Full Fatty Acid Amide Hydrolase Inhibition Combined with Partial Monoacylglycerol Lipase Inhibition: Augmented and Sustained Antinociceptive Effects with Reduced Cannabimimetic Side Effects in Mice

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 · see citing works

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 · see citing works

Cannabinoid receptor localization in brain.

Herkenham, M., Lynn, A. B., Little, M. D., Johnson, M. R., Melvin, L. S., de Costa, B. R., & Rice, K. C. (1990) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.87.5.1932 · Cited by 2,321 · see citing works

2-Arachidonoylgylcerol: A Possible Endogenous Cannabinoid Receptor Ligand in Brain

Sugiura, T., Kondo, S., Sukagawa, A., Nakane, S., Shinoda, A., Itoh, K., Yamashita, A., & Waku, K. (1995) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1995.2437 · Cited by 2,196 · see citing works

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 · see citing works

Brain monoglyceride lipase participating in endocannabinoid inactivation

Dinh, T. P., Carpenter, D., Leslie, F. M., Freund, T. F., Katona, I., Sensi, S. L., Kathuria, S., & Piomelli, D. (2002) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.152334899 · Cited by 1,373 · see citing works

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 · 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

Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects

Long, J. Z., Li, W., Booker, L., Burston, J. J., Kinsey, S. G., Schlosburg, J. E., Pavón, F. J., Serrano, A., Selley, D. E., Parsons, L. H., et al. (2008) · Nature Chemical Biology · doi:10.1038/nchembio.129 · Cited by 938 · see citing works

Endocannabinoid Hydrolysis Generates Brain Prostaglandins That Promote Neuroinflammation

Nomura, D. K., Morrison, B. E., Blankman, J. L., Long, J. Z., Kinsey, S. G., Marcondes, M. C. G., Ward, A. M., Hahn, Y. K., Lichtman, A. H., Conti, B., et al. (2011) · Science · doi:10.1126/science.1209200 · Cited by 727 · see citing works

Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system

Schlosburg, J. E., Blankman, J. L., Long, J. Z., Nomura, D. K., Pan, B., Kinsey, S. G., Nguyen, P. T., Ramesh, D., Booker, L., Burston, J. J., et al. (2010) · Nature Neuroscience · doi:10.1038/nn.2616 · Cited by 641 · see citing works

Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

Ahn, K., Johnson, D. S., Mileni, M., Beidler, D., Long, J. Z., McKinney, M. K., Weerapana, E., Sadagopan, N., Liimatta, M., Smith, S. E., et al. (2009) · Chemistry & Biology · doi:10.1016/j.chembiol.2009.02.013 · Cited by 439 · see citing works

Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo

Long, J. Z., Nomura, D. K., Vann, R. E., Walentiny, D. M., Booker, L., Jin, X., Burston, J. J., Sim‐Selley, L. J., Lichtman, A. H., Wiley, J. L., et al. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0909411106 · Cited by 393 · see citing works

Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain

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.109.155465 · Cited by 330 · see citing works

Characterization of Monoacylglycerol Lipase Inhibition Reveals Differences in Central and Peripheral Endocannabinoid Metabolism

Long, J. Z., Nomura, D. K., & Cravatt, B. F. (2009) · Chemistry & Biology · doi:10.1016/j.chembiol.2009.05.009 · Cited by 305 · see citing works

Mice lacking fatty acid amide hydrolase exhibit a cannabinoid receptor-mediated phenotypic hypoalgesia

Lichtman, A. H., Shelton, C. C., Advani, T., & Cravatt, B. F. (2004) · Pain · doi:10.1016/j.pain.2004.01.022 · Cited by 301 · see citing works

Pharmacology and stereoselectivity of structurally novel cannabinoids in mice.

