Cited by 345Cannabis and Cannabinoid ResearchPain Mechanisms and TreatmentsIon Channels and Receptors

The DOI matches its Crossref record; 41 of the 43 references it cites were found in a registry or an index.

Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain

Open access

Kinsey, S.G., Long, J.Z., O’Neal, S.T., Abdullah, R.A., Poklis, J.L., Boger, D.L., Cravatt, B.F., Lichtman, A.H.·2009·The Journal of Pharmacology and Experimental Therapeutics

DOI 10.1124/jpet.109.155465PMC PMC2729802

Open this paper in CoChat — free account Open PDF

Abstract

Direct-acting cannabinoid receptor agonists are well known to reduce hyperalgesic responses and allodynia after nerve injury, although their psychoactive side effects have damped enthusiasm for their therapeutic development. Alternatively, inhibiting fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), the principal enzymes responsible for the degradation of the respective endogenous cannabinoids, anandamide (AEA) and 2-arachydonylglycerol (2-AG), reduce nociception in a variety of nociceptive assays, with no or minimal behavioral effects. In the present study we tested whether inhibition of these enzymes attenuates mechanical allodynia, and acetone-induced cold allodynia in mice subjected to chronic constriction injury of the sciatic nerve. Acute administration of the irreversible FAAH inhibitor, cyclohexylcarbamic acid 3'-carbamoylbiphenyl-3-yl ester (URB597), or the reversible FAAH inhibitor, 1-oxo-1-[5-(2-pyridyl)-2-yl]-7-phenylheptane (OL-135), decreased allodynia in both tests. This attenuation was completely blocked by pretreatment with either CB(1) or CB(2) receptor antagonists, but not by the TRPV1 receptor antagonist, capsazepine, or the opioid receptor antagonist, naltrexone. The novel MAGL inhibitor, 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) also attenuated mechanical and cold allodynia via a CB(1), but not a CB(2), receptor mechanism of action. Whereas URB597 did not elicit antiallodynic effects in FAAH(-/-) mice, the effects of JZL184 were FAAH-independent. Finally, URB597 increased brain and spinal cord AEA levels, whereas JZL184 increased 2-AG levels in these tissues, but no differences in either endo-cannabinoid were found between nerve-injured and control mice. These data indicate that inhibition of FAAH and MAGL reduces neuropathic pain through distinct receptor mechanisms of action and present viable targets for the development of analgesic therapeutics.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1124/jpet.109.155465

Cites

41 of 41 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Quantitative assessment of tactile allodynia in the rat paw
Chaplan, S. R., Bach, F. W., Pogrel, J. W., Chung, J. M., & Yaksh, T. L. (1994) · Journal of Neuroscience Methods · doi:10.1016/0165-0270(94)90144-9 · Cited by 7,740
Isolation and Structure of a Brain Constituent That Binds to the Cannabinoid Receptor
Devane, W. A., Hanuš, L., Breuer, A., Pertwee, R. G., Stevenson, L. A., Griffin, G., Gibson, D., Mandelbaum, A., Etinger, A., & Mechoulam, R. (1992) · Science · doi:10.1126/science.1470919 · Cited by 5,633
Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors
Mechoulam, R., Ben-Shabat, S., Hanus, L., Ligumsky, M., Kaminski, N. E., Schatz, A. R., Gopher, A., Almog, S., Martin, B. R., Compton, D. R., et al. (1995) · Biochemical Pharmacology · doi:10.1016/0006-2952(95)00109-d · Cited by 2,913
Spared nerve injury: an animal model of persistent peripheral neuropathic pain
Décosterd, I., & Woolf, C. J. (2000) · Pain · doi:10.1016/s0304-3959(00)00276-1 · Cited by 2,317
Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides
Cravatt, B. F., Giang, D. K., Mayfield, S. P., Boger, D. L., Lerner, R. A., & Gilula, N. B. (1996) · Nature · doi:10.1038/384083a0 · Cited by 2,125
Self-citation
Expression of Central and Peripheral Cannabinoid Receptors in Human Immune Tissues and Leukocyte Subpopulations
Galiègue, S., Mary, S., Marchand, J., Dussossoy, D., Carrière, D., Carayon, P., Bouaboula, M., Shire, D. J., Fur, G. L., & Casellas, P. (1995) · European Journal of Biochemistry · doi:10.1111/j.1432-1033.1995.tb20780.x · Cited by 1,776
Identification and Functional Characterization of Brainstem Cannabinoid CB2Receptors
Van Sickle, M. D., Duncan, M., Kingsley, P. J., Mouihate, A., Urbani, P., Mackie, K., Stella, N., Makriyannis, A., Piomelli, D., Davison, J. S., et al. (2005) · Science · doi:10.1126/science.1115740 · Cited by 1,470
Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase
Cravatt, B. F., Demarest, K., Patricelli, M. P., Bracey, M. H., Giang, D. K., Martin, B. R., & Lichtman, A. H. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.161191698 · Cited by 1,310
Self-citation
Modulation of anxiety through blockade of anandamide hydrolysis
Kathuria, S., Gaetani, S., Fegley, D., Valiño, F., Duranti, A., Tontini, A., Mor, M., Tarzia, G., Rana, G. L., Calignano, A., et al. (2003) · Nature Medicine · doi:10.1038/nm803 · Cited by 1,293
Interleukin-1β-mediated induction of Cox-2 in the CNS contributes to inflammatory pain hypersensitivity
Samad, T. A., Moore, K. A., Sapirstein, A., Billet, S. E., Allchorne, A. J., Poole, S., Bonventre, J. V., & Woolf, C. J. (2001) · Nature · doi:10.1038/35068566 · Cited by 1,282

Flagged first, then by citations

Show all 43 references

2 of the 43 references couldn’t be matched to a known paper.

