Modulation of the anti‐nociceptive effects of 2‐arachidonoyl glycerol by peripherally administered FAAH and MGL inhibitors in a neuropathic pain model
Open accessAbstract
Background and purpose: There are limited options for the treatment of neuropathic pain. Endocannabinoids, such as anandamide and 2‐arachidonoyl glycerol (2‐AG), are promising pain modulators and there is recent evidence of interactions between anandamide and 2‐AG biosynthesis and metabolism. It has been clearly demonstrated that 2‐AG degradation is mainly catalysed not only by monoacylglycerol lipase (MGL) but also by a fatty acid amide hydrolase (FAAH). Inhibitors specifically targeting these two enzymes have also been described: URB602 and URB597, respectively. However, the anti‐nociceptive effects of the combination of peripherally injected 2‐AG, URB602 and URB597 in a neuropathic pain model have not yet been determined. This was performed in the presence or absence of cannabinoid CB 1 (AM251) and CB 2 (AM630) receptor antagonists. Experimental approach: Mechanical allodynia and thermal hyperalgesia were evaluated in 213 male Wistar rats allocated to 32 different groups. Drugs were injected subcutaneously in the dorsal surface of the hind paw (50 μL) 15 min before pain tests. Key results: 2‐AG, URB602 and URB597 significantly decreased mechanical allodynia and thermal hyperalgesia with ED50 of 1.6±1.5 and 127±83 μg for 2‐AG and URB602, respectively. These effects were mediated locally and were mostly inhibited by the two cannabinoid antagonists. Conclusions and implications: The combination of the three compounds did not produce any greater anti‐allodynic or anti‐hyperalgesic effects, suggesting that FAAH inhibition could reduce or limit the anti‐nociceptive effects of 2‐AG. Peripheral administration of endocannabinoids or MGL/FAAH inhibitors is a promising analgesic approach requiring further investigation. British Journal of Pharmacology (2008) 155 , 913–924; doi: 10.1038/bjp.2008.322 ; published online 11 August 2008
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
Cites
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?
In both SNL and pSNL models, the FAAH inhibitor URB597 evoked anti-allodynic as well as anti-hyperalgesic effects.
“In both SNL and pSNL models, the FAAH inhibitor URB597 evoked anti-allodynic (de Novellis et al, 2011), as well as anti-hyperalgesic effects (Desroches et al, 2008(Desroches et al, , 2014b)).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Desroches et al, 2008
2-AG produces anti-hyperalgesic and anti-allodynic effects through activation of both peripheral CB1 and CB2 receptors.
“whereas 2-AG produced anti-hyperalgesic and anti-allodynic effects through activation of both peripheral CB1 and CB2 receptors.67”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [67]
URB602 administered locally in the paw suppressed neuropathic nociception in the Seltzer model through activation of both CB1 and CB2 receptors.
“The MGL inhibitor URB602 (which cannot be used systemically as a selective MGL inhibitor), administered locally in the paw, also suppressed neuropathic nociception in this model through activation of both CB1 and CB2 receptors.67”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [67]
URB597 administered locally in the paw, but not systemically, suppressed both thermal hyperalgesia and mechanical allodynia through a CB1 mechanism.
“The FAAH inhibitor URB597, administered locally in the paw,67 but not systemically62 suppressed both thermal hyperalgesia and mechanical allodynia through a CB1 mechanism.”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [67]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Cites
Statistical principles in experimental design.