Little, P., Compton, D. M., Johnson, M. R., Melvin, L. S., & Martin, B. R. (1988) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)13256-4 · Cited by 290 · 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

Monoacylglycerol Lipase Activity Is a Critical Modulator of the Tone and Integrity of the Endocannabinoid System

Chanda, P. K., Gao, Y., Mark, L., Btesh, J., Strassle, B. W., Lu, P., Piesla, M. J., Zhang, M.-Y., Bingham, B., Uveges, A. J., et al. (2010) · Molecular Pharmacology · doi:10.1124/mol.110.068304 · Cited by 228 · see citing works

A FAAH-Regulated Class of N- Acyl Taurines That Activates TRP Ion Channels

Saghatelian, A., McKinney, M. K., Bandell, M., Patapoutian, A., & Cravatt, B. F. (2006) · Biochemistry · doi:10.1021/bi0608008 · Cited by 213 · see citing works

The fatty acid amide hydrolase inhibitor URB597 (cyclohexylcarbamic acid 3′-carbamoylbiphenyl-3-yl ester) reduces neuropathic pain after oral administration in mice

Russo, R., LoVerme, J., La Rana, G., Compton, T. R., Parrott, J., Duranti, A., Tontini, A., Mor, M., Tarzia, G., Calignano, A., et al. (2007) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.107.119941 · Cited by 182 · see citing works

Enhancement of endocannabinoid signaling with JZL184, an inhibitor of the 2-arachidonoylglycerol hydrolyzing enzyme monoacylglycerol lipase, produces anxiolytic effects under conditions of high environmental aversiveness in rats

Sciolino, N. R., Zhou, W., & Hohmann, A. G. (2011) · Pharmacological Research · doi:10.1016/j.phrs.2011.04.010 · Cited by 179 · see citing works

Repeated Low-Dose Administration of the Monoacylglycerol Lipase Inhibitor JZL184 Retains Cannabinoid Receptor Type 1–Mediated Antinociceptive and Gastroprotective Effects

Kinsey, S. G., Wise, L. E., Ramesh, D., Abdullah, R., Selley, D. E., Cravatt, B. F., & Lichtman, A. H. (2013) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.112.201426 · Cited by 169 · see citing works

Inhibitors of fatty acid amide hydrolase reduce carrageenan‐induced hind paw inflammation in pentobarbital‐treated mice: comparison with indomethacin and possible involvement of cannabinoid receptors

Holt, S., Comelli, F., Costa, B., & Fowler, C. J. (2005) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706348 · Cited by 168 · see citing works

Inhibition of fatty acid amide hydrolase produces analgesia by multiple mechanisms

Chang, L., Luo, L., Palmer, J. A., Sutton, S. W., Wilson, S. J., Barbier, A., Breitenbucher, J. G., Chaplan, S. R., & Webb, M. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706773 · Cited by 166 · see citing works

Alterations in endocannabinoid tone following chemotherapy-induced peripheral neuropathy: Effects of endocannabinoid deactivation inhibitors targeting fatty-acid amide hydrolase and monoacylglycerol lipase in comparison to reference analgesics following cisplatin treatment

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

Evaluation of NHS Carbamates as a Potent and Selective Class of Endocannabinoid Hydrolase Inhibitors

Niphakis, M. J., Cognetta, A. B., Chang, J. W., Buczynski, M. W., Parsons, L. H., Byrne, F., Burston, J. J., Chapman, V., & Cravatt, B. F. (2013) · ACS Chemical Neuroscience · doi:10.1021/cn400116z · Cited by 157 · see citing works

Inhibition of fatty acid amide hydrolase produces analgesia by multiple mechanisms

Chang, L., Luo, L., Palmer, J. A., Sutton, S., Wilson, S. J., Barbier, A. J., Breitenbucher, J. G., Chaplan, S. R., & Webb, M. (2006) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0706699 · Cited by 155 · see citing works

Alterations of Endocannabinoid Signaling, Synaptic Plasticity, Learning, and Memory in Monoacylglycerol Lipase Knock-out Mice

Pan, B., Wang, W., Zhong, P., Blankman, J. L., Cravatt, B. F., & Liu, Q.-S. (2011) · Journal of Neuroscience · doi:10.1523/jneurosci.2075-11.2011 · Cited by 147 · 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