Sorted by citations

Items 101–200 of 345

Diacylglycerol lipase β inhibition reverses nociceptive behaviour in mouse models of inflammatory and neuropathic pain
Wilkerson, J. L., Ghosh, S., Bağdaş, D., Mason, B. L., Crowe, M. S., Hsu, K., Wise, L. E., Kinsey, S. G., Damaj, M. I., Cravatt, B. F., et al. (2016) · British Journal of Pharmacology · doi:10.1111/bph.13469 · Cited by 57
Self-citation
Spinal administration of the monoacylglycerol lipase inhibitor JZL 184 produces robust inhibitory effects on nociceptive processing and the development of central sensitization in the rat
Woodhams, S. G., Wong, A., Barrett, D. A., Bennett, A. J., Chapman, V., & Alexander, S. (2012) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2012.02179.x · Cited by 55
Full Fatty Acid Amide Hydrolase Inhibition Combined with Partial Monoacylglycerol Lipase Inhibition: Augmented and Sustained Antinociceptive Effects with Reduced Cannabimimetic Side Effects in Mice
Ghosh, S., Kinsey, S. G., Liu, Q.-S., Hruba, L., McMahon, L. R., Grim, T. W., Merritt, C. R., Wise, L. E., Abdullah, R. A., Selley, D. E., et al. (2015) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.115.222851 · Cited by 54
Self-citation
Inhibitors of monoacylglycerol lipase, fatty-acid amide hydrolase and endocannabinoid transport differentially suppress capsaicin-induced behavioral sensitization through peripheral endocannabinoid mechanisms
Spradley, J. M., Guindon, J., & Hohmann, A. G. (2010) · Pharmacological Research · doi:10.1016/j.phrs.2010.03.007 · Cited by 54
X-ray Crystallographic Analysis of α-Ketoheterocycle Inhibitors Bound to a Humanized Variant of Fatty Acid Amide Hydrolase
Mileni, M., Garfunkle, J., Ezzili, C., Kimball, F. S., Cravatt, B. F., Stevens, R. C., & Boger, D. L. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm9012196 · Cited by 52
Self-citation
A pro-nociceptive phenotype unmasked in mice lacking fatty-acid amide hydrolase
Carey, L. M., Slivicki, R. A., Leishman, E., Cornett, B., Mackie, K., Bradshaw, H. B., & Hohmann, A. G. (2016) · Molecular Pain · doi:10.1177/1744806916649192 · Cited by 53
Targeting Peripherally Restricted Cannabinoid Receptor 1, Cannabinoid Receptor 2, and Endocannabinoid-Degrading Enzymes for the Treatment of Neuropathic Pain Including Neuropathic Orofacial Pain
Hossain, M. Z., Ando, H., Unno, S., & Kitagawa, J. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21041423 · Cited by 54
Immunofluorescent spectral analysis reveals the intrathecal cannabinoid agonist, AM1241, produces spinal anti‐inflammatory cytokine responses in neuropathic rats exhibiting relief from allodynia
Wilkerson, J. L., Gentry, K. R., Dengler, E. C., Wallace, J. A., Kerwin, A. A., Kuhn, M. N., Zvonok, A. M., Thakur, G. A., Makriyannis, A., & Milligan, E. D. (2012) · Brain and Behavior · doi:10.1002/brb3.44 · Cited by 51
Endocannabinoids decrease neuropathic pain-related behavior in mice through the activation of one or both peripheral CB1 and CB2 receptors
Desroches, J., Charron, S., Bouchard, J., & Beaulieu, P. (2013) · Neuropharmacology · doi:10.1016/j.neuropharm.2013.10.006 · Cited by 51
Dual-Acting Compounds Targeting Endocannabinoid and Endovanilloid Systems—A Novel Treatment Option for Chronic Pain Management
Małek, N., & Starowicz, K. (2016) · Frontiers in Pharmacology · doi:10.3389/fphar.2016.00257 · Cited by 51
Combined inhibition of FAAH and COX produces enhanced anti-allodynic effects in mouse neuropathic and inflammatory pain models
Grim, T. W., Ghosh, S., Hsu, K.-L., Cravatt, B. F., Kinsey, S. G., & Lichtman, A. H. (2014) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2014.07.008 · Cited by 50
Self-citation
JZL184 is anti-hyperalgesic in a murine model of cisplatin-induced peripheral neuropathy
Khasabova, I. A., Yao, X., Paz, J., Lewandowski, C. T., Lindberg, A. E., Coicou, L., Burlakova, N., Simone, D. A., & Seybold, V. S. (2014) · Pharmacological Research · doi:10.1016/j.phrs.2014.09.008 · Cited by 50
Cannabinoid receptors and pain
Starowicz, K., Małek, N., & Przewłocka, B. (2013) · Wiley Interdisciplinary Reviews Membrane Transport and Signalling · doi:10.1002/wmts.83 · Cited by 50
Inhibitors of the Endocannabinoid-Degrading Enzymes, or how to Increase Endocannabinoids Activity by Preventing their Hydrolysis
Feledziak, M., Lambert, D. M., Marchand‐Brynaert, J., & Muccioli, G. G. (2011) · Recent Patents on CNS Drug Discovery · doi:10.2174/157488912798842223 · Cited by 50
Palmitoylethanolamide Reverses Paclitaxel-Induced Allodynia in Mice
Donvito, G., Wilkerson, J. L., Damaj, M. I., & Lichtman, A. H. (2016) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.116.236182 · Cited by 50
Self-citation