Winer, B. J. (1962) · McGraw-Hill Book Company · doi:10.1037/11774-000 · Cited by 27,137 · see citing works
Draper, N. R., & Smith, H. (2005) · Technometrics · doi:10.1198/tech.2005.s303 · Cited by 17,993 · see citing works
A new and sensitive method for measuring thermal nociception in cutaneous hyperalgesia
Hargreaves, K., Dubner, R. A., Brown, F. J., Flores, C., & Joris, J. L. (1988) · Pain · doi:10.1016/0304-3959(88)90026-7 · Cited by 5,155 · see citing works
Draper, N. R., & Smith, H. (1998) · Wiley series in probability and statistics · doi:10.1002/9781118625590 · Cited by 5,086 · see citing works
Statistical Principles in Experimental Design
Green, P. E., Winer, B. J., Brown, D. R., & Michels, K. M. (1992) · Journal of Marketing Research · doi:10.2307/3172747 · Cited by 4,333 · see citing works
Gunst, R. F., Draper, N. R., & Smith, H. C. (1999) · Technometrics · doi:10.2307/1270576 · Cited by 3,795 · see citing works
Ledent, C. A., Valverde, O., Cossu, G., Petitet, F., Aubert, J.-F., Beslot, F., Böhme, G. A., Impérato, A., Pedrazzini, T., Roques, B. P., et al. (1999) · Science · doi:10.1126/science.283.5400.401 · Cited by 3,612 · see citing works
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 · see citing works
DeLÉAN, A., Munson, P. J., & Rodbard, D. (1978) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.1978.235.2.e97 · Cited by 2,384 · see citing works
Seltzer, Z., Dubner, R., & Shir, Y. (1990) · Pain · doi:10.1016/0304-3959(90)91074-s · Cited by 1,847 · see citing works
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 · see citing works
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 · see citing works
A Comprehensive Profile of Brain Enzymes that Hydrolyze the Endocannabinoid 2-Arachidonoylglycerol
Blankman, J. L., Simon, G. M., & Cravatt, B. F. (2007) · Chemistry & Biology · doi:10.1016/j.chembiol.2007.11.006 · Cited by 1,177 · see citing works
Enzyme changes in neonatal skeletal muscle: effect of thyroid deficiency
Baldwin, K. M., Hooker, A. M., Campbell, P., & Lewis, R. (1978) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.1978.235.3.c97 · Cited by 1,118 · see citing works
Increased mortality, hypoactivity, and hypoalgesia in cannabinoid CB1 receptor knockout mice
Zimmer, A., Zimmer, A. M., Hohmann, A. G., Herkenham, M. A., & Bonner, T. I. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.10.5780 · Cited by 1,065 · see citing works
Control of pain initiation by endogenous cannabinoids
Calignano, A., Rana, G. L., Giuffrida, A., & Piomelli, D. (1998) · Nature · doi:10.1038/28393 · Cited by 1,055 · see citing works
Targeting the endocannabinoid system: to enhance or reduce?
Marzo, V. D. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2553 · Cited by 798 · see citing works
An endocannabinoid mechanism for stress-induced analgesia
Hohmann, A. G., Suplita, R. L., Bolton, N. M., Neely, M. H., Fegley, D., Mangieri, R., Krey, J. F., Michael Walker, J., Holmes, P. V., Crystal, J. D., et al. (2005) · Nature · doi:10.1038/nature03658 · Cited by 778 · see citing works
Cannabinoids mediate analgesia largely via peripheral type 1 cannabinoid receptors in nociceptors
Agarwal, N., Pacher, P., Tegeder, I., Amaya, F., Constantin, C. E., Brenner, G. J., Rubino, T., Michalski, C. W., Marsicano, G., Monory, K., et al. (2007) · Nature Neuroscience · doi:10.1038/nn1916 · Cited by 571 · see citing works
Gulyas, A. I., Cravatt, B. F., Bracey, M. H., Dinh, T. P., Piomelli, D., Boscia, F., & Freund, T. F. (2004) · European Journal of Neuroscience · doi:10.1111/j.1460-9568.2004.03428.x · Cited by 561 · see citing works
The pharmacology of cannabinoid receptors and their ligands: an overview
