title: Assay of CB1 Receptor Binding.
abstract: Type-1 cannabinoid receptor (CB1), one of the main targets of endocannabinoids, plays a key role in several pathophysiological conditions that affect both 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 receptor-dependent human diseases.
authors.affiliation: Department of Experimental Medicine and Surgery, Tor Vergata University of Rome, via Montpellier 1, 00133, Rome, Italy.
authors.forename: Valeria M
authors.initials: VM
authors.lastname: Catani
authors.affiliation: Department of Experimental Medicine and Surgery, Tor Vergata University of Rome, via Montpellier 1, 00133, Rome, Italy. gasperi@med.uniroma2.it.
authors.forename: Valeria
authors.initials: V
authors.lastname: Gasperi
mesh_terms: D002478:Cells, Cultured; D055808:Drug Discovery; D057166:High-Throughput Screening Assays / Q000295:instrumentation / Q000379:methods; D006801:Humans; D007700:Kinetics; D008024:Ligands; D011485:Protein Binding; D011869:Radioligand Assay / Q000295:instrumentation / Q000379:methods*; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D008024:Ligands; D043884:Receptor, Cannabinoid, CB1
keywords: CP55.940; Filtration assay; Radioligand-receptor binding; SR141716; Type-1 cannabinoid receptor