Chapter title |
Radioligand Binding Assay for an Exon 11-Associated Mu Opioid Receptor Target
|
---|---|
Chapter number | 16 |
Book title |
G Protein-Coupled Receptors in Drug Discovery
|
Published in |
Methods in molecular biology, January 2015
|
DOI | 10.1007/978-1-4939-2914-6_16 |
Pubmed ID | |
Book ISBNs |
978-1-4939-2913-9, 978-1-4939-2914-6
|
Authors |
Gina F. Marrone, Susruta Majumdar, Gavril W. Pasternak, Marrone, Gina F., Majumdar, Susruta, Pasternak, Gavril W. |
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. |
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