Pertwee, R. G. (2006) · International Journal of Obesity · doi:10.1038/sj.ijo.0803272 · Cited by 558 · see citing works
Ibrahim, M. M., Porreca, F., Lai, J., Albrecht, P. J., Rice, F. L., Khodorova, A., Davar, G., Makriyannis, A., Vanderah, T. W., Mata, H. P., et al. (2005) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0409888102 · Cited by 521 · see citing works
Tal, M., & Bennett, G. J. (1994) · Pain · doi:10.1016/0304-3959(94)90013-2 · Cited by 436 · see citing works
Guindon, J., & Hohmann, A. G. (2008) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707531 · Cited by 423 · see citing works
Self-citationCB2 cannabinoid receptor-mediated peripheral antinociception
Malan, P. T., Ibrahim, M. M., Deng, H., Liu, Q., Mata, H. P., Vanderah, T., Porreca, F., & Makriyannis, A. (2001) · Pain · doi:10.1016/s0304-3959(01)00321-9 · Cited by 391 · see citing works
Evidence for novel cannabinoid receptors
Begg, M., Pacher, P., Bátkai, S., Osei‐Hyiaman, D., Offertáler, L., Mo, F.-M., LIU, J., & Kunos, G. (2005) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2004.11.005 · Cited by 385 · see citing works
Gonsiorek, W., Lunn, C. A., Fan, X., Narula, S. K., Lundell, D. J., & Hipkin, R. W. (2000) · Molecular Pharmacology · doi:10.1016/s0026-895x(24)26516-0 · Cited by 370 · see citing works
Cannabinoids and neuroinflammation
Walter, L. M., & Stella, N. (2004) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0705667 · Cited by 334 · see citing works
Cannabinoid 1 receptors are expressed in nociceptive primary sensory neurons
Ahluwalia, J. P., Urbán, L., Capogna, M., Bevan, S., & Nagy, I. (2000) · Neuroscience · doi:10.1016/s0306-4522(00)00389-4 · Cited by 302 · see citing works
Anandamide inhibits metabolism and physiological actions of 2-arachidonoylglycerol in the striatum
Maccarrone, M., Rossi, S., Bari, M., Chiara, V. D., Fezza, F., Musella, A., Gasperi, V., Prosperetti, C., Bernardi, G., Finazzi‐Agrò, A., et al. (2008) · Nature Neuroscience · doi:10.1038/nn2042 · Cited by 293 · see citing works
Endocannabinoids and the regulation of their levels in health and disease
Marzo, V. D., & Petrosino, S. (2007) · Current Opinion in Lipidology · doi:10.1097/mol.0b013e32803dbdec · Cited by 289 · see citing works
Actions of the FAAH inhibitor URB597 in neuropathic and inflammatory chronic pain models
Jayamanne, A., Greenwood, R., Mitchell, V. A., Aslan, S., Piomelli, D., & Vaughan, C. W. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706510 · Cited by 287 · see citing works
2-Arachidonoylglycerol and the cannabinoid receptors
Sugiura, T., & Waku, K. (2000) · Chemistry and Physics of Lipids · doi:10.1016/s0009-3084(00)00189-4 · Cited by 231 · see citing works
Changes in spinal and supraspinal endocannabinoid levels in neuropathic rats
Petrosino, S., Palazzo, E., de Novellis, V., Bisogno, T., Rossi, F., Maione, S., & Di Marzo, V. (2007) · Neuropharmacology · doi:10.1016/j.neuropharm.2006.08.011 · Cited by 227 · see citing works
Dinh, T. P., Kathuria, S., & Piomelli, D. (2004) · Molecular Pharmacology · doi:10.1124/mol.104.002071 · Cited by 227 · see citing works
Goparaju, S. K., Ueda, N., Taniguchi, K., & Yamamoto, S. (1999) · Biochemical Pharmacology · doi:10.1016/s0006-2952(98)00314-1 · Cited by 212 · see citing works
Mitrirattanakul, S., Ramakul, N., Guerrero, A. V., Matsuka, Y., Ono, T., Iwase, H., Mackie, K., Faull, K. F., & Spigelman, I. (2006) · Pain · doi:10.1016/j.pain.2006.06.016 · Cited by 207 · see citing works
The endocannabinoid signalling system: Biochemical aspects
Bisogno, T., Ligresti, A., & Marzo, V. D. (2005) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2005.01.027 · Cited by 200 · see citing works
