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Endocannabinoid Turnover

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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase

Keith, J. M., Jones, W. M., Pierce, J. M., Seierstad, M. J., Palmer, J. A., Webb, M., Karbarz, M. J., Scott, B. P., Wilson, S. J., Luo, L., et al. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2013.12.113 · Cited by 30 · see citing works

Pain and beyond: fatty acid amides and fatty acid amide hydrolase inhibitors in cardiovascular and metabolic diseases

Pillarisetti, S., Alexander, C. W., & Khanna, I. (2009) · Drug Discovery Today · doi:10.1016/j.drudis.2009.08.002 · Cited by 29 · see citing works

The Endocannabinoid Anandamide Inhibits Voltage-Gated Sodium Channels Nav1.2, Nav1.6, Nav1.7, and Nav1.8 in Xenopus Oocytes

Okura, D., Horishita, T., Ueno, S., Yanagihara, N., Sudo, Y., Uezono, Y., & Sata, T. (2014) · Anesthesia & Analgesia · doi:10.1213/ane.0000000000000070 · Cited by 28 · see citing works

Design, Synthesis, and Characterization of α-Ketoheterocycles That Additionally Target the Cytosolic Port Cys269 of Fatty Acid Amide Hydrolase

Otrubova, K., Cravatt, B. F., & Boger, D. L. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm401820q · Cited by 28 · see citing works

The cytoprotective effects of oleoylethanolamide in insulin‐secreting cells do not require activation of GPR119

Stone, V. M., Dhayal, S., Smith, D. M., Lenaghan, C., Brocklehurst, K. J., & Morgan, N. G. (2011) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2011.01755.x · Cited by 26 · see citing works

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase

Gattinoni, S., Simone, C. D., Dallavalle, S., Fezza, F., Nannei, R., Battista, N., Minetti, P., Quattrociocchi, G., Caprioli, A., Borsini, F., et al. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.06.050 · Cited by 25 · see citing works

Heteroaryl urea inhibitors of fatty acid amide hydrolase: Structure–mutagenicity relationships for arylamine metabolites

Tichenor, M. S., Keith, J. M., Jones, W. M., Pierce, J. M., Merit, J. E., Hawryluk, N. A., Seierstad, M. J., Palmer, J. A., Webb, M., Karbarz, M. J., et al. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.10.076 · Cited by 24 · see citing works

2-Amino-5-arylbenzoxazole derivatives as potent inhibitors of fatty acid amide hydrolase (FAAH)

Estiarte, M. A., Johnson, R. J. K., Kaub, C. J., Gowlugari, S., O’Mahony, D. J. R., Nguyen, M. T. L., Emerling, D. E., Kelly, M. G., Kincaid, J., Vincent, F., et al. (2012) · MedChemComm · doi:10.1039/c2md00307d · Cited by 17 · see citing works

Biochemical characterization and in vitro activity of AZ513, a noncovalent, reversible, and noncompetitive inhibitor of fatty acid amide hydrolase

Scott, C. W., Tian, G., Yu, X. H., Paschetto, K. A., Wilkins, D. E., Meury, L., Cao, C. Q., Varnes, J. G., & Edwards, P. D. (2011) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2011.05.052 · Cited by 15 · see citing works

Fatty Acid Amide Hydrolase (FAAH) Inhibitors Exert Pharmacological Effects, but Lack Antinociceptive Efficacy in Rats with Neuropathic Spinal Cord Injury Pain

Hama, A. T., Germano, P., Varghese, M. S., Cravatt, B. F., Milne, G. T., Pearson, J. P., & Sagen, J. (2014) · PLoS ONE · doi:10.1371/journal.pone.0096396 · Cited by 15 · see citing works

Practical Considerations for the Use of Cannabis in Cancer Pain Management—What a Medical Oncologist Should Know

Gorzo, A., Havasi, A. D., Spînu, Ș., Oprea, A. L., Burz, C. C., & Sur, D. G. (2022) · Journal of Clinical Medicine · doi:10.3390/jcm11175036 · Cited by 13 · see citing works

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

Keith, J. M., Hawryluk, N. A., Apodaca, R. L., Chambers, A., Pierce, J. M., Seierstad, M. J., Palmer, J. A., Webb, M., Karbarz, M. J., Scott, B. P., et al. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.01.064 · Cited by 12 · see citing works

The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors

Keith, J. M., Tichenor, M. S., Apodaca, R. L., Xiao, W., Jones, W. M., Seierstad, M. J., Pierce, J. M., Palmer, J. A., Webb, M., Karbarz, M. J., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.05.001 · Cited by 12 · see citing works

Discovery libraries targeting the major enzyme classes: The serine hydrolases

Otrubova, K., Srinivasan, V., & Boger, D. L. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.06.063 · Cited by 12 · see citing works

Therapeutic Targeting of Peripheral Cannabinoid Receptors in Inflammatory and Neuropathic Pain States

Spigelman, I. (2009) · Frontiers in neuroscience · doi:10.1201/9781439812105-c5 · Cited by 12 · see citing works