<i>In vivo</i> characterization of the highly selective monoacylglycerol lipase inhibitor <scp>KML</scp>29: antinociceptive activity without cannabimimetic side effects

Ignatowska‐Jankowska, B. M., Ghosh, S., Crowe, M. S., Kinsey, S. G., Niphakis, M. J., Abdullah, R. A., Tao, Q., O' Neal, S. T., Walentiny, D. M., Wiley, J. L., et al. (2014) · British Journal of Pharmacology · doi:10.1111/bph.12298 · Cited by 128 · see citing works

The monoacylglycerol lipase inhibitor JZL184 suppresses inflammatory pain in the mouse carrageenan model

Ghosh, 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

Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain

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

Molecular mechanisms of pain in the anterior cingulate cortex

Zhuo, M. (2006) · Journal of Neuroscience Research · doi:10.1002/jnr.21003 · Cited by 101 · see citing works

Inhibition of Monoacylglycerol Lipase Attenuates Nonsteroidal Anti-Inflammatory Drug-Induced Gastric Hemorrhages in Mice

Kinsey, S. G., Nomura, D. K., O’Neal, S. T., Long, J. Z., Mahadevan, A., Cravatt, B. F., Grider, J. R., & Lichtman, A. H. (2011) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.110.175778 · Cited by 93 · see citing works

FAAH−/− Mice Display Differential Tolerance, Dependence, and Cannabinoid Receptor Adaptation After Δ9-Tetrahydrocannabinol and Anandamide Administration

Falenski, K. W., Thorpe, A. J., Schlosburg, J. E., Cravatt, B. F., Abdullah, R. A., Smith, T. H., Selley, D. E., Lichtman, A. H., & Sim‐Selley, L. J. (2010) · Neuropsychopharmacology · doi:10.1038/npp.2010.44 · Cited by 83 · see citing works

Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model

Anderson, W. B., Gould, M. J., Torres, R. D., Mitchell, V. A., & Vaughan, C. W. (2014) · Neuropharmacology · doi:10.1016/j.neuropharm.2013.12.018 · Cited by 67 · see citing works

Characterization of the Effects of Reuptake and Hydrolysis Inhibition on Interstitial Endocannabinoid Levels in the Brain: An in Vivo Microdialysis Study

Wiskerke, J., Irimia, C., Cravatt, B. F., Vries, T. J. D., Schoffelmeer, A. N. M., Pattij, T., & Parsons, L. H. (2012) · ACS Chemical Neuroscience · doi:10.1021/cn300036b · Cited by 65 · see citing works

Dual Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase Blockade Produces THC-Like Morris Water Maze Deficits in Mice

Wise, L. E., Long, K. A., Abdullah, R. A., Long, J. Z., Cravatt, B. F., & Lichtman, A. H. (2012) · ACS Chemical Neuroscience · doi:10.1021/cn200130s · Cited by 64 · see citing works

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 · see citing works

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 · see citing works

Cannabinoid agonists differentially substitute for the discriminative stimulus effects of Δ9-tetrahydrocannabinol in C57BL/6J mice

McMahon, L. R., Ginsburg, B. C., & Lamb, R. J. (2007) · Psychopharmacology · doi:10.1007/s00213-007-0900-2 · Cited by 44 · see citing works

Individual and additive effects of neuromodulators on the slow components of afterhyperpolarization currents in layer V pyramidal cells of the rat medial prefrontal cortex

Satake, T., Mitani, H., Nakagome, K., & Kaneko, K. (2008) · Brain Research · doi:10.1016/j.brainres.2008.06.098 · Cited by 31 · see citing works

Endocannabinoid contribution to Δ9-tetrahydrocannabinol discrimination in rodents

Wiley, J. L., Walentiny, D. M., Wright, M. J., Beardsley, P. M., Burston, J. J., Poklis, J. L., Lichtman, A. H., & Vann, R. E. (2014) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2014.05.013 · Cited by 31 · see citing works

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 · see citing works

Phenotypic assessment of THC discriminative stimulus properties in fatty acid amide hydrolase knockout and wildtype mice