Cannabinoid Mechanisms of Pain Suppression
Walker, J. M., & Hohmann, A. G. (2005) · Handbook of experimental pharmacology · doi:10.1007/3-540-26573-2_17 · Cited by 177 · see citing works
Identification of a Novel Endocannabinoid-Hydrolyzing Enzyme Expressed by Microglial Cells
Muccioli, G. G., Xu, C., Odah, E., Cudaback, E., Cisneros, J. A., Lambert, D. M., López-Rodríguez, M. L., Bajjalieh, S., & Stella, N. (2007) · Journal of Neuroscience · doi:10.1523/jneurosci.4830-06.2007 · Cited by 172 · see citing works
CB2 cannabinoid receptor mediation of antinociception
Ibrahim, M. M., Rude, M. L., Stagg, N. J., Mata, H. P., Lai, J. Y., Vanderah, T. W., Porreca, F., Buckley, N. E., Makriyannis, A., & Malan, P. T. (2006) · Pain · doi:10.1016/j.pain.2005.12.018 · Cited by 172 · see citing works
Elmes, S. J. R., Jhaveri, M. D., Smart, D., Kendall, D. A., & Chapman, V. (2004) · European Journal of Neuroscience · doi:10.1111/j.1460-9568.2004.03690.x · Cited by 160 · see citing works
Analgesic effects of fatty acid amide hydrolase inhibition in a rat model of neuropathic pain
Jhaveri, M. D., Richardson, D., Kendall, D. A., Barrett, D. A., & Chapman, V. (2006) · The Journal of Neuroscience · doi:10.1523/jneurosci.3326-06.2006 · Cited by 159 · see citing works
Endocannabinoid metabolism and uptake: novel targets for neuropathic and inflammatory pain
Jhaveri, M. D., Richardson, D. S., & Chapman, V. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707433 · Cited by 145 · see citing works
Walczak, J.-S., Pichette, V., Leblond, F., Desbiens, K., & Beaulieu, P. (2005) · Neuroscience · doi:10.1016/j.neuroscience.2005.02.010 · Cited by 133 · see citing works
Self-citationLever, I. J., & Rice, A. S. C. (2007) · Springer eBooks · doi:10.1007/978-3-540-33823-9_10 · Cited by 108 · see citing works
King, A. R., Duranti, A., Tontini, A., Rivara, S., Rosengarth, A., Clapper, J. R., Astarita, G., Geaga, J. A., Luecke, H., Mor, M., et al. (2007) · Chemistry & Biology · doi:10.1016/j.chembiol.2007.10.017 · Cited by 108 · see citing works
Gutierrez, T., Farthing, J. N., Zvonok, A. M., Makriyannis, A., & Hohmann, A. G. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706984 · Cited by 106 · see citing works
Guindon, J., Desroches, J., & Beaulieu, P. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706990 · Cited by 101 · see citing works
Self-citationRole of the endogenous cannabinoid system in the formalin test of persistent pain in the rat
Beaulieu, P., Bisogno, T., Punwar, S., Farquhar-Smith, W. P., Ambrosino, G., Marzo, V. D., & Rice, A. S. C. (2000) · European Journal of Pharmacology · doi:10.1016/s0014-2999(00)00226-0 · Cited by 101 · see citing works
Self-citationLack of selectivity of URB602 for 2‐oleoylglycerol compared to anandamide hydrolysis in vitro
Vandevoorde, S., Jonsson, K., Labar, G., Persson, E., Lambert, D. M., & Fowler, C. J. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706971 · Cited by 96 · see citing works
Oka, S., Shin, Y., Ikeda, S., Gokoh, M., Kishimoto, S., Waku, K., Ishima, Y., & Sugiura, T. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m413260200 · Cited by 92 · see citing works
Guindon, J., & Beaulieu, P. (2006) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.12.002 · Cited by 90 · see citing works
Self-citationCannabinoid CB2 Receptor-Mediated Anti-nociception in Models of Acute and Chronic Pain
Jhaveri, M. D., Sagar, D. R., Elmes, S. J. R., Kendall, D. A., & Chapman, V. (2007) · Molecular Neurobiology · doi:10.1007/s12035-007-8007-7 · Cited by 89 · see citing works
Suplita, R. L., Gutierrez, T., Fegley, D., Piomelli, D., & Hohmann, A. G. (2005) · Neuropharmacology · doi:10.1016/j.neuropharm.2005.10.007 · Cited by 78 · see citing works