N-(4-Methoxy-2-nitrophenyl)hexadecanamide, a palmitoylethanolamide analogue, reduces formalin-induced nociception

Roa‐Coria, J. E., Navarrete‐Vázquez, G., Fowler, C. J., Flores‐Murrieta, F. J., Déciga‐Campos, M., & Granados‐Soto, V. (2012) · Life Sciences · doi:10.1016/j.lfs.2012.09.024 · Cited by 11 · see citing works

Design, Synthesis and Biological Activity Evaluation of Arylpiperazine Derivatives for the Treatment of Neuropathic Pain

Chen, Y., Wang, G., Xu, X., Liu, B., Li, J., & Zhang, G. (2011) · Molecules · doi:10.3390/molecules16075785 · Cited by 11 · see citing works

Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors

Vincent, F., Nguyen, M. T. L., Emerling, D. E., Kelly, M. G., & Duncton, M. A. J. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.09.086 · Cited by 9 · see citing works

Pharmacological characterization of a novel, potent, selective, and orally active fatty acid amide hydrolase inhibitor, PKM‐833 [(R)‐N‐(pyridazin‐3‐yl)‐4‐(7‐(trifluoromethyl)chroman‐4‐yl)piperazine‐1‐carboxamide] in rats: Potential for the treatment of inflammatory pain

Endo, T., Takeuchi, T., & Maehara, S. (2020) · Pharmacology Research & Perspectives · doi:10.1002/prp2.569 · Cited by 6 · see citing works

The Life Cycle of the Endocannabinoids: Formation and Inactivation

Alexander, S. P. H., & Kendall, D. A. (2009) · Current topics in behavioral neurosciences · doi:10.1007/978-3-540-88955-7_1 · Cited by 6 · see citing works

FAAH-Catalyzed C–C Bond Cleavage of a New Multitarget Analgesic Drug

Ligresti, A., Silvestri, C., Vitale, R. M., Martos, J. L., Piscitelli, F., Wang, J. W., Allarà, M., Carling, R. W., Luongo, L., Guida, F., et al. (2018) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.8b00315 · Cited by 5 · see citing works

Biochemical Mechanisms of Fatty Liver and Bioactive Foods

Sharma, R. K. (2012) · Elsevier eBooks · doi:10.1016/b978-0-12-397154-8.00181-0 · Cited by 5 · see citing works

Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase

Keith, J. M., Jones, W., Pierce, J. M., Seierstad, M. J., Palmer, J. A., Webb, M., Karbarz, M. J., Scott, B. P., Wilson, S. J., Luo, L., et al. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127463 · Cited by 5 · see citing works

The contribution of baseline circulating endocannabinoids to individual differences in human pain sensitivity: a quantitative sensory testing study

Fatemi, S. A., Abssy, S. S., Bourke, S. L., Murray, K., Kyeremaa-Adjei, C., Honigman, L., Mohabir, N., Sexton, C. A., Cormie, M. A., Tomin, R., et al. (2025) · Pain · doi:10.1097/j.pain.0000000000003850 · Cited by 3 · see citing works

Targeting G protein coupled receptors for alleviating neuropathic pain

Kumari, P., Yadav, A., Patel, M., & Yadav, P. N. (2022) · Progress in molecular biology and translational science · doi:10.1016/bs.pmbts.2022.06.004 · Cited by 3 · see citing works

Fatty acid amide hydrolase activity in the dorsal periaqueductal gray attenuates neuropathic pain and associated dysautonomia

Woyach, V. L., Sherman, K., Hillard, C. J., Hopp, F. A., Hogan, Q. H., & Dean, C. (2022) · American Journal of Physiology-Regulatory, Integrative and Comparative Physiology · doi:10.1152/ajpregu.00073.2022 · Cited by 1 · see citing works

Premedication and general anesthetic agents decrease plasma concentration of the endocannabinoid anandamide in dogs

Chua, A., McMichael, M., Jukier, T., Arnold, R. D., Hung, W., Harris, S., Zhang, C., & Bustamante, H. (2025) · American Journal of Veterinary Research · doi:10.2460/ajvr.24.11.0366 · Cited by 1 · see citing works

Investigating the role of the endogenous cannabinoid system in emotional modulation of pain: neurochemical and molecular mechanisms

Olango, W. M. (2012) · Arrow@dit (Dublin Institute of Technology) · doi:10.13025/17506 · Cited by 1 · see citing works

Targeted Lipid Biomarker Quantitation Using Liquid Chromatography–Mass Spectrometry (LC–MS)

Salamatipour, A., Blair, I. A., & Mesaros, C. (2017) · Wiley eBooks · doi:10.1002/9781119413073.ch17 · Cited by 1 · see citing works

fatty acid amide hydrolase 3.5.1.99

Schomburg, D., & Schomburg, I. (2013) · Springer eBooks · doi:10.1007/978-3-642-36260-6_10 · Cited by 1 · see citing works

