Targeting the endocannabinoid system: to enhance or reduce?

The Endocannabinoid System as an Emerging Target of Pharmacotherapy

Pacher, P., Bátkai, S., & Kunos, G. (2006) · Pharmacological Reviews · doi:10.1124/pr.58.3.2 · Cited by 2,077

The endogenous cannabinoid system controls extinction of aversive memories

Marsicano, G., Wotjak, C. T., Azad, S. C., Bisogno, T., Rammes, G., Cascio, M. G., Hermann, H., Tang, J., Hofmann, C., Zieglgänsberger, W., et al. (2002) · Nature · doi:10.1038/nature00839 · Cited by 1,728

The orphan receptor GPR55 is a novel cannabinoid receptor

Ryberg, E., Larsson, N., Sjögren, S., Hjorth, S., Hermansson, N., Leonova, J., Elebring, T., Nilsson, K., Drmota, T., & Greasley, P. J. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707460 · Cited by 1,568

Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia

Després, J.-P., Golay, A., & Sjöström, L. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa044537 · Cited by 1,392

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

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

Endocannabinoid-mediated rescue of striatal LTD and motor deficits in Parkinson's disease models

Kreitzer, A. C., & Malenka, R. C. (2007) · Nature · doi:10.1038/nature05506 · Cited by 735

Cannabinoid-based drugs as anti-inflammatory therapeutics

Klein, T. W. (2005) · Nature Reviews Immunology · doi:10.1038/nri1602 · Cited by 728

Regulation of bone mass, bone loss and osteoclast activity by cannabinoid receptors

Idris, A. I., van 't Hof, R. J., Greig, I. R., Ridge, S. A., Baker, D., Ross, R. A., & Ralston, S. H. (2005) · Nature Medicine · doi:10.1038/nm1255 · Cited by 356

Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin‐like activity

De Petrocellis, L., Bisogno, T., Davis, J. B., Pertwee, R. G., & Di Marzo, V. (2000) · FEBS Letters · doi:10.1016/s0014-5793(00)02082-2 · Cited by 347

Cannabinoids and the expanded endocannabinoid system in neurological disorders

Cristino, L., Bisogno, T., & Di Marzo, V. (2020) · Nature Reviews Neurology · doi:10.1038/s41582-019-0284-z · Cited by 970

The endocannabinoid system links gut microbiota to adipogenesis

Muccioli, G. G., Naslain, D., Bäckhed, F., Reigstad, C. S., Lambert, D. M., Delzenne, N. M., & Cani, P. D. (2010) · Molecular Systems Biology · doi:10.1038/msb.2010.46 · Cited by 691

The Endocannabinoid System and Pain

Guindon, J., & Hohmann, A. (2009) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/187152709789824660 · Cited by 476

Emerging strategies for exploiting cannabinoid receptor agonists as medicines

Pertwee, R. G. (2009) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2008.00048.x · Cited by 436

Bioactive Lipids and Chronic Inflammation: Managing the Fire Within

Chiurchiù, V., Leuti, A., & Maccarrone, M. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2018.00038 · Cited by 427

Strategies for Discovering and Derisking Covalent, Irreversible Enzyme Inhibitors

Johnson, D. S., Weerapana, E., & Cravatt, B. F. (2010) · Future Medicinal Chemistry · doi:10.4155/fmc.10.21 · Cited by 387

Chemical Probes of Endocannabinoid Metabolism

Blankman, J. L., & Cravatt, B. F. (2013) · Pharmacological Reviews · doi:10.1124/pr.112.006387 · Cited by 327

Identification of intracellular carriers for the endocannabinoid anandamide

Kaczocha, M., Glaser, S. T., & Deutsch, D. G. (2009) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0901515106 · Cited by 326

Phytocannabinoids as novel therapeutic agents in {CNS} disorders.

Hill, A. J., Williams, C. M., Whalley, B. J., & Stephens, G. J. (2012) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2011.09.002 · Cited by 312

The Endocannabinoid System: A Potential Target for the Treatment of Various Diseases

Lowe, H., Toyang, N., Steele, B., Bryant, J., & Ngwa, W. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22179472 · Cited by 303

Cannabidiol exerts sebostatic and antiinflammatory effects on human sebocytes

Oláh, A., Tóth, B. I., Borbíró, I., Sugawara, K., Szöllõsi, A. G., Czifra, G., Pál, B., Ambrus, L., Kloepper, J., Camera, E., et al. (2014) · Journal of Clinical Investigation · doi:10.1172/jci64628 · Cited by 268

Endocannabinoids in Amygdala and Nucleus Accumbens Mediate Social Play Reward in Adolescent Rats

Trezza, V., Damsteegt, R., Manduca, A., Petrosino, S., Van Kerkhof, L. W. M., Pasterkamp, R. J., Zhou, Y., Campolongo, P., Cuomo, V., Di Marzo, V., et al. (2012) · The Journal of Neuroscience · doi:10.1523/jneurosci.0114-12.2012 · Cited by 190

Phytocannabinoids beyond the Cannabis plant – do they exist?