Reversible Competitive α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Containing Additional Conformational Constraints in the Acyl Side Chain: Orally Active, Long-Acting Analgesics
Ezzili, C., Mileni, M., McGlinchey, N., Long, J. Z., Kinsey, S. G., Hochstatter, D. G., Stevens, R. C., Lichtman, A. H., Cravatt, B. F., Bilsky, E. J., et al. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm101597x · Cited by 49
Self-citation
Sex differences in the expression of the endocannabinoid system within V1M cortex and PAG of Sprague Dawley rats
Levine, A. A., Liktor‐Busa, E., Lipinski, A. A., Couture, S. A., Balasubramanian, S., Aicher, S. A., Langlais, P. R., Vanderah, T. W., & Largent‐Milnes, T. M. (2021) · Biology of Sex Differences · doi:10.1186/s13293-021-00402-2 · Cited by 53
Lipases and their inhibitors in health and disease
Nomura, D. K., & Casida, J. E. (2016) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2016.04.004 · Cited by 50
The dynamic interaction between pain and opioid misuse
Wilson‐Poe, A. R., & Morón, J. A. (2017) · British Journal of Pharmacology · doi:10.1111/bph.13873 · Cited by 49
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors
Gustin, D. J., Ma, Z., Min, X., Li, Y., Hedberg, C., Guimarães, C. R. W., Porter, A. C., Lindström, M., Lester-Zeiner, D., Xu, G., et al. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.02.052 · Cited by 49
The effect of FAAH , MAGL , and Dual FAAH / MAGL inhibition on inflammatory and colorectal distension‐induced visceral pain models in Rodents
Sakın, Y. S., Dogrul, A. B., İlkaya, F., Seyrek, M., Ulaş, Ü. H., Gülşen, M., & Bagci, S. (2015) · Neurogastroenterology & Motility · doi:10.1111/nmo.12563 · Cited by 47
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 46
Combined inhibition of monoacylglycerol lipase and cyclooxygenases synergistically reduces neuropathic pain in mice
Crowe, M. S., Leishman, E., Banks, M. L., Gujjar, R., Mahadevan, A., Bradshaw, H. B., & Kinsey, S. G. (2014) · British Journal of Pharmacology · doi:10.1111/bph.13012 · Cited by 45
Self-citation
The dual FAAH/MAGL inhibitor JZL195 has enhanced effects on endocannabinoid transmission and motor behavior in rats as compared to those of the MAGL inhibitor JZL184
Seillier, A., Aguilar, D. D., & Giuffrida, A. (2014) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2014.05.022 · Cited by 45
An Endocannabinoid Uptake Inhibitor from Black Pepper Exerts Pronounced Anti-Inflammatory Effects in Mice
Reynoso-Moreno, I., Najar-Guerrero, I., Escareño, N., Flores-Soto, M. E., Gertsch, J., & Paredes, J. M. V. (2017) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.7b02979 · Cited by 48
An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present)
Bononi, G., Poli, G., Rizzolio, F., Tuccinardi, T., Macchia, M., Minutolo, F., & Granchi, C. (2020) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2021.1841166 · Cited by 45
Prolonged monoacylglycerol lipase blockade causes equivalent cannabinoid receptor type 1 receptor-mediated adaptations in fatty acid amide hydrolase wild-type and knockout mice
Schlosburg, J. E., Kinsey, S. G., Ignatowska-Jankowska, B., Ramesh, D., Abdullah, R. A., Tao, Q., Booker, L., Long, J. Z., Selley, D. E., Cravatt, B. F., et al. (2014) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.114.212753 · Cited by 44
Self-citation
Effects of Alterations in Cannabinoid Signaling, Alone and in Combination with Morphine, on Pain-Elicited and Pain-Suppressed Behavior in Mice
Miller, L. L., Picker, M. J., Umberger, M. D., Schmidt, K. T., & Dykstra, L. A. (2012) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.112.191478 · Cited by 44
Mechanism of platelet activation induced by endocannabinoids in blood and plasma
Brantl, S. A., Khandoga, A. L., & Siess, W. (2013) · Platelets · doi:10.3109/09537104.2013.803530 · Cited by 44
Characterization of Sigma 1 Receptor Antagonist CM-304 and Its Analog, AZ-66: Novel Therapeutics Against Allodynia and Induced Pain
Cirino, T. J., Eans, S. O., Medina, J. M., Wilson, L., Mottinelli, M., Intagliata, S., McCurdy, C. R., & McLaughlin, J. P. (2019) · Frontiers in Pharmacology · doi:10.3389/fphar.2019.00678 · Cited by 43
WWL70 protects against chronic constriction injury-induced neuropathic pain in mice by cannabinoid receptor-independent mechanisms
Wen, J., Jones, M., Tanaka, M., Selvaraj, P., Symes, A. J., Cox, B. M., & Zhang, Y. (2018) · Journal of Neuroinflammation · doi:10.1186/s12974-017-1045-9 · Cited by 43
Targeting the endocannabinoid system: a predictive, preventive, and personalized medicine-directed approach to the management of brain pathologies
Reddy, V. P., Grogan, D. P., Ahluwalia, M., Salles, É. L., Ahluwalia, P. K., Khodadadi, H., Alverson, K., Nguyen, A., Raju, S. P., Gaur, P., et al. (2020) · The EPMA Journal · doi:10.1007/s13167-020-00203-4 · Cited by 45