Biochemical Mechanisms of Fatty Liver and Bioactive Foods

Sharma, R. D. (2012) · Elsevier eBooks · doi:10.1016/b978-0-12-397154-8.00041-5

Endocannabinoid turnover (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

Alexander, S. P. H., Doherty, P., Fowler, C. J., Gertsch, J., & van der Stelt, M. (2019) · IUPHAR/BPS Guide to Pharmacology CITE · doi:10.2218/gtopdb/f943/2019.4

Endocannabinoid turnover in GtoPdb v.2021.3

Alexander, S. P. H., Doherty, P., Fowler, C. J., Gertsch, J., & van der Stelt, M. (2021) · IUPHAR/BPS Guide to Pharmacology CITE · doi:10.2218/gtopdb/f943/2021.3

Inactivation Mechanism of the Fatty Acid Amide Hydrolase Inhibitor BIA 10‐2474

Cerqueira, N. M. F. S. A., Neves, M., Rocha, J. F., Silva, P. S., & Palma, P. N. (2022) · ChemBioChem · doi:10.1002/cbic.202200166

Endocannabinoid turnover in GtoPdb v.2023.1

Alexander, S. P. H., Doherty, P., Fowler, C. J., Gertsch, J., & van der Stelt, M. (2023) · IUPHAR/BPS Guide to Pharmacology CITE · doi:10.2218/gtopdb/f943/2023.1

Imaging the endocannabinoid enzyme fatty acid amide hydrolase in the living human brain

Shyu, C., Lora, S., Best, L. M., Bereznick, S., & Boileau, I. (2024) · Elsevier eBooks · doi:10.1016/b978-0-443-19081-0.00004-4

Endocannabinoids in pain modulation

Chapman, V., & Woodhams, S. G. (2025) · Handbook of behavioral neuroscience · doi:10.1016/b978-0-443-13908-6.00010-4

Role of the type-1 cannabinoid receptor in the control of water intake

Zhao, Z. (2019) · theses.fr (ABES) · doi:10.70675/ca103186z8d92z4d94zaf67zcce657f39cd1

BindingDB Entry 50040948: Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites.

BindingDB (2013) · UC San Diego · doi:10.7270/q28s4r30

BindingDB Entry 50032002: A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

BindingDB (2011) · UC San Diego · doi:10.7270/q24q7v5b

BindingDB Entry 50031353: Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.

BindingDB (2010) · UC San Diego · doi:10.7270/q2bv7grn

BindingDB Entry 50047561: The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors.

BindingDB (2017) · UC San Diego · doi:10.7270/q25b04f3

BindingDB Entry 50043910: 1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.

BindingDB (2014) · UC San Diego · doi:10.7270/q2th8p67

BindingDB Entry 50043951: Design, synthesis, and characterization ofa-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase.

BindingDB (2014) · UC San Diego · doi:10.7270/q2hx1f5k

BindingDB Entry 50030892: X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase.

BindingDB (2010) · UC San Diego · doi:10.7270/q2fn168n

BindingDB Entry 50033248: Reversible competitivea-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics.

BindingDB (2011) · UC San Diego · doi:10.7270/q2zk5h08

BindingDB Entry 50040466: Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate.

BindingDB (2013) · UC San Diego · doi:10.7270/q2jq124t

BindingDB Entry 50045245: Discovery libraries targeting the major enzyme classes: the serine hydrolases.

BindingDB (2016) · UC San Diego · doi:10.7270/q2vm4dwq

Novel Mechanistic Class of Fatty Acid Amide Hydrolase Inhibitors with Remarkable Selectivity

Ahn, K., Johnson, D. S., Fitzgerald, L. R., Liimatta, M. B., Arendse, A., Stevenson, T. I., Lund, E. T., Nugent, R. A., Nomanbhoy, T. K., Alexander, J. P., et al. (2007) · Biochemistry · doi:10.1021/bi701378g · Cited by 217 · see citing works

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase

Keith, J. M., Hawryluk, N. A., Apodaca, R. L., Chambers, A., Pierce, J. M., Seierstad, M. J., Palmer, J. A., Webb, M., Karbarz, M. J., Scott, B. P., et al. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.01.064 · Cited by 12 · see citing works

Preclinical Characterization of the FAAH Inhibitor JNJ-42165279

Keith, J. M., Jones, W. M., Tichenor, M. S., Liu, J., Seierstad, M. J., Palmer, J. A., Webb, M., Karbarz, M. J., Scott, B. P., Wilson, S. J., et al. (2015) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.5b00353 · Cited by 64 · see citing works

Novel inhibitors of fatty acid amide hydrolase

Sit, S. Y., Conway, C., Bertekap, R., Xie, K., Bourin, C., Burris, K., & Deng, H. (2007) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2007.04.009 · Cited by 52 · see citing works

A novel inhibitor of fatty acid amide hydrolase, the enzyme responsible for the hydrolysis of the endocannabinoid anandamide

Fowler, C. J., Björklund, E., Congiu, C., & Onnis, V. (2009) · The FASEB Journal · doi:10.1096/fasebj.23.1_supplement.756.15