Walentiny, D. M., Vann, R. E., & Wiley, J. L. (2015) · Neuropharmacology · doi:10.1016/j.neuropharm.2015.02.004 · Cited by 11 · see citing works

Breaking barriers to novel analgesic drug development

Yekkirala, A. S., Roberson, D. P., Bean, B. P., & Woolf, C. J. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.87 · Cited by 366 · see citing works

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

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

Don't Worry, Be Happy: Endocannabinoids and Cannabis at the Intersection of Stress and Reward

Volkow, N. D., Hampson, A. J., & Baler, R. (2016) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-010716-104615 · Cited by 150 · see citing works

Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake

Chicca, A., Nicolussi, S., Bartholomäus, R., Blunder, M., Rey, A. A., Petrucci, V., Reynoso-Moreno, I., Paredes, J. M. V., Gens, M. D., Lutz, B., et al. (2017) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1704065114 · Cited by 96 · see citing works

A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents

Tripathi, R. K. P. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111953 · Cited by 95 · see citing works

The endocannabinoid hydrolysis inhibitor SA-57: intrinsic antinociceptive effects, augmented morphine-induced antinociception, and attenuated heroin seeking behavior in mice

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

N -acyl taurines are endogenous lipid messengers that improve glucose homeostasis

Grevengoed, T. J., Trammell, S. A. J., McKinney, M. K., Petersen, N., CARDONE, R. L., Svenningsen, J. S., Ogasawara, D., Nexøe-Larsen, C., Knop, F. K., Schwartz, T. W., et al. (2019) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1916288116 · Cited by 56 · see citing works

Role of Cannabinoids in Gastrointestinal Mucosal Defense and Inflammation

Gyires, K., & Zádori, Z. (2016) · Current Neuropharmacology · doi:10.2174/1570159x14666160303110150 · Cited by 57 · see citing works

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 52 · see citing works

Polypharmacological Approaches for CNS Diseases: Focus on Endocannabinoid Degradation Inhibition

Papa, A., Pasquini, S., Contri, C., Gemma, S., Campiani, G., Butini, S., Varani, K., & Vincenzi, F. (2022) · Cells · doi:10.3390/cells11030471 · Cited by 45 · see citing works

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 42 · see citing works

Molecular Understanding of the Activation of CB1 and Blockade of TRPV1 Receptors: Implications for Novel Treatment Strategies in Osteoarthritis

Mlost, J., Kostrzewa, M., Małek, N., & Starowicz, K. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19020342 · Cited by 36 · see citing works

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 29 · see citing works

Harnessing the pyrroloquinoxaline scaffold for FAAH and MAGL interaction: definition of the structural determinants for enzyme inhibition

Brindisi, M., Brogi, S., Maramai, S., Grillo, A., Borrelli, G., Butini, S., Novellino, E., Allarà, M., Ligresti, A., Campiani, G., et al. (2016) · RSC Advances · doi:10.1039/c6ra12524g · Cited by 29 · see citing works

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 27 · see citing works

Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

Pietra, A. D., Krivoshein, G., Ivanov, K., Giniatullina, R., Jyrkkänen, H.-K., Leinonen, V., Lehtonen, M., van den Maagdenberg, A. M. J. M., Savinainen, J. R., & Giniatullin, R. A. (2023) · The Journal of Headache and Pain · doi:10.1186/s10194-023-01568-3 · Cited by 26 · see citing works

Potential Therapeutic Targets to Modulate the Endocannabinoid System in Alzheimer’s Disease

Kanwal, H., Sangineto, M., Ciarnelli, M., Castaldo, P., Villani, R., Romano, A. D., Serviddio, G., & Cassano, T. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25074050 · Cited by 26 · see citing works

Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system

Chicca, A., Arena, C., Bertini, S., Gado, F., Ciaglia, E., Abate, M., Digiacomo, M., Lapillo, M., Poli, G., Bifulco, M., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.05.019 · Cited by 22 · see citing works