Gertsch, J., Pertwee, R. G., & Di Marzo, V. (2010) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2010.00745.x · Cited by 188

A catalytically silent FAAH-1 variant drives anandamide transport in neurons

Fu, J., Bottegoni, G., Sasso, O., Bertorelli, R., Rocchia, W., Masetti, M., Guijarro, A., Lodola, A., Armirotti, A., Garau, G., et al. (2012) · Nature Neuroscience · doi:10.1038/nn.2986 · Cited by 175

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

Motion Sickness, Stress and the Endocannabinoid System

Choukèr, A., Kaufmann, I., Kreth, S., Hauer, D., Feuerecker, M., Thieme, D., Vogeser, M., Thiel, M., & Schelling, G. (2010) · PLoS ONE · doi:10.1371/journal.pone.0010752 · Cited by 140

In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML 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

A Reversible and Selective Inhibitor of Monoacylglycerol Lipase Ameliorates Multiple Sclerosis

Hernández‐Torres, G., Cipriano, M., Hedén, E., Björklund, E., Canales, Á., Zian, D., Feliú, A., Mecha, M., Guaza, C., Fowler, C. J., et al. (2014) · Angewandte Chemie International Edition · doi:10.1002/anie.201407807 · Cited by 125

Opposing Roles for Cannabinoid Receptor Type-1 (CB1) and Transient Receptor Potential Vanilloid Type-1 Channel (TRPV1) on the Modulation of Panic-Like Responses in Rats

Casarotto, P. C., Terzian, A. L. B., Aguiar, D. C., Zangrossi, H., Guimarães, F. S., Wotjak, C. T., & Moreira, F. A. (2012) · Neuropsychopharmacology · doi:10.1038/npp.2011.207 · Cited by 117

Enzymological studies on the biosynthesis of N-acylethanolamines

Ueda, N., Tsuboi, K., & Uyama, T. (2010) · Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids · doi:10.1016/j.bbalip.2010.08.010 · Cited by 112

Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin

Leonti, M., Casu, L., Raduner, S., Cottiglia, F., Floris, C., Altmann, K.-H., & Gertsch, J. (2010) · Biochemical Pharmacology · doi:10.1016/j.bcp.2010.02.015 · Cited by 95

Chapter 5 The Endocannabinoid System as A Target for Novel Anxiolytic and Antidepressant Drugs

Gaetani, S., Dipasquale, P., Romano, A., Righetti, L., Cassano, T., Piomelli, D., & Cuomo, V. (2009) · International Review of Neurobiology · doi:10.1016/s0074-7742(09)85005-8 · Cited by 83

Effects of parabolic flight and spaceflight on the endocannabinoid system in humans

Strewe, C., Feuerecker, M., Nichiporuk, I., Kaufmann, I., Hauer, D., Morukov, B., Schelling, G., & Choukèr, A. (2012) · Reviews in the Neurosciences · doi:10.1515/revneuro-2012-0057 · Cited by 63

Modulation of the anti‐nociceptive effects of 2‐arachidonoyl glycerol by peripherally administered FAAH and MGL inhibitors in a neuropathic pain model

Desroches, J., Guindon, J., Lambert, C., & Beaulieu, P. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.322 · Cited by 63

TRPV1 and Endocannabinoids: Emerging Molecular Signals that Modulate Mammalian Vision

Ryskamp, D., Redmon, S., Jo, A., & Križaj, D. (2014) · Cells · doi:10.3390/cells3030914 · Cited by 60

Modulation of defensive behavior by transient receptor potential vanilloid type-1 (TRPV1) channels

Aguiar, D. C., Moreira, F. A., Terzian, A. L., Fogaça, M. V., Lisboa, S. F., Wotjak, C. T., & Guimaraes, F. S. (2014) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2014.03.026 · Cited by 57

Induction of SIRT1 by melatonin improves alcohol‐mediated oxidative liver injury by disrupting the CRBN‐YY1‐CYP2E1 signaling pathway

Lee, S., Koh, H., Joo, D. J., Nedumaran, B., Jeon, H., Park, C., Harris, R. A., & Kim, Y. D. (2020) · Journal of Pineal Research · doi:10.1111/jpi.12638 · Cited by 48

Cannabinoids in Chronic Pain: Therapeutic Potential Through Microglia Modulation

van den Hoogen, N. J., Harding, E. K., Davidson, C. E. D., & Trang, T. (2022) · Frontiers in Neural Circuits · doi:10.3389/fncir.2021.816747 · 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

Modulation of anxiety-like behavior by the endocannabinoid 2-arachidonoylglycerol (2-AG) in the dorsolateral periaqueductal gray

Almeida-Santos, A. F., Gobira, P. H., Rosa, L. C., Guimaraes, F. S., Moreira, F. A., & Aguiar, D. C. (2013) · Behavioural Brain Research · doi:10.1016/j.bbr.2013.05.027 · Cited by 41