Sokal, D. M., Elmes, S. J. R., Kendall, D. A., & Chapman, V. (2003) · Neuropharmacology · doi:10.1016/s0028-3908(03)00195-3 · Cited by 67 · see citing works
Walczak, J., Pichette, V., Leblond, F., Desbiens, K., & Beaulieu, P. (2006) · Journal of Neuroscience Research · doi:10.1002/jnr.20821 · Cited by 62 · see citing works
Self-citationTherapeutic Potential of Endocannabinoid‐Hydrolysing Enzyme Inhibitors
Saario, S. M., & Laitinen, J. T. (2007) · Basic & Clinical Pharmacology & Toxicology · doi:10.1111/j.1742-7843.2007.00130.x · Cited by 60 · see citing works
Reassessment of the role of cannabinoids in the management of pain
Beaulieu, P., & Ware, M. (2007) · Current Opinion in Anaesthesiology · doi:10.1097/aco.0b013e3282efd175 · Cited by 34 · see citing works
Self-citation
Flagged first, then by citations
1 of the 60 references couldn’t be matched to a known paper.
Cited by
Sorted by citations
The Endocannabinoid System and Pain
Guindon, J., & Hohmann, A. (2009) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/187152709789824660 · Cited by 476 · see citing works
Self-citationChemical Probes of Endocannabinoid Metabolism
Blankman, J. L., & Cravatt, B. F. (2013) · Pharmacological Reviews · doi:10.1124/pr.112.006387 · Cited by 327 · see citing works
Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside
Rahn, E. J., & Hohmann, A. G. (2009) · Neurotherapeutics · doi:10.1016/j.nurt.2009.08.002 · Cited by 305 · see citing works
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
Peripheral gating of pain signals by endogenous lipid mediators
Piomelli, D., & Sasso, O. (2014) · Nature Neuroscience · doi:10.1038/nn.3612 · Cited by 236 · see citing works
2-Arachidonoylglycerol: A signaling lipid with manifold actions in the brain
Baggelaar, M. P., Maccarrone, M., & van der Stelt, M. (2018) · Progress in Lipid Research · doi:10.1016/j.plipres.2018.05.002 · Cited by 224 · see citing works
The Role of the Endocannabinoid System in Pain
Woodhams, S. G., Sagar, D. R., Burston, J. J., & Chapman, V. (2015) · Handbook of experimental pharmacology · doi:10.1007/978-3-662-46450-2_7 · Cited by 205 · see citing works
Targeting Fatty Acid Amide Hydrolase (FAAH) to Treat Pain and Inflammation
Schlosburg, J. E., Kinsey, S. G., & Lichtman, A. H. (2009) · The AAPS Journal · doi:10.1208/s12248-008-9075-y · Cited by 165 · see citing works
Guindon, J., Lai, Y., Takacs, S. M., Bradshaw, H. B., & Hohmann, A. G. (2013) · Pharmacological Research · doi:10.1016/j.phrs.2012.10.013 · Cited by 160 · see citing works
Self-citationGhosh, S., Wise, L. E., Chen, Y., Gujjar, R., Mahadevan, A., Cravatt, B. F., & Lichtman, A. H. (2013) · Life Sciences · doi:10.1016/j.lfs.2012.06.020 · Cited by 127 · see citing works
Guindon, J., Guijarro, A. I., Piomelli, D., & Hohmann, A. G. (2010) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2010.01192.x · Cited by 120 · see citing works
Self-citationLötsch, J., Weyer-Menkhoff, I., & Tegeder, I. (2017) · European Journal of Pain · doi:10.1002/ejp.1148 · Cited by 118 · see citing works
Booker, L., Kinsey, S. G., Abdullah, R. A., Blankman, J. L., Long, J. Z., Ezzili, C., Boger, D. L., Cravatt, B. F., & Lichtman, A. H. (2012) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2011.01445.x · Cited by 116 · see citing works
Discovery of Potent and Reversible Monoacylglycerol Lipase Inhibitors
King, A. R., Dotsey, E. Y., Lodola, A., Jung, K., Ghomian, A., Qiu, Y., Fu, J., Mor, M., & Piomelli, D. (2009) · Chemistry & Biology · doi:10.1016/j.chembiol.2009.09.012 · Cited by 117 · 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
Monoacylglycerol lipase – a target for drug development?
