Abstract
Type-1 cannabinoid receptor (CB1), one of the main targets of endocannabinoids, plays a key role in several pathophysiological conditions that affect both the central nervous system and peripheral tissues. Today, its biochemical identification and pharmacological characterization, as well as the screening of thousands of novel ligands that might be useful for developing CB1-based therapies, are the subject of intense research. Among available techniques that allow the analysis of CB1 binding activity, radioligand-based assays represent one of the best, fast, and reliable methods.
Here, we describe radioligand binding methods standardized in our laboratory to assess CB1 binding in both tissues and cultured cells. We also report a high-throughput radioligand binding assay that allows to evaluate efficacy and potency of different compounds, which might represent the basis for the development of new drugs that target CB1-dependent human diseases.
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References
Matsuda LA, Lolait SJ, Brownstein MJ et al (1990) Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 346:561–564
Tantimonaco M, Ceci R, Sabatini S et al (2014) Physical activity and the endocannabinoid system: an overview. Cell Mol Life Sci 71:2681–2698
Pertwee RG, Howlett AC, Abood ME et al (2010) International union of basic and clinical pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB1 and CB2. Pharmacol Rev 62:588–631
Howlett AC, Abood ME (2017) CB1 and CB2 receptor pharmacology. Adv Pharmacol 80:169–206
Gasperi V, Evangelista D, Savini I et al (2015) Downstream effects of endocannabinoid on blood cells: implications for health and disease. Cell Mol Life Sci 72:3235–3252
O’Sullivan SE, Yates AS, Porter RK (2021) The peripheral cannabinoid receptor type 1 (CB1) as a molecular target for modulating body weight in man. Molecules 26:6178
Winters BL, Vaughan CW (2021) Mechanisms of endocannabinoid control of synaptic plasticity. Neuropharmacology 197:108736
Pucci M, Zaplatic E, Micioni Di Bonaventura MV et al (2021) On the role of central type-1 cannabinoid receptor gene regulation in food intake and eating behaviors. Int J Mol Sci 22:398
Miralpeix C, Reguera AC, Fosch A et al (2021) Hypothalamic endocannabinoids in obesity: an old story with new challenges. Cell Mol Life Sci 31:1–22
Cecconi S, Rapino C, Di Nisio V et al (2020) The (endo)cannabinoid signaling in female reproduction: what are the latest advances? Prog Lipid Res 77:101019
Mechoulam R, Parker LA (2013) The endocannabinoid system and the brain. Annu Rev Psychol 64:21–47
Gatta-Cherifi B, Cota D (2016) New insights on the role of the endocannabinoid system in the regulation of energy balance. Int J Obes 40:210–219
Rinaldi-Carmona M, Barth F, Héaulme M et al (1994) SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350:240–244
Sink KS, McLaughlin PJ, Wood JAT et al (2008) The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats. Neuropsychopharmacology 33:946–955
Dow RL, Carpino PA, Hadcock JR et al (2009) Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2 H -pyrazolo[3,4- f ][1,4]oxazepin-8(5 H )-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. J Med Chem 52:2652–2655
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© 2023 The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature
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Gasperi, V., Savini, I., Catani, M.V. (2023). Assay of CB1 Receptor Binding. In: Maccarrone, M. (eds) Endocannabinoid Signaling. Methods in Molecular Biology, vol 2576. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-2728-0_7
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DOI: https://doi.org/10.1007/978-1-0716-2728-0_7
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