The DOI matches its Crossref record; 48 of the 48 references it cites were found in a registry or an index.
Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects
Open accessAbstract
2-Arachidonoylglycerol (2-AG) and anandamide are endocannabinoids that activate cannabinoid receptors CB1 and CB2. Endocannabinoid signaling is terminated by enzymatic hydrolysis, a process that, for anandamide, is mediated by fatty acid amide hydrolase (FAAH) and, for 2-AG, is thought to involve monoacylglycerol lipase (MAGL). FAAH inhibitors produce a select subset of the behavioral effects observed with CB1 agonists, intimating a functional segregation of endocannabinoid signaling pathways in vivo. Testing this hypothesis, however, requires specific tools to independently block anandamide and 2-AG metabolism. Here, we report a potent and selective inhibitor of MAGL, JZL184, that, upon administration to mice, raises brain 2-AG by 8-fold without altering anandamide. JZL184-treated mice exhibited a broad array of CB1-dependent behavioral effects, including analgesia, hypothermia, and hypomotility. These data indicate that 2-AG endogenously modulates several behavioral processes classically associated with the pharmacology of cannabinoids and point to overlapping and unique functions for 2-AG and anandamide in vivo.
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Cites
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Self-citationThe endogenous cannabinoid system controls extinction of aversive memories
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Self-citationEndocannabinoid Hydrolysis Generates Brain Prostaglandins That Promote Neuroinflammation
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Self-citationEmerging roles of lipid metabolism in cancer metastasis
Luo, X., Cheng, C., Tan, Z., Li, N., Tang, M., Yang, L., & Cao, Y. (2017) · Molecular Cancer · doi:10.1186/s12943-017-0646-3 · Cited by 677
Lipolysis – A highly regulated multi-enzyme complex mediates the catabolism of cellular fat stores
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Metadata
- Authors
- Long, J. Z., Li, W., Booker, L., Burston, J. J., Kinsey, S. G., Schlosburg, J. E., Pavón, F. J., Serrano, A. M., Selley, D. E., Parsons, L. H., Lichtman, A. H., & Cravatt, B. F.
- Venue
- Nature Chemical Biology
- Published
- 2008-11-23
- Volume
- 5
- Issue
- 1
- Pages
- 37-44
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- OpenAlex
- W2051554315
- Cited by
- 934
- References
- 48
- FWCI
- 34.56
- Type
- journal article
- Language
- en
- Open access
- green
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- Long, J. Z., Li, W., Booker, L., Burston, J. J., Kinsey, S. G., Schlosburg, J. E., Pavón, F. J., Serrano, A. M., Selley, D. E., Parsons, L. H., Lichtman, A. H., & Cravatt, B. F. (2009). Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects. Nature Chemical Biology. https://doi.org/10.1038/nchembio.129
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