Fowler, C. (2012) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2012.01950.x · Cited by 95 · see citing works
Role of Cannabinoids in the Treatment of Pain and (Painful) Spasticity
Karst, M., Wippermann, S., & Ahrens, J. (2010) · Drugs · doi:10.2165/11585260-000000000-00000 · Cited by 91 · see citing works
King, A., Lodola, A., Carmi, C., Fu, J., Mor, M., & Piomelli, D. (2009) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2009.00276.x · Cited by 91 · see citing works
Exercise and Neuropathic Pain: A General Overview of Preclinical and Clinical Research
Leitzelar, B. N., & Koltyn, K. F. (2021) · Sports Medicine - Open · doi:10.1186/s40798-021-00307-9 · Cited by 84 · see citing works
Wilkerson, J. L., Ghosh, S., Mustafa, M., Abdullah, R. A., Niphakis, M. J., Cabrera, R., Maldonado, R. L., Cravatt, B. F., & Lichtman, A. H. (2017) · Neuropharmacology · doi:10.1016/j.neuropharm.2016.11.015 · Cited by 78 · see citing works
Cannabinoids in pain management: CB1, CB2 and non-classic receptor ligands
Davis, M. P. (2014) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.2014.918603 · Cited by 79 · see citing works
Khasabova, I. A., Chandiramani, A., Harding-Rose, C., Simone, D. A., & Seybold, V. S. (2011) · Pharmacological Research · doi:10.1016/j.phrs.2011.03.007 · Cited by 75 · see citing works
Caprioli, A., Coccurello, R., Rapino, C., Serio, S. D., Tommaso, M. D., Vertechy, M., Vacca, V., Battista, N., Pavone, F., Maccarrone, M., et al. (2012) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.191403 · Cited by 68 · see citing works
Monoglyceride lipase: Structure and inhibitors
Scalvini, L., Piomelli, D., & Mor, M. (2015) · Chemistry and Physics of Lipids · doi:10.1016/j.chemphyslip.2015.07.011 · Cited by 66 · see citing works
Cannabinoid Therapeutics in Chronic Neuropathic Pain: From Animal Research to Human Treatment
Campos, R. M. P., Aguiar, A. F. L., Paes-Colli, Y., Trindade, P. M. P., Ferreira, B. K., Reis, R. A. D. M., & Sampaio, L. D. S. (2021) · Frontiers in Physiology · doi:10.3389/fphys.2021.785176 · Cited by 59 · see citing works
Targeting the cannabinoid system for pain relief?