Novel Analgesics with Peripheral Targets

Ciotu, C. I., & Fischer, M. J. M. (2020) · Neurotherapeutics · doi:10.1007/s13311-020-00937-z · Cited by 21 · see citing works

Endocannabinoid Signaling in the Central Amygdala and Bed Nucleus of the Stria Terminalis: Implications for the Pathophysiology and Treatment of Alcohol Use Disorder

Bedse, G., Centanni, S. W., Winder, D. G., & Patel, S. (2019) · Alcoholism Clinical and Experimental Research · doi:10.1111/acer.14159 · Cited by 19 · see citing works

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 18 · see citing works

Inhibition of the endocannabinoid-regulating enzyme monoacylglycerol lipase elicits a CB1 receptor-mediated discriminative stimulus in mice

Owens, R. A., Mustafa, M. A., Ignatowska-Jankowska, B. M., Damaj, M. I., Beardsley, P. M., Wiley, J. L., Niphakis, M. J., Cravatt, B. F., & Lichtman, A. H. (2017) · Neuropharmacology · doi:10.1016/j.neuropharm.2017.06.032 · Cited by 17 · see citing works

Cannabinoids and the Brain: The Effects of Endogenous and Exogenous Cannabinoids on Brain Systems and Function

Atkinson, D. L., & Abbott, J. K. (2017) · Elsevier eBooks · doi:10.1016/b978-0-12-804791-0.00003-3 · Cited by 16 · see citing works

Inhibition of 2-arachydonoylgycerol degradation attenuates orofacial neuropathic pain in trigeminal nerve-injured mice

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

Cannabinoids and agmatine as potential therapeutic alternatives for cisplatin-induced peripheral neuropathy

Dönertaş, B., Ünel, Ç. Ç., & Erol, K. (2018) · Journal of Experimental Pharmacology · doi:10.2147/jep.s162059 · Cited by 14 · see citing works

Behavioral Battery for Testing Candidate Analgesics in Mice. II. Effects of Endocannabinoid Catabolic Enzyme Inhibitors and ∆9-Tetrahydrocannabinol

Diester, C. M., Lichtman, A. H., & Negus, S. S. (2021) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.121.000497 · Cited by 13 · see citing works

Inhibition of 2-AG hydrolysis alleviates posttraumatic headache attributed to mild traumatic brain injury

Wen, J., Tanaka, M., & Zhang, Y. (2024) · The Journal of Headache and Pain · doi:10.1186/s10194-024-01817-z · Cited by 10 · see citing works

Cannabinoid CB1 Discrimination: Effects of Endocannabinoids and Catabolic Enzyme Inhibitors

Leonard, M. Z., Alapafuja, S. O., Ji, L., Shukla, V. G., Liu, Y., Nikas, S. P., Makriyannis, A., Bergman, J., & Kangas, B. D. (2017) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.117.244392 · Cited by 10 · see citing works

Effects of the Dual FAAH/MAGL Inhibitor AKU-005 on Trigeminal Hyperalgesia in Male Rats

Greco, R., Demartini, C., Francavilla, M., Zanaboni, A. M., Facchetti, S., Palmisani, M., Franco, V., & Tassorelli, C. (2024) · Cells · doi:10.3390/cells13100830 · Cited by 9 · see citing works

Impact of Δ9-Tetrahydrocannabinol on Rheumatoid Arthritis Synovial Fibroblasts Alone and in Co-Culture with Peripheral Blood Mononuclear Cells

Lowin, T., Kok, C., Smutny, S., & Pongratz, G. (2022) · Biomedicines · doi:10.3390/biomedicines10051118 · Cited by 10 · see citing works

Effects of Repeated Treatment with the Monoacylglycerol Lipase Inhibitor MJN110 on Pain-Related Depression of Nesting and Cannabinoid 1 Receptor Function in Male and Female Mice

Diester, C. M., Balint, H., Gillespie, J. C., Lichtman, A. H., Sim‐Selley, L. J., Selley, D. E., & Negus, S. S. (2024) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.123.001940 · Cited by 7 · see citing works

