an important modulatory sex-dependent role on brain endocannabinoid levels and THC metabolism
Penman, S. L., Senetra, A. S., Roeder, N. M., Richardson, B., Pareek, O., Owada, Y., Kagawa, Y., Gold, M. S., McCurdy, C. R., Sharma, A., et al. (2024) · PLoS ONE · doi:10.1371/journal.pone.0313091 · Cited by 7 · see citing works
Dimethylaminophenyl Hydrazides as Inhibitors of the Lipid Transport Protein LprG in Mycobacteria
Bai, L., Parkin, L. A., Zhang, H., Shum, R., Previti, M. L., & Seeliger, J. C. (2020) · ACS Infectious Diseases · doi:10.1021/acsinfecdis.9b00497 · Cited by 7 · see citing works
Incarvillateine produces antinociceptive and motor suppressive effects via adenosine receptor activation
Kim, J., Bogdan, D., Elmes, M. W., Awwa, M., Su, Y., Che, J., Lee, G., Deutsch, D. G., Rizzo, R. C., Kaczocha, M., et al. (2019) · PLoS ONE · doi:10.1371/journal.pone.0218619 · Cited by 7 · see citing works
Self-citation
Fatty acid binding proteins and their involvement in anxiety and mood disorders
Jones, M., Uzuneser, T. C., & Laviolette, S. R. (2025) · Neurobiology of Disease · doi:10.1016/j.nbd.2025.106952 · Cited by 6 · see citing works

Fatty Acid Binding Protein Deletion Suppresses Inflammatory Pain through Endocannabinoid/<i>N</i>-Acylethanolamine-Dependent Mechanisms
Kaczocha, M., Glaser, S. T., Maher, T., Clavin, B., Hamilton, J., Rourke, J. O., Rebecchi, M., Puopolo, M., Owada, Y., & Thanos, P. K. (2015) · Molecular Pain · doi:10.1186/s12990-015-0056-8 · Cited by 68 · see citing works
Self-citation
FABP5 deletion in nociceptors augments endocannabinoid signaling and suppresses TRPV1 sensitization and inflammatory pain
Bogdan, D., Studholme, K. M., DiBua, A., Gordon, C., Kanjiya, M. P., Yu, M., Puopolo, M., & Kaczocha, M. (2022) · Scientific Reports · doi:10.1038/s41598-022-13284-0 · Cited by 22 · see citing works
Self-citation
Targeting Fatty Acid Binding Protein (FABP) Anandamide Transporters – A Novel Strategy for Development of Anti-Inflammatory and Anti-Nociceptive Drugs
Berger, W. T., Ralph, B. P., Kaczocha, M., Sun, J. Y., Balius, T. E., Rizzo, R. C., Haj‐Dahmane, S., Ojima, I., & Deutsch, D. G. (2012) · PLoS ONE · doi:10.1371/journal.pone.0050968 · Cited by 164 · see citing works
Self-citation
Fatty-acid-binding protein inhibition produces analgesic effects through peripheral and central mechanisms
Peng, X., Studholme, K. M., Kanjiya, M. P., Luk, J., Bogdan, D., Elmes, M. W., Carbonetti, G., Tong, S., Teng, Y. G., Rizzo, R. C., et al. (2017) · Molecular Pain · doi:10.1177/1744806917697007 · Cited by 39 · see citing works
Self-citation
Evaluating FABP5 as a Therapeutic Target for Pain Management
Warren, W. G., Osborn, M., Kaczocha, M., Yates, A. S., & O’Sullivan, S. E. (2026) · European Journal of Pain · doi:10.1002/ejp.70267 · Cited by 1 · see citing works
Self-citation

Authors: Kaczocha, M., Rebecchi, M. J., Ralph, B. P., Teng, Y.-H. G., Berger, W. T., Galbavy, W., Elmes, M. W., Glaser, S. T., Wang, L., Rizzo, R. C., Deutsch, D. G., & Ojima, I.
Affiliations: Stony Brook University (US)
Kingsborough Community College (US)
Corresponding author: Kaczocha, Martin
ORCID: Kaczocha, Martin
Rebecchi, Mario J.
Teng, Yu-Han Gary
Galbavy, William
Wang, Liqun
Rizzo, Robert C.
Ojima, Iwao
Venue: PLoS ONE
Publisher: Public Library of Science (PLoS)
Published: 2014-04-04
Volume: 9
Issue: 4
Pages: e94200
ISSN: 1932-6203 (ISSN-L)
DOI: 10.1371/journal.pone.0094200
PMC: PMC3976407
OpenAlex: W2057639794
Cited by: 142
References: 53
Citations by year: 2026: 7 · 2025: 14 · 2024: 15 · 2023: 10 · 2022: 12 · 2021: 4 · 2020: 10 · 2019: 14 · 2018: 15 · 2017: 15 · 2016: 10 · 2015: 15 · 2014: 1
FWCI: 10.20
Type: journal article
Language: en
Open access: gold
doi.org
Licence: cc-by
creativecommons.org/licenses/by/4.0/ (unspecified)
Locations: PLoS ONE (publishedVersion, cc-by)
Europe PMC (PubMed Central) (publishedVersion, cc-by)
PubMed Central (publishedVersion, cc-by)
PubMed (publishedVersion)
CUNY Academic Works (City University of New York) (submittedVersion)
DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders: National Institutes of Health (DA032232)
National Institute on Drug Abuse (DA032232, R01DA035923, DA035923, R01DA016419, DA016419, R21DA032232)
Topics: Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
Health Sciences › Nursing › Nutrition and Dietetics › Fatty Acid Research and Health
Keywords: fatty acid binding protein, anandamide, endocannabinoid system, fatty acid amide hydrolase, FABP5, FABP3, FABP7, antinociception, analgesia, inflammatory pain, visceral pain, neuropathic pain, CB1 receptor, PPARα, N-acylethanolamines
MeSH terms: Analgesia, Analgesics, Animals, Arachidonic Acids, Brain, Disease Models, Animal, Hyperalgesia, Male, Models, Molecular, Molecular Conformation, Neuralgia, Protein Binding, Receptor, Cannabinoid, CB1, PPAR alpha, Fatty Acid-Binding Proteins, Mice, Rats, Polyunsaturated Alkamides, Molecular Docking Simulation, Endocannabinoids

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Inhibition of Fatty Acid Binding Proteins Elevates Brain Anandamide Levels and Produces Analgesia

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