Attenuation of persistent pain-related behavior by fatty acid amide hydrolase (FAAH) inhibitors in a rat model of HIV sensory neuropathy
Nasirinezhad, F., Jergová, S., Pearson, J. P., & Sagen, J. (2014) · Neuropharmacology · doi:10.1016/j.neuropharm.2014.11.024 · Cited by 41
α9-Nicotinic Acetylcholine Receptors Contribute to the Maintenance of Chronic Mechanical Hyperalgesia, but Not Thermal or Mechanical Allodynia
Mohammadi, S. A., & Christie, M. J. (2014) · Molecular Pain · doi:10.1186/1744-8069-10-64 · Cited by 40
Fatty Acid Amide Hydrolase (FAAH) Inhibition Reduces l-3,4-Dihydroxyphenylalanine-Induced Hyperactivity in the 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Lesioned Non-Human Primate Model of Parkinson’s Disease
Johnston, T. H., Huot, P., Fox, S. H., WAKEFIELD, J. D., Sykes, K. A., Bartolini, W. P., Milne, G. T., Pearson, J. P., & Brotchie, J. M. (2010) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.110.169532 · Cited by 40
Non-psychotropic analgesic drugs from the endocannabinoid system: “Magic bullet” or “multiple-target” strategies?
Starowicz, K., & Marzo, V. D. (2013) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2013.01.075 · Cited by 39
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors
Afzal, O., Kumar, S., Kumar, R., Firoz, A., Jaggi, M., & Bawa, S. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.06.029 · Cited by 38
CB2 receptor deletion on myeloid cells enhanced mechanical allodynia in a mouse model of neuropathic pain
Nent, E., Nozaki, C., Schmöle, A., Otte, D. M., & Zimmer, A. (2019) · Scientific Reports · doi:10.1038/s41598-019-43858-4 · Cited by 37
Effects of COX-2 inhibition on spinal nociception: the role of endocannabinoids.
Staniaszek, L., Norris, L., Kendall, D., Barrett, D., & Chapman, V (2010) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2010.00703.x · Cited by 36
Endocannabinoid Overload
Lichtman, A. H., Blankman, J. L., & Cravatt, B. F. (2010) · Molecular Pharmacology · doi:10.1124/mol.110.069427 · Cited by 37
Self-citation
Fluoride-Mediated Capture of a Noncovalent Bound State of a Reversible Covalent Enzyme Inhibitor: X-ray Crystallographic Analysis of an Exceptionally Potent α-Ketoheterocycle Inhibitor of Fatty Acid Amide Hydrolase
Mileni, M., Garfunkle, J., Ezzili, C., Cravatt, B. F., Stevens, R. C., & Boger, D. L. (2011) · Journal of the American Chemical Society · doi:10.1021/ja110877y · Cited by 35
Self-citation
Activity-based proteomic and metabolomic approaches for understanding metabolism
Hunerdosse, D. M., & Nomura, D. K. (2014) · Current Opinion in Biotechnology · doi:10.1016/j.copbio.2014.02.001 · Cited by 35
Distinct Activity of Endocannabinoid-Hydrolyzing Enzymes MAGL and FAAH in Key Regions of Peripheral and Central Nervous System Implicated in Migraine
Pietra, A. D., Giniatullin, R. A., & Savinainen, J. R. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22031204 · Cited by 36
α-Ketoheterocycle-Based Inhibitors of Fatty Acid Amide Hydrolase (FAAH)
Otrubova, K., & Boger, D. L. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn2001206 · Cited by 35
Self-citation
Therapeutical Potential of CB2 Receptors in Immune-Related Diseases
Leleu‐Chavain, N., Desreumaux, P., Chavatte, P., & Millet, R. (2014) · Current Molecular Pharmacology · doi:10.2174/1874467207666140219122337 · Cited by 37
Inhibition of Fatty Acid Amide Hydrolase Improves Depressive-Like Behaviors Independent of Its Peripheral Antinociceptive Effects in a Rat Model of Neuropathic Pain
Jiang, H., Ke, B., Liu, J., Ma, G., Hai, K., Gong, D., Yang, Z., & Zhou, C. (2018) · Anesthesia & Analgesia · doi:10.1213/ane.0000000000003563 · Cited by 35
Cannabinoids modulate spontaneous synaptic activity in retinal ganglion cells
Middleton, T. P., & Protti, D. A. (2011) · Visual Neuroscience · doi:10.1017/s0952523811000198 · Cited by 34
Hemopressin, an inverse agonist of cannabinoid receptors, inhibits neuropathic pain in rats
Toniolo, E. F., Maique, E. T., Ferreira, W. A., Heimann, A. S., Ferro, E. S., Ramos‐Ortolaza, D. L., Miller, L. K., Devi, L. A., & Dale, C. S. (2014) · Peptides · doi:10.1016/j.peptides.2014.03.016 · Cited by 34
Structure–Activity Relationship of a New Series of Reversible Dual Monoacylglycerol Lipase/Fatty Acid Amide Hydrolase Inhibitors
Cisneros, J. A., Björklund, E., González-Gil, I., Hu, Y., Canales, Á., Medrano, F. J., Romero, A., Ortega‐Gutiérrez, S., Fowler, C. J., & López-Rodríguez, M. L. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm201327p · Cited by 33
WWL70 attenuates PGE2 production derived from 2-arachidonoylglycerol in microglia by ABHD6-independent mechanism