Chiou, L., Hu, S. S., & Ho, Y. (2013) · Acta anaesthesiologica Taiwanica · doi:10.1016/j.aat.2013.10.004 · Cited by 57 · see citing works
Spradley, J. M., Guindon, J., & Hohmann, A. G. (2010) · Pharmacological Research · doi:10.1016/j.phrs.2010.03.007 · Cited by 54 · see citing works
Self-citationCB1 and CB2 receptor agonists promote analgesia through synergy in a murine model of tumor pain
Khasabova, I. A., Gielissen, J. M., Chandiramani, A., Harding-Rose, C., Odeh, D. A., Simone, D. A., & Seybold, V. S. (2011) · Behavioural Pharmacology · doi:10.1097/fbp.0b013e3283474a6d · Cited by 53 · see citing works
Desroches, J., Charron, S., Bouchard, J., & Beaulieu, P. (2013) · Neuropharmacology · doi:10.1016/j.neuropharm.2013.10.006 · Cited by 51 · see citing works
Self-citationHossain, M. Z., Ando, H., Unno, S., & Kitagawa, J. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21041423 · Cited by 52 · see citing works
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 · see citing works
Biochanin A, a naturally occurring inhibitor of fatty acid amide hydrolase
Thors, L., Burston, J. J., Alter, B. J., McKinney, M., Cravatt, B., Ross, R., Pertwee, R. G., th, R. W. G., Wiley, J. L., & Fowler, C. (2010) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2010.00716.x · Cited by 46 · see citing works
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
Slivicki, R. A., Saberi, S. A., Iyer, V., Vemuri, K. V., Makriyannis, A., & Hohmann, A. G. (2018) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.118.252288 · Cited by 45 · see citing works
Starowicz, K., & Marzo, V. D. (2013) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2013.01.075 · Cited by 38 · see citing works
Munawar, N., Oriowo, M. A., & Masocha, W. (2017) · Frontiers in Pharmacology · doi:10.3389/fphar.2017.00136 · Cited by 36 · see citing works
Ma, W.-X., Yu, T.-S., Fan, Y., Zhang, S., Ren, P., Wang, S.-B., Zhao, R., Pi, J., & Guan, D.-W. (2011) · International Journal of Legal Medicine · doi:10.1007/s00414-011-0567-4 · Cited by 31 · see citing works
Uhelski, M. L., Cain, D. M., Harding-Rose, C., & Simone, D. A. (2013) · Neuroscience · doi:10.1016/j.neuroscience.2013.05.003 · Cited by 30 · see citing works
The Effects of Peptide and Lipid Endocannabinoids on Arthritic Pain at the Spinal Level
Petrovszki, Z., Kovács, G. Z., Tömböly, C., Benedek, G., & Horváth, G. (2012) · Anesthesia & Analgesia · doi:10.1213/ane.0b013e31824c4eeb · Cited by 21 · see citing works
Scarpelli, R., Sasso, O., & Piomelli, D. (2015) · ChemMedChem · doi:10.1002/cmdc.201500395 · Cited by 21 · see citing works
Petrenko, A. B., Yamazaki, M., Sakimura, K., Kano, M., & Baba, H. (2014) · Behavioural Brain Research · doi:10.1016/j.bbr.2014.05.063 · Cited by 17 · see citing works
Mecs, L., Tuboly, G., Toth, K., Nagy, E., Nyari, T., Benedek, G., & Horvath, G. (2010) · Clinical and Experimental Pharmacology and Physiology · doi:10.1111/j.1440-1681.2010.05346.x · Cited by 16 · see citing works
Kamimura, R., Hossain, M. Z., Unno, S., Ando, H., Masuda, Y., TAKAHASHI, K., Otake, M., Saito, I., & Kitagawa, J. (2018) · Journal of Oral Science · doi:10.2334/josnusd.17-0005 · Cited by 16 · see citing works
No more pain upon G q‐protein‐coupled receptor activation: role of endocannabinoids
Hu, S. S., Ho, Y., & Chiou, L. (2014) · European Journal of Neuroscience · doi:10.1111/ejn.12475 · Cited by 14 · see citing works
RetractedKeimpema, E., Hökfelt, T. G. M., Harkany, T., & Doherty, P. (2014) · European Journal of Neuroscience · doi:10.1111/ejn.12431 · Cited by 13 · see citing works
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