Synthesis and evaluation of carbamate derivatives as fatty acid amide hydrolase and monoacylglycerol lipase inhibitors

Jaiswal, S., Gupta, G., & Ayyannan, S. R. (2022) · Archiv der Pharmazie · doi:10.1002/ardp.202200081 · Cited by 6 · see citing works

Visceral Pain in Preterm Infants with Necrotizing Enterocolitis: Underlying Mechanisms and Implications for Treatment

ten Barge, J. A., van den Bosch, G. E., Slater, R., van den Hoogen, N. J., Reiss, I. K. M., & Simons, S. H. P. (2025) · Pediatric Drugs · doi:10.1007/s40272-024-00676-0 · Cited by 6 · see citing works

Endogenous Cannabinoids in Crohn’s Disease

Bochenek, M. S., Tomasik, J. T., Wędrychowicz, A., & Tomasik, P. (2024) · Applied Sciences · doi:10.3390/app14156646 · Cited by 5 · see citing works

Discriminative Stimulus Properties of the Endocannabinoid Catabolic Enzyme Inhibitor SA-57 in Mice

Owens, R. A., Ignatowska-Jankowska, B. M., Mustafa, M. A., Beardsley, P. M., Wiley, J. L., Jali, A. M., Selley, D. E., Niphakis, M. J., Cravatt, B. F., & Lichtman, A. H. (2016) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.115.229492 · Cited by 4 · see citing works

MAGL Inhibition Relieves Psoriasiform Inflammation and Pruritus Via Modulation of ALOX12-12-HETE Axis in Mice

Lin, S., Liu, X., Jiang, J., Ge, W., Tao, Q., Liu, S., Zhanmu, O., Yang, Y., Li, M., & Chen, H. (2026) · Inflammation · doi:10.1007/s10753-025-02383-5 · Cited by 3 · see citing works

Chronic intermittent ethanol produces nociception through endocannabinoid-independent mechanisms in mice

Miliano, C., Dong, Y., Proffit, M., Cabanas, N. C., Natividad, L. A., Buczynski, M. W., & Gregus, A. M. (2025) · Neuropharmacology · doi:10.1016/j.neuropharm.2025.110502 · Cited by 3 · see citing works

SGIP1 Deletion in Mice Attenuates Mechanical Hypersensitivity Elicited by Inflammation

Durydivka, O., Kuchař, M., & Blahoš, J. (2024) · Cannabis and Cannabinoid Research · doi:10.1089/can.2024.0020 · Cited by 2 · see citing works

Anti-nociceptive potential of an isatin-derived dual fatty acid amide hydrolase-monoacylglycerol lipase inhibitor

Jaiswal, S., Akhilesh, A., Tiwari, V., & Ayyannan, S. R. (2023) · Pharmacological Reports · doi:10.1007/s43440-023-00468-2 · Cited by 2 · see citing works

Stimulatory effect of monoacylglycerol lipase inhibitor MJN110 on locomotion and step kinematics demonstrated by high-precision 3D motion capture in micePreprint

Ignatowska-Jankowska, B. M., Özer, A. G., Kuck, A., Niphakis, M. J., Ogasawara, D., Cravatt, B. F., & Uusisaari, M. Y. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.06.25.546437 · Cited by 2 · see citing works

Effect of chronic upregulation of endocannabinoid signaling in vivo with JZL184 on striatal synaptic plasticity and motor learning in YAC128 Huntington disease micePreprint

Sepers, M. D., Woodard, C. L., Ramandi, D., Vecchiarelli, H. A., Hill, M. N., & Raymond, L. A. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.09.25.614804 · Cited by 2 · see citing works

Piezo channels in peripheral trigeminal nociception

Khan, S., Zafar, S., Tariq, T., & Seo, E. K. (2024) · Elsevier eBooks · doi:10.1016/b978-0-443-24705-7.00011-9 · Cited by 1 · see citing works

Synthesis and biological evaluation of methylene spacer incorporated 4-methylsulfonyl phenyl semicarbazones as dual FAAH-MAGL inhibitors