Tanaka, M., Moran, S., Wen, J., Affram, K. O., Chen, T., Symes, A. J., & Zhang, Y. (2017) · Journal of Neuroinflammation · doi:10.1186/s12974-016-0783-4 · Cited by 35
Rational Design of Fatty Acid Amide Hydrolase Inhibitors That Act by Covalently Bonding to Two Active Site Residues
Otrubova, K., Brown, M. A., McCormick, M. S., Han, G. W., O’Neal, S. T., Cravatt, B. F., Stevens, R. C., Lichtman, A. H., & Boger, D. L. (2013) · Journal of the American Chemical Society · doi:10.1021/ja4014997 · Cited by 32
Self-citation
Synthesis and preclinical evaluation of [11C-carbonyl]PF-04457845 for neuroimaging of fatty acid amide hydrolase
Hicks, J. W., Parkes, J., Sadovski, O., Tong, J., Houle, S., Vasdev, N., & Wilson, A. A. (2013) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2013.04.008 · Cited by 35
Design of Benzoxathiazin-3-one 1,1-Dioxides as a New Class of Irreversible Serine Hydrolase Inhibitors: Discovery of a Uniquely Selective PNPLA4 Inhibitor
Kornahrens, A. F., Cognetta, A. B., Brody, D. M., Matthews, M. L., Cravatt, B. F., & Boger, D. L. (2017) · Journal of the American Chemical Society · doi:10.1021/jacs.7b02985 · Cited by 32
Self-citation
Brain permeant and impermeant inhibitors of fatty-acid amide hydrolase suppress the development and maintenance of paclitaxel-induced neuropathic pain without producing tolerance or physical dependence in vivo and synergize with paclitaxel to reduce tumor cell line viability in vitro
Slivicki, R. A., Xu, Z., Mali, S. S., & Hohmann, A. G. (2019) · Pharmacological Research · doi:10.1016/j.phrs.2019.02.002 · Cited by 31
Therapeutic Effect of Tetrapanax papyriferus and Hederagenin on Chronic Neuropathic Pain of Chronic Constriction Injury of Sciatic Nerve Rats Based on KEGG Pathway Prediction and Experimental Verification
Zhang, D., Sun, J., Yang, B. Y., Ma, S., Zhang, C., & Zhao, G. (2020) · Evidence-based Complementary and Alternative Medicine · doi:10.1155/2020/2545806 · Cited by 31
Anandamide deficiency and heightened neuropathic pain in aged mice
Bishay, P., Häußler, A., Lim, H., Oertel, B. G., Galve‐Roperh, I., Ferreirós, N., & Tegeder, I. (2013) · Neuropharmacology · doi:10.1016/j.neuropharm.2013.03.021 · Cited by 33
Investigation of Diacylglycerol Lipase Alpha Inhibition in the Mouse Lipopolysaccharide Inflammatory Pain Model
Wilkerson, J. L., Donvito, G., Grim, T. W., Abdullah, R. A., Ogasawara, D., Cravatt, B. F., & Lichtman, A. H. (2017) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.117.243808 · Cited by 30
Self-citation
Increased tonic cannabinoid CB1R activity and brain region-specific desensitization of CB1R Gi/o signaling axis in mice with global genetic knockout of monoacylglycerol lipase
Navia‐Paldanius, D., Aaltonen, N., Lehtonen, M., Savinainen, J. R., Taschler, U., Radner, F. P. W., Zimmermann, R., & Laitinen, J. T. (2015) · European Journal of Pharmaceutical Sciences · doi:10.1016/j.ejps.2015.06.005 · Cited by 30
Peripheral Effects of FAAH Deficiency on Fuel and Energy Homeostasis: Role of Dysregulated Lysine Acetylation
Vaitheesvaran, B., Yang, L., Hartil, K., Glaser, S. T., Yazulla, S., Bruce, J. E., & Kurland, I. J. (2012) · PLoS ONE · doi:10.1371/journal.pone.0033717 · Cited by 29
Beyond the Direct Activation of Cannabinoid Receptors: New Strategies to Modulate the Endocannabinoid System in CNS-Related Diseases
Chicca, A., Arena, C., & Manera, C. (2016) · Recent Patents on CNS Drug Discovery · doi:10.2174/1574889810999160603185126 · Cited by 29
Peripheral deficiency and antiallodynic effects of 2-arachidonoyl glycerol in a mouse model of paclitaxel-induced neuropathic pain
Thomas, A., Okine, B. N., Finn, D. P., & Masocha, W. (2020) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2020.110456 · Cited by 32
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 29
Self-citation
The multiplicity of spinal AA-5-HT anti-nociceptive action in a rat model of neuropathic pain
Małek, N., Kostrzewa, M., Makuch, W., Pajak, A., Kucharczyk, M. W., Piscitelli, F., Przewłocka, B., Marzo, V. D., & Starowicz, K. (2016) · Pharmacological Research · doi:10.1016/j.phrs.2016.06.012 · Cited by 28
The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice
Donvito, G., Bağdaş, D., Toma, W. B., Rahimpour, E., Jackson, A. B., Meade, J. A., AlSharari, S. D., Kulkarni, A., Carroll, F. I., Lichtman, A. H., et al. (2017) · Experimental Neurology · doi:10.1016/j.expneurol.2017.06.014 · Cited by 28
Self-citation
Targeting the endogenous cannabinoid system to treat neuropathic pain
Lau, B. K., & Vaughan, C. W. (2014) · Frontiers in Pharmacology · doi:10.3389/fphar.2014.00028 · Cited by 27
N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases
