title: Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target.
abstract: Receptor binding provides a valuable approach for characterization of drugs and their receptors. There are three major families of opioid receptors: mu, delta, and kappa. Highly selective radioligands are available for all three classes of traditional receptors. Of the three, the mu receptor undergoes extensive alternative splicing, generating a number of traditional mu receptor subtypes as well as a nontraditional, truncated set of variants associated with exon 11. These exon 11-associated truncated variants are not readily labeled with current radioligands. Here we describe the synthesis of a radioiodinated ligand suitable for carrying out binding studies for this target.
authors.affiliation: Department of Neurology and Molecular Pharmacology and Chemistry Program, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
authors.forename: Gina F
authors.initials: GF
authors.lastname: Marrone
authors.forename: Susruta
authors.initials: S
authors.lastname: Majumdar
authors.forename: Gavril W
authors.initials: GW
authors.lastname: Pasternak
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D005091:Exons / Q000235:genetics*; D007457:Iodine Radioisotopes / Q000378:metabolism*; D008024:Ligands; D051379:Mice; D009271:Naltrexone / Q000031:analogs & derivatives / Q000378:metabolism; D011485:Protein Binding; D017450:Receptors, Opioid, mu / Q000235:genetics* / Q000378:metabolism*
chemical_list: D007457:Iodine Radioisotopes; D008024:Ligands; D017450:Receptors, Opioid, mu; C570718:iodobenzoylnaltrexamide; D009271:Naltrexone