Jaiswal, S., & Ayyannan, S. R. (2025) · Phosphorus, sulfur, and silicon and the related elements · doi:10.1080/10426507.2025.2467438 · Cited by 1 · 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

Upregulation of endocannabinoid signaling in vivo restores striatal synaptic plasticity and motor performance in Huntington's disease mice

Sepers, M. D., Woodard, C. L., Ramandi, D., Vecchiarelli, H. A., Hill, M. N., & Raymond, L. A. (2025) · Journal of Huntington s Disease · doi:10.1177/18796397251337021 · Cited by 1 · see citing works

Effect of Cannabinoids and Stress on Motor Maps and Behaviour

Scullion, K. (2015) · Libraries and Cultural Resources (University of Calgary) · doi:10.11575/prism/25792

Discriminative Stimulus Properties of Endogenous Cannabinoid Degradative Enzyme Inhibitors

Owens, R. (2016) · VCU Scholars Compass (Virginia Commonwealth University) · doi:10.25772/h27y-zf33

Behavioral and Anti-inflammatory Effects of MAGL Inhibition in a Mouse Model of Inflammatory Arthritis

Steele, F. F. (2019) · doi:10.33915/etd.4114

Endocannabinoids in pain modulation

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

Additional file 2 of Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

Pietra, A. D., Krivoshein, G., Ivanov, K., Giniatullina, R., Jyrkkänen, H.-K., Leinonen, V., Lehtonen, M., van den Maagdenberg, A. M. J. M., Savinainen, J. R., & Giniatullin, R. A. (2024) · Figshare · doi:10.6084/m9.figshare.26580935

Additional file 1 of Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

Pietra, A. D., Krivoshein, G., Ivanov, K., Giniatullina, R., Jyrkkänen, H.-K., Leinonen, V., Lehtonen, M., van den Maagdenberg, A. M. J. M., Savinainen, J. R., & Giniatullin, R. A. (2024) · Figshare · doi:10.6084/m9.figshare.26580932

Additional file 3 of Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

Pietra, A. D., Krivoshein, G., Ivanov, K., Giniatullina, R., Jyrkkänen, H.-K., Leinonen, V., Lehtonen, M., van den Maagdenberg, A. M. J. M., Savinainen, J. R., & Giniatullin, R. A. (2024) · Figshare · doi:10.6084/m9.figshare.26580938

The Endocannabinoid System’s Contribution to Placebo AnalgesiaPreprint

Tomin, R., Murray, K., Hadjis, G. E., Khalil, O., Sexton, C. A., Bourke, S. L., Khan, J. S., Finn, D. P., Atlas, L. Y., & Moayedi, M. (2026) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2026.02.25.707676

BindingDB Entry 50011778: A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents.

BindingDB (2022) · UC San Diego · doi:10.7270/q2bc436z

BindingDB Entry 50001855: Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.

BindingDB (2020) · UC San Diego · doi:10.7270/q24f1t87

BindingDB Entry 50006982: N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.

BindingDB (2021) · UC San Diego · doi:10.7270/q2rx9gcw

Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase Inhibitors Produce Anti-Allodynic Effects in Mice Through Distinct Cannabinoid Receptor Mechanisms

Kinsey, S. G., Long, J. Z., Cravatt, B. F., & Lichtman, A. H. (2010) · The Journal of Pain · doi:10.1016/j.jpain.2010.04.001 · Cited by 118 · see citing works

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 · see citing works

Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain

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.109.155465 · Cited by 330 · see citing works

Blockade of Endocannabinoid-Degrading Enzymes Attenuates

Pain, N., 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)

Dual Fatty Acid Amide Hydrolase (FAAH) and Monoacylglycerol Lipase (MGL) Inhibitors Produce Ratio-Dependent Cannabinoid Activity In Vivo (Abstract ID: 225992)

Morrisson, D., Alafapuja, S. O., Nikas, S. P., Iliopoulos‐Tsoutsouvas, C., Georgiadis, M., Makriyannis, A., & Desai, R. I. (2026) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/j.jpet.2026.104278