Otrubova, K., Chatterjee, S., Ghimire, S., Cravatt, B. F., & Boger, D. L. (2019) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2019.03.020 · Cited by 28
Self-citation
Increased anandamide uptake by sensory neurons contributes to hyperalgesia in a model of cancer pain
Khasabova, I. A., Holman, M. A., Morse, T., Burlakova, N., Coicou, L. G., Harding-Rose, C., Simone, D. A., & Seybold, V. S. (2013) · Neurobiology of Disease · doi:10.1016/j.nbd.2013.04.018 · Cited by 26
Evaluation of different drug classes on transient sciatic nerve injury–depressed marble burying in mice
Wilkerson, J. L., Curry, Z. A., Kinlow, P. D., Mason, B. L., Hsu, K., van der Stelt, M., Cravatt, B. F., & Lichtman, A. H. (2018) · Pain · doi:10.1097/j.pain.0000000000001199 · Cited by 27
Self-citation
Cannabinoid subtype-2 receptors modulate the antihyperalgesic effect of WIN 55,212-2 in rats with neuropathic spinal cord injury pain
Ahmed, M. M., Rajpal, S., Sweeney, C., Gerovac, T. A., Allcock, B., McChesney, S. L., Patel, A. U., Tilghman, J. I., Miranpuri, G. S., & Resnick, D. K. (2010) · The Spine Journal · doi:10.1016/j.spinee.2010.08.015 · Cited by 26
Comparative studies of endocannabinoid modulation of pain
Paulsen, R. T., & Burrell, B. D. (2019) · Philosophical Transactions of the Royal Society B Biological Sciences · doi:10.1098/rstb.2019.0279 · Cited by 26
Analgesic effects of FAAH inhibitor in the insular cortex of nerve-injured rats
Kim, M. J., Tanioka, M., Um, S. W., Hong, S., & Lee, B. H. (2018) · Molecular Pain · doi:10.1177/1744806918814345 · Cited by 25
CB1 positive allosteric modulation attenuates Δ9-THC withdrawal and NSAID-induced gastric inflammation
Trexler, K. R., Eckard, M. L., & Kinsey, S. G. (2018) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2018.12.009 · Cited by 25
Self-citation
Simultaneous Inhibition of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase Shares Discriminative Stimulus Effects with Δ9-Tetrahydrocannabinol in Mice
Hrubá, L., Seillier, A., Zaki, A., Cravatt, B. F., Lichtman, A. H., Giuffrida, A., & McMahon, L. R. (2015) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.115.222836 · Cited by 24
Self-citation
The inhibition by di(2-ethylhexyl)-phthalate of erg-mediated K+ current in pituitary tumor (GH3) cells
Wu, S., Yang, W.-H., Yeh, C.-C., & Huang, H.-C. (2012) · Archives of Toxicology · doi:10.1007/s00204-012-0805-7 · Cited by 24
Exploring Metabolic Pathways and Regulation through Functional Chemoproteomic and Metabolomic Platforms
Medina-Cleghorn, D., & Nomura, D. K. (2014) · Chemistry & Biology · doi:10.1016/j.chembiol.2014.07.007 · Cited by 25
Inhibition of monoacylglycerol lipase by troglitazone,N‐arachidonoyl dopamine and the irreversible inhibitor JZL184: comparison of two different assays
Björklund, E., Norén, E., Nilsson, J., & Fowler, C. (2010) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2010.00974.x · Cited by 23
Intrathecal morphine administration reduces postoperative pain and peripheral endocannabinoid levels in total knee arthroplasty patients: a randomized clinical trial
Kaczocha, M., Azim, S., Nicholson, J., Rebecchi, M. J., Lu, Y., Feng, T., Romeiser, J. L., Reinsel, R. A., Rizwan, S., Shodhan, S., et al. (2018) · BMC Anesthesiology · doi:10.1186/s12871-018-0489-5 · Cited by 23
Potential of Endocannabinoids to Control Bladder Pain
Bjorling, D. E., & Wang, Z.-Y. (2018) · Frontiers in Systems Neuroscience · doi:10.3389/fnsys.2018.00017 · Cited by 24
Pharmacological blockade of 2-AG degradation ameliorates clinical, neuroinflammatory and synaptic alterations in experimental autoimmune encephalomyelitis
Guadalupi, L., Mandolesi, G., Vanni, V., Balletta, S., Caioli, S., Pavlovic, A., De Vito, F., Fresegna, D., Sanna, K., Vitiello, L., et al. (2024) · Neuropharmacology · doi:10.1016/j.neuropharm.2024.109940 · Cited by 22
Attenuation of serotonin-induced itch responses by inhibition of endocannabinoid degradative enzymes, fatty acid amide hydrolase and monoacylglycerol lipase
Tosun, N. C., Gündüz, Ö., & Ulugöl, A. (2014) · Journal of Neural Transmission · doi:10.1007/s00702-014-1251-x · Cited by 22
Combination Drug Therapy for Pain following Chronic Spinal Cord Injury
Hama, A. T., & Sagen, J. (2012) · Pain Research and Treatment · doi:10.1155/2012/840486 · Cited by 22
Analgesic Drugs Combinations in the Treatment of Different Types of Pain
Ortiz, M. I., Molina, M. A. R., Arai, Y.-C. P., & Romanò, C. L. (2012) · Pain Research and Treatment · doi:10.1155/2012/612519 · Cited by 22
Differential Tolerance to FTY720-Induced Antinociception in Acute Thermal and Nerve Injury Mouse Pain Models: Role of Sphingosine-1-Phosphate Receptor Adaptation
Sim‐Selley, L. J., Wilkerson, J. L., Burston, J. J., Hauser, K. F., McLane, V. D., Welch, S. P., Lichtman, A. H., & Selley, D. E. (2018) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.118.248260 · Cited by 21
