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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

Authors

Jeremy Shonberg

ROB LANE ROB.LANE@NOTTINGHAM.AC.UK
Associate Professor

Peter J Scammells

Ben Capuano



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