Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor

Shonberg, Jeremy; Lane, J. Robert; Scammells, Peter J; Capuano, Ben

Abstract

Bivalent ligands represent useful tools to investigate the phenomenon of GPCR dimerization. We synthesized bivalent ligands based on (R)-apomorphine with variations in spacer length, and assessed these compounds in functional and binding assays at the dopamine D2 receptor. The results present novel SAR for bivalent ligands targeting the D2R, and identify a relationship for spacer length with ligand potency, efficacy and affinity. © The Royal Society of Chemistry.

Citation

Shonberg, J., Lane, J. R., Scammells, P. J., & Capuano, B. (2013). Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor. MedChemComm, 4(9), 1290-1296. https://doi.org/10.1039/c3md00154g

• Journal Article Type: Article
• Acceptance Date: Jul 16, 2013
• Online Publication Date: Jul 18, 2013
• Publication Date: Jan 1, 2013
• Deposit Date: Apr 22, 2020
• Journal: MedChemComm
• Print ISSN: 2040-2503
• Electronic ISSN: 2040-2511
• Publisher: Royal Society of Chemistry
• Peer Reviewed: Peer Reviewed
• Volume: 4
• Issue: 9
• Pages: 1290-1296
• DOI: https://doi.org/10.1039/c3md00154g
• Public URL: http://xlink.rsc.org/?DOI=c3md00154g
• Publisher URL: https://pubs.rsc.org/en/content/articlelanding/2013/md/c3md00154g#!divAbstract