Self-citation
Inhibition of Monoacylglycerol Lipase Reduces the Reinstatement of Methamphetamine-Seeking and Anxiety-Like Behaviors in Methamphetamine Self-Administered Rats
Nawata, Y., Yamaguchi, T., Fukumori, R., & Yamamoto, T. (2018) · The International Journal of Neuropsychopharmacology · doi:10.1093/ijnp/pyy086 · Cited by 21
Monoacylglycerol Lipase Inhibition Using JZL184 Attenuates Paw Inflammation and Functional Deficits in a Mouse Model of Inflammatory Arthritis
Nass, S. R., Steele, F. F., Ware, T. B., Libby, A. H., Hsu, K., & Kinsey, S. G. (2021) · Cannabis and Cannabinoid Research · doi:10.1089/can.2020.0177 · Cited by 20
Self-citation
Attenuation of anticipatory nausea in a rat model of contextually elicited conditioned gaping by enhancement of the endocannabinoid system
Limebeer, C. L., Abdullah, R. A., Rock, E. M., Imhof, E., Wang, K., Lichtman, A. H., & Parker, L. A. (2013) · Psychopharmacology · doi:10.1007/s00213-013-3282-7 · Cited by 21
Self-citation
The monoacylglycerol lipase inhibitor KML29 with gabapentin synergistically produces analgesia in mice
Crowe, M. S., Wilson, C. D., Leishman, E., Prather, P. L., Bradshaw, H. B., Banks, M. L., & Kinsey, S. G. (2017) · British Journal of Pharmacology · doi:10.1111/bph.14055 · Cited by 20
Self-citation
Endocannabinoid-mediated potentiation of nonnociceptive synapses contributes to behavioral sensitization
Wang, Y., & Burrell, B. D. (2017) · Journal of Neurophysiology · doi:10.1152/jn.00092.2017 · Cited by 20
Untapped endocannabinoid pharmacological targets: Pipe dream or pipeline?
Wilkerson, J. L., Bilbrey, J. A., Felix, J. S., Makriyannis, A., & McMahon, L. R. (2021) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2021.173192 · Cited by 20
The Central Role of Glia in Pathological Pain and the Potential of Targeting the Cannabinoid 2 Receptor for Pain Relief
Wilkerson, J. L., & Milligan, E. D. (2011) · ISRN Anesthesiology · doi:10.5402/2011/593894 · Cited by 20
2‐Arachidonoylglycerol ‐mediated endocannabinoid signaling modulates mechanical hypersensitivity associated with alcohol withdrawal in mice
Morgan, A., Adank, D. N., Johnson, K., Butler, E. C., & Patel, S. (2022) · Alcoholism Clinical and Experimental Research · doi:10.1111/acer.14949 · Cited by 20
Alterations in the Anandamide Metabolism in the Development of Neuropathic Pain
Małek, N., Kucharczyk, M. W., & Starowicz, K. (2014) · BioMed Research International · doi:10.1155/2014/686908 · Cited by 19
The endocannabinoid system: Novel targets for treating cancer induced bone pain
Sun, J., Zhou, Y., Chen, S., Wang, X., Xu, B., Li, D., Tian, Y., & Ye, D. (2019) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2019.109504 · Cited by 19
Druggable targets of the endocannabinoid system: Implications for the treatment of HIV-associated neurocognitive disorder
Wu, M. M., Zhang, X., Asher, M. J., & Thayer, S. A. (2019) · Brain Research · doi:10.1016/j.brainres.2019.146467 · Cited by 19
Inhibiting Endocannabinoid Hydrolysis as Emerging Analgesic Strategy Targeting a Spectrum of Ion Channels Implicated in Migraine Pain
Pietra, A. D., Savinainen, J. R., & Giniatullin, R. A. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23084407 · Cited by 19
The endocannabinoid system as a therapeutic target in neuropathic pain: a review
Quintero, J.-M., Díaz, L. E., Galve‐Roperh, I., Bustos, R., Leon, M.-X., Beltran, S., & Dodd, S. (2024) · Expert Opinion on Therapeutic Targets · doi:10.1080/14728222.2024.2407824 · Cited by 18
Heterogeneous presynaptic distribution of monoacylglycerol lipase, a multipotent regulator of nociceptive circuits in the mouse spinal cord
Horváth, E., Woodhams, S. G., Nyilas, R., Henstridge, C. M., Kano, M., Sakimura, K., Watanabe, M., & Katona, I. (2014) · European Journal of Neuroscience · doi:10.1111/ejn.12470 · Cited by 18
MAGL inhibition modulates gastric secretion and motility following NSAID exposure in mice
Crowe, M. S., & Kinsey, S. G. (2017) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2017.05.006 · Cited by 18
Self-citation
Conformational gating, dynamics and allostery in human monoacylglycerol lipase
Tyukhtenko, S. I., Ma, X., Rajarshi, G., Karageorgos, I. L., Anderson, K. W., Hudgens, J. W., Guo, J. J., Nasr, M. L., Zvonok, N., Vemuri, K. V., et al. (2020) · Scientific Reports · doi:10.1038/s41598-020-75497-5 · Cited by 20
Analgesic and Anticancer Activity of Benzoxazole Clubbed 2-Pyrrolidinones as Novel Inhibitors of Monoacylglycerol Lipase
Afzal, O., Altamimi, A. S. A., Shahroz, M. M., Sharma, H. K., Riadi, Y., & Hassan, M. Q. (2021) · Molecules · doi:10.3390/molecules26082389 · Cited by 18