Morales‐Soto, W., Thomasi, B. B. D. M., & Gulbransen, B. D. (2024) · Glia · doi:10.1002/glia.24599 · Cited by 11 · see citing works
Filipiuc, L.-E., Creangă-Murariu, I., Tamba, B.-I., Ababei, D. C., Rusu, R.-N., Stanciu, G. D., Ştefănescu, R., Ciorpac, M., Szilagyi, A., Gogu, M.-R., et al. (2024) · Scientific Reports · doi:10.1038/s41598-024-67154-y · Cited by 9 · see citing works
Shimoyama, H., Tsuda, M., Masuda, T., Yoshinaga, R., Tsukamoto, K., Tozaki‐Saitoh, H., & Inoue, K. (2014) · The Open Pain Journal · doi:10.2174/1876386301407010001 · Cited by 3 · see citing works
Interaction between the dopaminergic and endocannabinoid systems promotes peripheral antinociception
de Queiroz, B. F. G., Fonseca, F. C. D. S., Barra, W. C. P., Valério, G. B., Irie, A. L., Perez, A. C., Romero, T. R. L., & Duarte, I. D. G. (2024) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2024.177195 · Cited by 2 · see citing works
Relação do uso do canabidiol na dor: uma revisão sistemática
Comunello, M. E., & Rangel, M. P. (2023) · Research Society and Development · doi:10.33448/rsd-v12i5.41478 · Cited by 1 · see citing works
Targeting the Endocannabinoid Metabolic Enzymes to Reduce Inflammatory Pain
Ghosh, S. (2014) · VCU Scholars Compass (Virginia Commonwealth University) · doi:10.25772/ngv2-th75 · Cited by 1 · see citing works
Philosophy at Virginia Commonwealth University.
Booker, L. (2011)
The cannabinoid system and its role in nociception
Beltramo, M. (2016) · Wiley eBooks · doi:10.1002/9781118455968.ch6
Endocannabinoid modulation of capsaicin-induced behavioral hypersensitivity
Spradley, J. M. (2010)
Neurochemistry of Endogenous Antinociception
Horváth, G. (2010) · Advances in neurobiology · doi:10.1007/978-1-4419-7104-3_15
Endocannabinoids in pain modulation
Chapman, V., & Woodhams, S. G. (2025) · Handbook of behavioral neuroscience · doi:10.1016/b978-0-443-13908-6.00010-4
Castañeda‐Ruelas, G. M., Grijalva-Contreras, L. E., & Quiñonez‐Bastidas, G. N. (2026) · Medical Sciences · doi:10.3390/medsci14050560
BindingDB Entry 4628: Discovery of potent and reversible monoacylglycerol lipase inhibitors.
BindingDB (2011) · UC San Diego · doi:10.7270/q2hh6hj3
Targeting the endocannabinoid system to reduce nociception
Booker, L. (2011) · VCU Scholars Compass (Virginia Commonwealth University) · doi:10.25772/j2fe-wf53
- Authors
- Desroches, J., Guindon, J., Lambert, C., & Beaulieu, P.
- Affiliations
- Centre Hospitalier de l’Université de Montréal (CA)
- Corresponding author
- Beaulieu, P
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2008-11
- Volume
- 155
- Issue
- 6
- Pages
- 913-924
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- PMC
- PMC2597245
- OpenAlex
- W1999646805
- Cited by
- 63
- References
- 60
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 3 · 2023: 1 · 2022: 1 · 2021: 2 · 2020: 1 · 2018: 4 · 2017: 6 · 2016: 2 · 2015: 5 · 2014: 7 · 2013: 5 · 2012: 6
- FWCI
- 4.45
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- British Journal of Pharmacology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- HAL (submittedVersion, other-oa)
- Funders
- Pfizer
- Topics
- Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- 2-arachidonoylglycerol, endocannabinoids, fatty acid amide hydrolase inhibition, monoacylglycerol lipase inhibition, URB597, neuropathic pain, mechanical allodynia, thermal hyperalgesia, CB1 receptor, CB2 receptor, antinociceptive effect, endocannabinoid metabolism
- MeSH terms
- Fatty Acid Amide Hydrolases, Amidohydrolases, Animals, Arachidonic Acids, Drug Combinations, Glycerides, Injections, Subcutaneous, Male, Models, Neurological, Monoacylglycerol Lipases, Pain, Pain Measurement, Rats, Wistar, Rats
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