Authors: Kinsey, S. G., Long, J. Z., O’Neal, S. T., Abdullah, R. A., Poklis, J. L., Boger, D. L., Cravatt, B. F., & Lichtman, A. H.
Affiliations: Virginia Commonwealth University (US)
Scripps Research Institute (US)
ORCID: Kinsey, S.G.
Long, J.Z.
O’Neal, S.T.
Poklis, J.L.
Boger, D.L.
Lichtman, A.H.
Venue: The Journal of Pharmacology and Experimental Therapeutics
Publisher: Elsevier BV
Published: 2009-09
Volume: 330
Issue: 3
Pages: 902-910
ISSN: 0022-3565 (ISSN-L)
DOI: 10.1124/jpet.109.155465
PMC: PMC2729802
OpenAlex: W2132380973
Cited by: 330
References: 43
Citations by year: 2026: 9 · 2025: 14 · 2024: 13 · 2023: 8 · 2022: 7 · 2021: 15 · 2020: 9 · 2019: 14 · 2018: 21 · 2017: 24 · 2016: 16 · 2015: 21 · 2014: 35 · 2013: 29 · 2012: 33
FWCI: 24.43
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: Institute of International Education
National Institute on Drug Abuse (DA015197, P01DA009789, DA-017259, R01DA015197, DA009789-11, DA007027-32, P01DA017259, DA 009789, DA015648, T32DA007027, DA007027)
Topics: Health Sciences › Medicine › Pharmacology (medical) › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Physiology (medical) › Pain Mechanisms and Treatments
Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
Keywords: neuropathic pain, endocannabinoid system, fatty acid amide hydrolase, monoacylglycerol lipase, anandamide, 2-arachidonoylglycerol, CB1 receptor, CB2 receptor, URB597, JZL184, chronic constriction injury, mechanical allodynia, cold allodynia, analgesic drug development
MeSH terms: Fatty Acid Amide Hydrolases, Amidohydrolases, Animals, Arachidonic Acids, Benzamides, Carbamates, Cold Temperature, Enzyme Inhibitors, Glycerides, Hyperalgesia, Male, Mice, Inbred C57BL, Monoacylglycerol Lipases, Narcotic Antagonists, Pain, Pain Measurement, Peripheral Nervous System Diseases, Piperidines, Pyridines, Analgesics, Non-Narcotic, Receptor, Cannabinoid, CB1, Receptor, Cannabinoid, CB2, TRPV Cation Channels, Mice, Benzodioxoles, Polyunsaturated Alkamides, Cannabinoid Receptor Modulators, Endocannabinoids

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Self-check

Citations

Cites

Cited by

Related

Metadata

Record

About these checks